Search Result
Results for "
tumor
" in MedChemExpress (MCE) Product Catalog:
4584
Inhibitors & Agonists
131
Biochemical Assay Reagents
115
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W460407
-
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1,2-Dimethylhydrazine dihydrochloride
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Biochemical Assay Reagents
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Cancer
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N,N'-Dimethylhydrazine (1,2-Dimethylhydrazine) dihydrochloride is a tumor inducer that induces colon tumors in rodents .
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-
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- HY-P99157
-
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CD276/B7-H3
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Cancer
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Omburtamab is a humanized monoclonal antibody targeting B7-H3 (CD276). Omburtamab selectively binds to B7-H3 highly expressed on the surface of tumor cells and activates anti-tumor immune responses mediated by T cells and natural killer (NK) cells. Omburtamab can promote the specific infiltration of CAR-T cells into tumors, enhance the killing function of NK cells through the CD16 signaling pathway, and regulate tumor cell glucose metabolism (such as inhibiting the Warburg effect). Omburtamab has the potential to inhibit solid tumors such as non-small cell lung cancer (NSCLC) .
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- HY-P2526
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LyP-1
2 Publications Verification
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Complement System
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Cancer
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LyP-1 is a cyclic 9‐amino‐acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
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-
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- HY-P3707
-
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Apoptosis
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Cancer
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Tumor targeted pro-apoptotic peptide (CNGRC-GG-D(KLAKLAK)2) is an anti-tumor peptide. Tumor targeted pro-apoptotic peptide disrupts mitochondrial membranes and promotes apoptosis, showing anticancer activity in mice .
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-
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- HY-19459A
-
-
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- HY-W854385
-
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SLeA
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Biochemical Assay Reagents
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Cancer
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Sialyl Lewis A (SLeA) is a carbohydrate-type antigen that can serve as a tumor marker, with upregulation observed in various tumor cells such as cervical cancer, human pancreatic cancer, and colon cancer cells. Sialyl Lewis A is involved in the migration and adhesion of tumor cells. Additionally, elevated expression of Sialyl Lewis A may also lead to pregnancy abnormalities .
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- HY-155523
-
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Microtubule/Tubulin
HDAC
Apoptosis
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Cancer
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Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with an IC50 of 0.403 μM, 0.591μM, 3.552μM, 0.459μM for HDAC1/2/3/6. Tubulin/HDAC-IN-2 blocks cell cycle arrest at G2 phase, induces cell apoptosis. Tubulin/HDAC-IN-2 inhibits the growth of hematoma and solid tumor cells, reduces tumor metastasis, and also inhibits tumor growth in a liver tumor allograft mouse model .
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- HY-P4111
-
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CXCR
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Cancer
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Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research .
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-
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- HY-P10295
-
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MDM-2/p53
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Cancer
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p53 (232-240) is a peptide segment of the 232-240 amino acid sequence of the human tumor suppressor protein p53. p53 (232-240) enhances its binding affinity to the Major histocompatibility complex (MHC), thereby enhancing the immunogenicity of this peptide to enhance the immune system's response to tumor antigens. p53 (232-240) can be used in the development of cancer vaccines and in the study of tumor cell recognition and clearance by the immune system .
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- HY-P2040
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Phosphatase
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Cancer
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Nodularin is a potent hepatotoxin, tumor promoter, and protein phosphatase inhibitor .
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- HY-P4998
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Biochemical Assay Reagents
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Cancer
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Chemotactic Domain of Elastin is an elastin-derived peptide with chemotactic effects on certain tumor cells, such as M27 tumor cells. Chemotactic Domain of Elastin can be used in cancer research .
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- HY-160843
-
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Apoptosis
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Cancer
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N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
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- HY-136538
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Survivin
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Cancer
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LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors .
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- HY-137724
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Cyclic-di-IMP
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STING
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Cancer
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C-di-IMP (Cyclic-di-IMP) is a STING agonist. C-di-IMP can be used for the research of tumor .
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- HY-W665796
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Drug Derivative
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Cancer
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N-Methyl-N-nitroso-2-propanamine is an N-nitrosamine, which induces tumor formation in mice .
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- HY-160768
-
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Deubiquitinase
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Inflammation/Immunology
Cancer
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OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) .
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- HY-105172A
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CAP-232 TFA; TLN-232 TFA
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Somatostatin Receptor
Apoptosis
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Cancer
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TT-232 TFA (CAP-232 TFA) is an analogue of somatostatin. TT-232 TFA can induce apoptosis of pancreatic tumor cell lines, inhibit tyrosine kinase activity and stimulate tyrosine phosphatase activity in colon tumor cell lines. TT-232 TFA inhibits the proliferation of tumor cells, induces apoptosis of tumor cells and shows strong anti-tumor effects. TT-232 TFA can be used in the development of anti-tumor drugs and the study of apoptosis mechanism .
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- HY-153638
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Phosphatase
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Cancer
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PTPN2/1-IN-2 is a PTPN2/1 antagonist that can be used in various tumor research .
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- HY-N15176
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DNA/RNA Synthesis
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Cancer
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Bisucaberin is a natural siderophore, is a DNA synthesis inhibitor. Bisucaberin shows cytostasis for tumor cells. Bisucaberin sensitizes tumor cells to macrophage-mediated cytolysis .
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- HY-P4091A
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Biochemical Assay Reagents
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Cancer
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LSD acetate is a peptide. LSD acetate can specifically recognize the lymphatics of C8161 melanoma, but it does not bind to the lymphatics of normal tissues or tumor blood vessels. When conjugated with a proapoptotic peptide, LSD acetate can reduce the number of tumor lymphatics. LSD acetate can be used in the research of targeted therapy and diagnosis of tumor lymphatics .
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- HY-P4091
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Biochemical Assay Reagents
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Cancer
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LSD is a peptide. LSD can specifically recognize the lymphatics of C8161 melanoma, but it does not bind to the lymphatics of normal tissues or tumor blood vessels. When conjugated with a proapoptotic peptide, LSD can reduce the number of tumor lymphatics. LSD can be used in the research of targeted therapy and diagnosis of tumor lymphatics .
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- HY-156363
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Ras
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Cancer
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K-Ras-IN-2 (Compound CHI-000-667) is a K-Ras antagonist, and can be used for tumor research .
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- HY-139586
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MK-1454
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STING
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Cancer
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Ulevostinag (MK-1454) is a potent cyclic dinucleotide agonist stimulator of interferon genes (STING). Ulevostinag (MK-1454) acts in the intra-tumoral route by targeting the stimulator of interferon genes (STING) protein. Ulevostinag (MK-1454) can be used for immuno-tumor cancer disease research .
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- HY-144038
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DNA-PK
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Cancer
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DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2) .
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- HY-144039
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DNA-PK
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Cancer
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DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6) .
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- HY-D2281
-
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FAP
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Cancer
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FAP Ligand 2, a FAPI-46 derivative, is a specific fibroblast activation protein (FAP)-targeted tracer. FAP Ligand 2 exhibits good tumor uptake and acts as a promising molecular tracer for FAP tumor imaging .
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- HY-160406
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STING
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Cancer
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SNX281 is a systemically active STING agonist that binds to the STING protein, promotes signal transduction of the cGAS-STING pathway, and increases cellular responses to tumor cells. SNX281 can be used in the study of anti-tumor immunity .
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- HY-157847
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STAT
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Cancer
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Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .
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- HY-172150
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Biochemical Assay Reagents
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Cancer
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XH02 is a compound based on L6 modification. XH02 ( 177Lu labeled) displays exceptional tumor growth inhibition in BxPC-3 tumors .
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- HY-P99489
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ABBV 181; PR 1648817
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PD-1/PD-L1
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Inflammation/Immunology
Cancer
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Budigalimab (ABBV 181; PR 1648817) is a humanized, recombinant IgG1 monoclonal antibody targeting programmed cell death 1 (PD-1) receptor. Budigalimab has an Fc mutation that reduces the inhibition of Fc receptor interactions and effector factors. Budigalimab can block the binding of PD-1 and PD-L1, which has anti-tumor activity. Budigalimab can be used in the study of solid tumors .
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- HY-151559
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Checkpoint Kinase (Chk)
STAT
CXCR
CCR
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Cancer
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Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .
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- HY-115514A
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BRK
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Cancer
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BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
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- HY-13546
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MMP
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Cancer
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ABT-518 is a matrix metalloproteinase inhibitor with anti-tumor activity. ABT-518 has potent inhibitory effects on gelatinase A and gelatinase B, which can inhibit tumor growth and metastasis .
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- HY-12710
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α-Yohimbine; Corynanthidine; Isoyohimbine
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Adrenergic Receptor
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Cancer
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Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis .
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- HY-159045
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p-Fluoro-SAHA
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HDAC
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Cancer
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F-SAHA is a HDAC inhibitor (HDACi) and its 18F labeled derivative can be used in tumor imaging research .
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- HY-117412
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Drug Derivative
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Cancer
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KCG 1 is a potent and selective anti-tumor agent that displays anti-prollferative and cytotoxic effects on epithelial tumoral cells .
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- HY-153243
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c-Fms
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Cancer
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IACS-9439 is a potent, selective, and orally active CSF1R inhibitor with a Ki value of 1 nM inhibitor. IACS-9439 can be used for advanced solid tumors research .
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- HY-127118
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Pteroyltriglutamic
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Drug Metabolite
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Cancer
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Pteropterin (Pteroyltriglutamic) is an active form of folate. Pteropterin shows inhibiting effect on tumor growth and has broad anticancer activity .
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- HY-127118A
-
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Pteroyltriglutamic monohydrate
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Drug Metabolite
Folate Receptor (FR)
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Cancer
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Pteropterin (Pteroyltriglutamic) monohydrate is an active form of folate. Pteropterin monohydrate shows inhibiting effect on tumor growth and has broad anticancer activity .
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- HY-149969
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Estrogen Receptor/ERR
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Cancer
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ER degrader 4 is a selective and orally active estrogen receptor degrader. ER degrader 4 has anti-tumor activity .
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- HY-107665
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NF-κB
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Cancer
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Ro 106-9920 is a potent inhibitor of NF-kappaB. Ro 106-9920 has the potential for the research of tumor and cancer diseases .
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- HY-P10679
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MMP
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Cancer
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GPLGLAGGWGERDGS is a peptide with MMP enzyme responsiveness and tumor targeting function, which can be used to monitor enzyme-guided nanoparticle assembly in tumors .
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- HY-N10673
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Others
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Cancer
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10α-Hydroxyepigambogic acid can be extracted from Garcinia hanburyi. 10α-Hydroxyepigambogic acid can be used in the research of tumors .
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- HY-137457A
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IDX-1197 hydrochloride
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PARP
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Cancer
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Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research .
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-
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- HY-P10284
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Interleukin Related
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Cancer
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S7 is an IL-6 receptor antagonist and inhibits the binding between IL-6 and IL-6R. S7 can inhibit angiogenesis and tumor growth .
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- HY-N12516
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Others
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Cancer
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Ginsenoside Mc is a natural product, that can be prepared by removal of two glucose molecules at 3-C of ginsenoside Rc (HY-N0042). Ginsenoside Mc has anti-tumor activity .
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- HY-16129
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Calmodulin
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Cancer
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CBP-501 is a cell-permeable and calmodulin-binding peptide that enhances the influx of platinum agents into tumor cells and tumor immunogenicity. CBP-501 can be utilized in cancer research .
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- HY-169017
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Toll-like Receptor (TLR)
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Cancer
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MTT5 is a toll-like receptor 7 (TLR7) agonist. MTT5 can couple with Deruxtecan (HY-13631E) and exert anti-tumor activity in HER2 positive solid tumors through tumor cell killing and immune activation .
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- HY-112243
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- HY-112243A
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- HY-156881
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Poly(ADP-ribose) Glycohydrolase (PARG)
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Cancer
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PARG-IN-4 (Formula (A)) is an orally active and cell-permeable PARG inhibitor. PARG-IN-4 effectively inhibits tumor growth in mouse models. PARG-IN-4 can be used in cancer research .
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- HY-119846
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Others
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Cancer
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Afromosin is an isoflavone, that can be isolated from Millettia dielsiana Harms. Afromosin exhibits remarkable tumor inhibitory effects .
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- HY-P99708
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ABBV-151; ARGX-115
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TGF-beta/Smad
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Cancer
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Livmoniplimab (ABBV-151) is a monoclonal antibody against GARP/TGF-β1 that can inhibit the release of active TGF-β1. Livmoniplimab has anti-tumor activity in colon cancer mice. Livmoniplimab can be used for the study of locally advanced or metastatic solid tumors .
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- HY-N7000R
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- HY-131991
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DNA Methyltransferase
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Cancer
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Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC50 of 8.4 µM .
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- HY-159129
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Ser/Thr Protease
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Cancer
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hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsin B, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
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- HY-P99523
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AMG 199
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CD3
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Cancer
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Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on T cells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces T cell activation and proliferation .
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- HY-117737A
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Raf
Apoptosis
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Cancer
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RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities .
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- HY-P99887
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JTX-4014
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PD-1/PD-L1
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Cancer
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Pimivalimab (JTX-4014) is a PD-1 inhibitor. Pimivalimab can be used for the research of solid tumor .
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- HY-105529
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(+)-Indicine N-oxide; NSC 132319
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Microtubule/Tubulin
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Cancer
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Indicine N-oxide (NSC 132319), a pyrrolizidine alkaloid, is an antitumor agent for pediatric cancer and solid tumors research .
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- HY-155003
-
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Fluorescent Dye
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Cancer
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TPEQM-DMA is a NIR-II photosensitizer. TPEQM-DMA accumulates in cancerous mitochondria, and inhibits cancer cell growth. TPEQM-DMA has potent type-I phototherapeutic efficacy to overcome the intrinsic pitfalls of PDT in combating hypoxic tumors .
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- HY-149081
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Estrogen Receptor/ERR
Cytochrome P450
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Cancer
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ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
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- HY-P2028
-
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GnRH Receptor
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Cancer
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BIM 21009 is a LHRH and GnRH receptor antagonist. BIM 21009 inhibits tumor growth .
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- HY-P34013
-
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Ser/Thr Protease
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Cancer
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Urinary Trypsin Inhibitor Fragment is a fragment derived from urinary trypsin inhibitor by proteolysis. Urinary Trypsin Inhibitor Fragment can inhibit tumor cell invasion by limited proteolysis .
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- HY-133800
-
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Biochemical Assay Reagents
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Cancer
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Volvaltrate B is an anticancer agent, iridoid, can be obtained from the root of valerian (Valeriana officinalis). Volvaltrate B is effective against ovarian tumors in female mice. Volvaltrate B has the potential to study cancer .
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- HY-149413
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RET
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Others
Cancer
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FHND5071 is a potent and selective RET kinase inhibitor, FHND5071 can exert antitumor effects by inhibiting RET autophosphorylation. FHND5071 can be used for tumor diseases research .
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- HY-132129
-
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Ras
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Cancer
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SOS1-IN-2 (Compound 1-1) is an inhibitor of SOS1 with an IC50 value of 5 nM. SOS1-IN-2 can be used in tumor research .
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- HY-B0291
-
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Parasite
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Infection
Cancer
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Oxfendazole is a sulfoxide form of fenbendazole that is effective when taken orally. Oxfendazole fights parasites and has tumor-promoting activity .
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- HY-128890B
-
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ADC Linker
Biochemical Assay Reagents
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Cancer
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DOTA-NHS-ester (TFA) is used as a linker for affibody molecules, and it can be employed in small animal positron emission tomography (PET), single photon emission computed tomography (SPECT), and CT scanning. DOTA-NHS-ester can be used to label radiotracers or imaging probes for tumor detection .
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- HY-13479
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HSP
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Cancer
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EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases . EC144 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-169084
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Glycosyltransferase
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Cancer
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ST-IN-1 (compound (R)-1) is a selective ST inhibitor (Ki=70 nM, rat a-2,6-ST; Ki=19 nM, hST6GAL1) with antitumor activity. ST-IN-1 inhibits tumor growth and metastasis by delipidating the surface of tumor cells .
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- HY-P991149
-
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TNF Receptor
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Cancer
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Nesfrotamig is a humanized immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2) and human tumor necrosis factor receptor superfamily member 9 (TNFRSF9). Nesfrotamig is promising for research of cancers, especially in ERBB2-positive related tumor diseases, such as breast cancer and gastric cancer .
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- HY-136927
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STING
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Inflammation/Immunology
Cancer
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MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
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- HY-15260C
-
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BMS-863233 hydrochloride
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CDK
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Cancer
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XL413 (BMS-863233) hydrochloride is an orally active and selective CDC7 inhibitor (IC50=3.4 nM). XL413 hydrochloride has favorable pharmacokinetic profiles and significantly inhibits tumor growth in rodent models. XL413 hydrochloride can be used in cancer research .
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- HY-P9978
-
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PD-1/PD-L1
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Cancer
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Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma .
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- HY-154927
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Liposome
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Cancer
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DSPE-PEG-Cy5 is an ammoniated reagent that can be used for the preparation of tumor-targeting vectors .
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-
- HY-133887
-
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Antifolate
DNA/RNA Synthesis
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Cancer
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Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent .
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-
- HY-P3441
-
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FAP
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Cancer
|
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3BP-4089 is a highly potent fibroblast activation protein (FAP)-targeting peptide for theranostics. 3BP-4089 is often coupled with radionuclides for tumor diagnosis and research .
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-
- HY-163965
-
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Toll-like Receptor (TLR)
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Cancer
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Antitumor agent-185 (compound 3) shows antitumor activity that could effectively reduce the growth of tumors and prolong the survival time of mice in vivo .
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-
- HY-N3055
-
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Apoptosis
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Cancer
|
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Pinusolide is a known platelet-activating factor (PAF) receptor binding antagonist. Pinusolide not only decreases the proliferation activity of tumor cells but specifically induces apoptosis .
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-
- HY-106263A
-
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Apoptosis
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Cancer
|
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Tyroserleutide TFA, isolated from the degradation products of porcine spleen , is a small molecular tripeptide which inhibits tumor growth both in vitro and in vivo .
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-
- HY-N0984
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Diacetylvilasinin
|
Drug Intermediate
|
Cancer
|
|
1,3-Diacetylvilasinin (Diacetylvilasinin), a bioactive Triterpenoid from Melia volkensii, shows marginal cytotoxicities against certain human tumor cell lines .
|
-
- HY-163545
-
|
|
Drug Derivative
|
Cancer
|
|
Tc-Me2P is a 99MTC-labeled acrylamide (PnAO) derivative that contains two 4-methyl-2-nitroimidazole groups. The primary activity of Tc-Me2P is as an imaging agent for tumor hypoxia. By specifically binding to hypoxic regions in tumor tissue, it can be used for single photon emission computed tomography (SPECT) and positron emission tomography (PET) imaging to detect hypoxia in tumors. Tc-Me2P can be used to study the targeting of different chemical structures in tumors and normal tissues .
|
-
- HY-137331
-
FAPI-46
1 Publications Verification
|
FAP
|
Cancer
|
|
FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted tracer. Use radioactivity FAPI-46 labeled with 68Ga or 177Lu can be used for tumor imaging in a variety of cancers and has higher tumor uptake rates and longer tumor accumulation .
|
-
- HY-161111
-
|
|
Ser/Thr Kinase
|
Cancer
|
|
KVS0001 is a potent inhibitor of SMG1 and nonsense mediated decay (NMD) that has anti-tumor activity .
|
-
- HY-147594
-
|
|
CD73
|
Cancer
|
|
CD73-IN-13 is a potent inhibitor of CD73. CD73 is closely associated with tumor growth, angiogenesis and metastasis. CD73-IN-13 be used for preparing a medicament for tumor-related diseases (extracted from patent CN114437039A, compound 7) .
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-
- HY-153450
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
|
-
- HY-124617A
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells . Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines .
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-
- HY-P3441A
-
|
|
FAP
|
Cancer
|
|
3BP-4089 TFA is a highly potent fibroblast activation protein (FAP)-targeting peptide for theranostics. 3BP-4089 TFA is often coupled with radionuclides for tumor diagnosis and research .
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-
- HY-148517
-
AZD0095
2 Publications Verification
|
Monocarboxylate Transporter
|
Cancer
|
|
AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .
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-
- HY-118942
-
|
ARC 111
|
Topoisomerase
|
Cancer
|
|
Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells .
|
-
- HY-116098
-
|
AL-4940
|
Biochemical Assay Reagents
|
Cancer
|
|
Anecortave desacetate (AL-4940) is an angiogenesis inhibitor. Anecortave is indicated for the study of exudative (wet) age-related macular degeneration as well as retinal tumors .
|
-
- HY-N4306
-
|
|
Others
|
Cancer
|
|
Sarracenin is a iridoid isolated from roots and rhizomes of Patrinia heterophylla. Sarracenin shows cytotoxic activities against tumor cells .
|
-
- HY-106263B
-
|
|
PTEN
PDK-1
MDM-2/p53
Apoptosis
Akt
|
Cancer
|
|
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .
|
-
- HY-N0462
-
-
- HY-155966
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-19 (Compound 32) is a selective and orally active CDK2 inhibitor (Ki: 0.18 nM). CDK2-IN-19 shows anticancer activity in mice bearing OVCAR3 tumors .
|
-
- HY-P991135
-
|
|
CCR
|
Cancer
|
|
Enzelkitug is a humanized immunoglobulin G1-κ monoclonal antibody targeting the human C-C motif chemokine receptor 8 (CCR8). Enzelkitug is promising for research of various solid tumors and hematological malignancies .
|
-
- HY-N11096
-
|
|
Flavivirus
Dengue Virus
|
Infection
Cancer
|
|
Sinococuline is a potent anti-dengue agent that is effective against all four serotypes of dengue virus (DENV). Sinococuline is also an effective tumor cell growth inhibitor .
|
-
- HY-P9969
-
|
EMD 72000
|
EGFR
|
Cancer
|
|
Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth .
|
-
- HY-156566
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
|
-
- HY-147827
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
|
-
- HY-147828
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-11 (Compound 5d) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 32.7 and 623.5 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
|
-
- HY-N10520
-
-
- HY-W075353
-
-
- HY-132292
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .
|
-
- HY-155681
-
|
|
PD-1/PD-L1
Monoamine Oxidase
|
Cancer
|
|
SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%) .
|
-
- HY-122341
-
|
FR 900840
|
Antibiotic
|
Cancer
|
|
Thrazarine (FR 900840) is an oncology antibiotic that can be produced by Streptomyces coerulescens MH802-fF5. Thrazarine directly inhibits DNA synthesis and tumor cell growth. Thrazarine can specifically induce lysis of tumor cells co-cultured with non-activated macrophages. Thrazarine is used in cancer research .
|
-
- HY-157412
-
|
|
CRM1
|
Cancer
|
|
CRM1-IN-3 (B28) is a noncovalent CRM1 inhibitor. CRM1-IN-3 can be used for the research of protein localization and tumor .
|
-
- HY-18052
-
|
|
MDM-2/p53
|
Cancer
|
|
AM-8553 is a MDM2/p53 inhibitor (KD: 0.4 nM for MDM2). AM-8553 has anti-tumor activity
|
-
- HY-162128
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Antitumor agent-130 (Compound 7b) is a p300 histone acetyltransferases (HAT) inhibitor with an IC50 of 1.51 μM. Antitumor agent-130 combinates with doxorubicin (HY-15142A) can significantly inhibit tumor growth and invasion in vitro and in vivo .
|
-
- HY-13459
-
|
|
Smo
|
Cancer
|
|
PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
|
-
- HY-13459A
-
|
|
Smo
|
Cancer
|
|
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
|
-
- HY-D2285
-
|
|
Fluorescent Dye
|
Cancer
|
|
MOR-CES2 is a near-infrared fluorescent probe (Ex= 630 nm, Em=735 nm) capable of identifying cancer cells and tissues, as well as exhibiting a sensitive response to inflammation. MOR-CES2 holds potential as an efficient imaging tool in assisting surgical resection of CES2-related tumors .
|
-
- HY-103665A
-
|
|
STING
|
Cancer
|
|
STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer .
|
-
- HY-W024644
-
|
|
Phosphatase
|
Cancer
|
Hydroxyethylthio Vitamin K3 is a Cdc25 phosphatase inhibitor, with IC50 values of 4.56 μM and 23.63 μM for Cdc25A and Cdc25B, respectively. Hydroxyethylthio Vitamin K3 can be used in tumor research .
|
-
- HY-132223
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
LH1306 is a C2-symmetric inhibitor of PD-1/PD-L1 protein-protein interaction (PPI), with an IC50 value of 25 nM. LH1306 can be used in anti-tumor research .
|
-
- HY-N10961
-
|
|
Others
|
Cancer
|
|
Daphnodorin B is a flavonoid. Daphnodorin B can be isolated from the roots of Daphne genkwa. Daphnodorin B can be used for the research of tumor .
|
-
- HY-137435
-
|
SM08502
|
CDK
|
Cancer
|
|
Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research .
|
-
- HY-19171
-
|
|
Drug Derivative
|
Cancer
|
|
Aranose is a nitrosourea derivative with antineoplastic activity. Aranose can be used for leukemia, plasmacytoma, and solid tumor research .
|
-
- HY-136824
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Napyradiomycin A1 is one enantioselective compound of napyradiomycins. napyradiomycins are an intriguing family of halogenated natural products with activity against several tumor cell lines as well as some bacterial strains .
|
-
- HY-P99643A
-
|
|
Dan family
|
Cancer
|
|
Ginisortamab (Mouse IgG1) is the anti-Gremlin-1 monoclonal antibody with mouse IgG1. Ginisortamab (Mouse IgG1) can be used in research of gastrointestinal (GI) tumors .
|
-
- HY-126906
-
|
|
Antibiotic
P-glycoprotein
|
Cancer
|
|
Milbemycin A4 inhibits P-glycoprotein activity, and reverses multidrug resistance of tumor cells. Milbemycins are a family of macrolide antibiotics with insecticidal and acaricidal activity sup>[2].
|
-
- HY-142118A
-
|
AP 12009 sodium
|
TGF-beta/Smad
|
Cancer
|
|
Trabedersen sodium is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen sodium can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
|
-
- HY-N11709
-
|
|
Others
|
Cancer
|
|
Theasaponin E1 is a tea saponin isolated from tea seeds. Theasaponin E1 exhibits potential antitumor activity against human tumor cell lines K562 and HL60. Theasaponin E1 also has quinone reductase (QR)-inducing activity and can act as an anti-tumor agent for cancer prevention .
|
-
- HY-141523
-
|
RMC-4630; SHP2-IN-7
|
SHP2
Phosphatase
|
Cancer
|
|
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
|
-
- HY-12768B
-
|
BLZ945 dihydrochloride
|
c-Fms
|
Neurological Disease
Cancer
|
|
Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
|
-
- HY-P3440
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PD-1/PD-L1
|
Cancer
|
|
WL12 is a specifically targeting programmed death ligand 1 (PD-L1) binding peptide. WL12 can be radiolabeled by different radionuclides, generating radiotracers, which can assess the tumor PD-L1 expression .
|
-
- HY-113889
-
|
|
Progesterone Receptor
|
Cancer
|
|
ZK112993 is a potent progesterone receptor (PR) antagonist. ZK112993 significantly inhibits the growth of T61 human tumors in nude mice .
|
-
- HY-136110
-
|
D-Galactosone
|
DNA/RNA Synthesis
|
Cancer
|
|
2-Keto-D-galactose (D-Galactosone) inhibits DNA synthesis, and inhibits proliferation of in vitro grown Ehrlich ascites tumor cells .
|
-
- HY-P3842
-
|
|
PKC
|
Cancer
|
|
Protein Kinase C (661-671) is a fragment peptide of β1 subspecies of protein kinase C (PKC). PKC plays a role in cellular growth control and tumor promotion .
|
-
- HY-154797
-
|
|
Topoisomerase
|
Cancer
|
|
N,N-Dimethyldoxorubicin is a Doxorubicin (HY-15142A) analogue. N,N-Dimethyldoxorubicin shows cytotoxicity against a panel of tumor cell lines (IC50s < 0.3 μM) .
|
-
- HY-135849A
-
|
|
Reactive Oxygen Species
|
Others
Cancer
|
|
Catalase, Bovine Liver is an enzyme widely found in various organisms, including animals, plants and microorganisms. Catalase, Bovine Liver mainly exists in the peroxisome of cells and is an important antioxidant enzyme. Catalase, Bovine Liver plays an important role in removing ROS and maintaining the balance of redox state. Catalase, Bovine Liver is closely related to the occurrence and development of tumors. Catalase, Bovine Liver has the potential to be used in tumor prevention research .
|
-
- HY-13674
-
|
NSC 153858
|
Microtubule/Tubulin
|
Cancer
|
|
Maytansine is a highly potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at subnanomolar concentrations .
|
-
- HY-107008
-
|
|
Drug Derivative
|
Cancer
|
|
SW 71425 inhibits cell growth against breast, colon, non-small cell lung, and ovarian tumors. .
|
-
- HY-142118
-
|
AP 12009
|
TGF-beta/Smad
|
Cancer
|
|
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
|
-
- HY-160421
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206 + and CX3CR1 + immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells .
|
-
- HY-139361
-
|
PIN1-3
|
PIN1
|
Cancer
|
|
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
|
-
- HY-111209
-
|
S14161
|
PI3K
|
Cancer
|
|
Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. Pichromene can effectively inhibit tumor growth in leukemia mouse models and can be used in cancer research .
|
-
- HY-P99271
-
|
Anti-Human F3 Recombinant Antibody
|
ADC Antibody
|
Cancer
|
|
Tisotumab (Anti-Human F3 Recombinant Antibody) is a human IgG1 monoclonal antibody and ADC antibody. Tisotumab targets tissue factor (TF). Tisotumab can be used for the research of solid tumors .
|
-
- HY-146780
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model .
|
-
- HY-D1450
-
|
S01448
|
Fluorescent Dye
|
Cancer
|
|
IR-1048 is a nitroreductase (NTR)-responsive near-infrared fluorescence (NIR)/photoacoustic (PA) imaging probe and photothermal agent. IR-1048 is coupled with a nitroimidazole group to form IR-1048-MZ. IR-1048-MZ is catalytically reduced by NTR in a hypoxic environment, restoring strong near-infrared absorption and fluorescence emission (NIR II window), while activating the photothermal effect. IR-1048 relies on NTR-mediated electron transfer to relieve intramolecular fluorescence quenching, achieving specific imaging and photothermal ablation of tumor hypoxic areas. IR-1048 is mainly used for high-contrast NIR II/photoacoustic imaging and photothermal therapy research and tumor diagnosis of the tumor hypoxic microenvironment .
|
-
- HY-153268
-
|
BDTX-1535; EGFR-IN-76
|
EGFR
|
Cancer
|
|
BDTX-1535 (EGFR-IN-76) is an orally available, blood-brain permeable, selective EGFR inhibitor with anti-tumor activity. BDTX-1535 is indicated in a variety of models including non-small cell lung cancer, glioblastoma patient-derived tumors, and intracranial tumors .
|
-
- HY-N0462R
-
|
|
Toll-like Receptor (TLR)
Reverse Transcriptase
Bacterial
Apoptosis
Autophagy
|
Infection
Inflammation/Immunology
Cancer
|
|
Corilagin (Standard) is the analytical standard of Corilagin. This product is intended for research and analytical applications. Corilagin, a gallotannin, has anti-tumor, anti-inflammatory and hepatoprotective activities. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin also inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows anti-tumor activity on hepatocellular carcinoma and ovarian cancer model. Corilagin shows low toxicity to normal cells and tissues .
|
-
- HY-10084
-
|
|
Kinesin
|
Cancer
|
|
CK0106023 is a potent and specific allosteric inhibitor of KSP with a Ki value of 12 nM, showing antitumor activity. CK0106023 causes mitotic arrest and growth inhibition in several tumor cell lines. CK0106023 exhibits antitumor activity in tumor-bearing mice .
|
-
- HY-E70302
-
|
ST8SIA6
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
ST8 alpha-2,8-Sialyltransferase 6 (ST8SIA6) is a sialyltransferase that generates α2,8-linked disialic acids, which bind to mouse Siglec-E and human Siglec-7 and -9, and accelerates tumor growth by suppressing anti-tumor immune responses .
|
-
- HY-101931
-
|
|
VEGFR
|
Cancer
|
|
hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression .
|
-
- HY-149898
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Antitumor agent-109 (compound 6) is an inhibitor of hyaluronic acid (HY-B0633A) targeting to CD44, as well as an anti-tumor agent. Hyaluronic acid interacts with differentiation cluster 44 (CD44) and is involved in tumor growth and invasion. Antitumor agent-109 inhibits MDA-MB-231 cells with EC50 value of 0.59 μM .
|
-
- HY-P991139
-
|
|
CTLA-4
|
Cancer
|
|
Futermestotug is a humanized immunoglobulin G1-κ monoclonal antibody targeting human cytotoxic T-lymphocyte associated protein 4 (CTLA4). Futermestotug is promising for research of various malignant tumors .
|
-
- HY-148756
-
NG-497
1 Publications Verification
|
ATGL
|
Cancer
|
|
NG-497 is a selective human adipose triglyceride lipase (ATGL) inhibitor that targets the enzymatically active patatin-like domain of human ATGL. NG-497 has potential value for tumor research .
|
-
- HY-78884
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
Anticancer agent 9, a glycine derivative, is an anticancer agent. Anticancer agent 9 can inhibit tumor cells viability of myelogenous leukemia and human prostate cancer .
|
-
- HY-128587
-
|
SY-1365
|
CDK
|
Cancer
|
|
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
|
-
- HY-143734
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11) .
|
-
- HY-W102669
-
|
|
Drug Intermediate
|
Cancer
|
|
Spiro[4.5]decane-7,9-dione (Compound 2e) is a cyclic 1,3-diketone. Spiro[4.5]decane-7,9-dione can be used in the study of glioma tumors .
|
-
![Spiro[4.5]decane-7,9-dione](//file.medchemexpress.com/product_pic/hy-w102669.gif)
- HY-169626
-
|
|
VEGFR
|
Cardiovascular Disease
Cancer
|
|
VEGFR-IN-6 (Compound 3) is a vascular endothelial growth factor receptor (VEGFR) inhibitor. VEGFR-IN-6 can inhibit angiogenesis. VEGFR-IN-6 is promising for research of tumor diseases that rely on angiogenesis .
|
-
- HY-168260
-
|
|
Apoptosis
Ferroptosis
MMP
|
Cancer
|
|
CQ-Mito is a Coumarin-Quinazolinone (CQ)-based derivative that targets mitochondria and exhibits profound phototherapeutic performances with an Phototoxic Index (PI) value of 167. CQ-Mito causes cell death by both apoptosis and ferroptosis. CQ-Mito mediates mitochondrial dysfunction, including mitochondrial morphology changed and the loss of MMP. CQ-Mito can efficiently inhibit the tumor growth in organoid tumor models .
|
-
- HY-148385
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Ganglioside GM2 is a human tumor antigen (OFA-I-1). Ganglioside GM2 is the major lysosomal storage compound of Tay-Sachs disease .
|
-
- HY-P990042
-
|
ONC-392; BNT 316
|
CTLA-4
|
Cancer
|
|
Gotistobart (ONC-392) is a humanized anti-CTLA-4 antibody that confers immunotherapeutic effect by selective depletion of regulatory T cells (Treg) in the tumor microenvironment .
|
-
- HY-153521
-
|
|
BCL6
|
Cancer
|
|
CCT374705 is an orally active BCL6 inhibitor with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
|
-
- HY-161412
-
|
|
HDAC
|
Cancer
|
|
STR-V-53 is an HDAC inhibitor (IC50 in nM).STR-V-53 increases histone acetylation in tumor cells by inhibiting the activity of these enzymes, which in turn regulates gene expression.STR-V-53 inhibits tumor growth, and induces apoptosis .
|
-
- HY-P3627
-
|
|
Drug Derivative
|
Cancer
|
|
Nagrestipen, a human macrophage inflammatory protein-1 alpha (MIP-1α) variant, also known as ECI 301. Nagrestipen has antitumor activity and can be used in therapeutic trials to study cancer, tumors, metastases, radiation oncology, and tumor metastasis .
|
-
- HY-129040A
-
|
MIBG sulfate
|
Adrenergic Receptor
|
Cancer
|
|
Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation) .
|
-
- HY-145938
-
|
|
FAP
|
Cancer
|
|
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
|
-
- HY-139245
-
|
|
ADC Linker
|
Cancer
|
|
MC-Ala-Ala-Asn-PAB is a linker extracted from patent CN104147612A, page 14. MC-Ala-Ala-Asn-PAB can be used to synthesis the tumor microenvironment specific activated micromolecular targeted conjugate .
|
-
- HY-157318
-
|
|
SHP2
|
Cancer
|
|
PB17-026-01 is a potent SHP2 allosteric inhibitor and shows the highest inhibitory activity with an IC50 value of 38.9?nM. PB17-026-01 can be used for the research of tumor .
|
-
- HY-P10893
-
|
|
Drug Derivative
|
Cancer
|
|
BCY8234 is a mono-methylauristatin E (MMAE)-free analogue of BT8009. BT8009 is a nectin-4 targeting bicycle toxin conjugate for the treatment of solid tumors. BCY8234 attenuates the response to BT8009 .
|
-
- HY-153699
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty .
|
-
- HY-149891
-
|
|
HSP
|
Cancer
|
|
HSP90-IN-23 (Comp 12-1) is an inhibitor of heat shock protein 90(HSP90) with an IC50 of 9 nM. HSP90-IN-23 induces apoptosis of tumor cells and arrests the tumor cell cycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research .
|
-
- HY-163548
-
|
|
Sialyltransferase
|
Cancer
|
|
SPP-002 is a sulfate analogue that acts as a potential Sialyltransferase (ST) inhibitor. SPP-002 selectively inhibits n-glycosialylation with inhibition at least an order of magnitude greater than that of unmodified parental cholic acid (LCA). SPP-002 reduces tumor cell migration and invasion by inhibiting the integrin /FAK/Paxillin signaling pathway. SPP-002 can be used in the study of tumor metastasis .
|
-
- HY-156681
-
|
STX-478
|
PI3K
|
Cancer
|
|
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .
|
-
- HY-P10920
-
|
|
Drug Derivative
|
Cancer
|
|
DOTAMTATE is a somatostatin analogue. DOTAMTATE marked 212Pb is promising for research of somatostatin receptor positive neuroendocrine tumors .
|
-
- HY-14934
-
|
STA 5312
|
Microtubule/Tubulin
|
Cancer
|
|
Rosabulin (STA 5312) is a potent and orally active microtubule inhibitor that inhibits microtubule assembly. Rosabulin has broad-spectrum anti-tumor activity .
|
-
- HY-13917
-
|
VS-4718; SR-2516
|
FAK
Apoptosis
|
Cancer
|
|
PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis .
|
-
- HY-13917A
-
|
VS-4718 hydrochloride; SR-2516 hydrochloride
|
FAK
Apoptosis
|
Cancer
|
|
PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis .
|
-
- HY-116828
-
|
|
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
ARI-3531 (compound 22) is a selective prolyl oligopeptidase (PREP) inhibitor (Ki=0.73 nM). ARI-3531 can be used to study tumor invasion and metastasis .
|
-
- HY-169129
-
|
ILX-295501
|
Drug Derivative
|
Cancer
|
|
LY-295501 is a sulfonylurea compound that has demonstrated in-vivo antitumor activity against a broad spectrum of solid tumors. LY-295501 can be utilized in cancer research .
|
-
- HY-155052
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-2 (compound 5i) is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils .
|
-
- HY-145034
-
-
- HY-151255
-
|
|
CDK
|
Cancer
|
|
CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies .
|
-
- HY-123886
-
|
|
Antibiotic
|
Cancer
|
|
Aranciamycin (Compound 1) is an anthracycline antibiotic with collagenase inhibitory activity (IC503.7*10-7M). Aranciamycin can be used to inhibit DNA synthesis in tumor cells .
|
-
- HY-118343
-
|
|
Sirtuin
|
Cancer
|
|
AC-93253 is a selective, potent SIRT2 inhibitor. AC93253 can inhibit SIRT2 with an IC50 value of 6 μM. AC93253 can be used for the research of tumors .
|
-
- HY-120264
-
|
|
Zinc Finger Protein
|
Cancer
|
|
YPC-22026 is a zinc-finger protein 143 (ZNF143) inhibitor with an IC50 value of 9.0 μM. YPC-22026 is a potent tumor regression inducer. YPC-22026 exhibits anti‐tumor activities .
|
-
- HY-162858
-
|
|
Caspase
|
Cancer
|
BRD-810 is a highly selective MCL1 inhibitor. BRD-810 can bind to the BH3 groove of MCL1 and block the sequestration of pro-apoptotic proteins, quickly inducing caspase activation in MCL1-dependent cell lines. BRD-810 shows anti-tumor activity in models of blood cancers and solid tumors .
|
-
- HY-153552A
-
|
|
FAP
|
Cancer
|
|
NH2-UAMC1110 TFA is a UAMC1110 derivative that can be used in the synthesis of FAPI-QS. UAMC1110 is a fibroblast activation protein (FAP) inhibitor. FAPI-QS is a chelating agent that can be used to synthesize high tumor selectivity and high dose radiotracers for the diagnosis and treatment of tumors .
|
-
- HY-P10501
-
|
|
Antifolate
|
Cancer
|
|
FRα-targeting peptide C7 is a selective peptide ligand for folate receptor α (FRα) that has specific binding to FRα expressing cells and in vivo tumor targeting ability. FRα-targeting peptide C7 can be used in the research of tumor diagnosis and treatment .
|
-
- HY-P99667
-
|
OMP-54F28; FZD8-Fc
|
Wnt
|
Cancer
|
|
Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
|
-
- HY-135818
-
|
|
Others
|
Cancer
|
|
XM462 is a dihydroceramide desaturase inhibitor. XM462 produced a mixed-type inhibition (Ki=2 μM) in vitro. XM462 has dihydroceramide desaturase inhibition both in vitro and in cultured cells with IC50 values of 8.2 and 0.78 μM, respectively. XM462 can be used for the research of tumor .
|
-
- HY-155052A
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-2 (compound 5i) TFA is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 TFA inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils .
|
-
- HY-137457
-
|
IDX-1197
|
PARP
|
Cancer
|
|
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research .
|
-
- HY-162247
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2-IN-26 (compound A3) is an MDM2 inhibitor that can activate the tumor suppressor function of p53 by blocking the interaction between MDM2 and p53 (MDM2 is the main negative regulator of p53). MDM2-IN-26 can be used for cancer research .
|
-
- HY-136279
-
|
|
Apoptosis
|
Cancer
|
|
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo .
|
-
- HY-N6955
-
|
|
Others
|
Cancer
|
|
Eupalinilide B is a guaiane type sesquiterpene lactone that can be found in Eupatorium lindleyanum. Eupalinilide B shows potent cytotoxicity against P-388 and A-549 tumor cell lines .
|
-
- HY-161234
-
|
|
Ras
|
Cancer
|
|
KRAS ligand 3 (compound 1) is BTX-6654 target-binding ligand that can bind KRAS inhibitor and diaplay synergistic tumor growth inhibiton .
|
-
- HY-P99619
-
|
SCT-I10A
|
PD-1/PD-L1
|
Cancer
|
|
Finotonlimab (SCT-I10A) is a recombinant humanised IgG PD-1 antibody. Finotonlimab has the potential for solid tumors or lymphomas research .
|
-
- HY-164360
-
|
|
Integrin
|
Inflammation/Immunology
Cancer
|
αVβ8-IN-1 is a αVβ8 integrin inhibitor. αVβ8-IN-1 has been shown to inhibit the growth of tumors such as EMT6, CT26, KPC, and TKCC-10. αVβ8-IN-1 can be used in research related to idiopathic pulmonary fibrosis (IPF), non-specific interstitial pneumonia (NSIP), and tumors .
|
-
- HY-147593
-
|
|
CD73
|
Cancer
|
|
CD73-IN-12 is a potent inhibitor of CD73. CD73 is closely associated with tumor growth, angiogenesis and metastasis. CD73-IN-12 be used for preparing a medicament for tumor-related diseases (extracted from patent CN114437038A, compound 9) . CD73-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-Y1365
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
Cancer
|
|
Gelatins is a non-toxic, non carcinogenic, biodegradable, and non irritating natural polymer derived from partial hydrolysis of collagen. Due to its strong liquid absorption and swelling ability, Gelatins has excellent hemostatic properties and can be used as a matrix material for the reduction, growth, and stability of metal nanoparticles. Gelatins can also be used for tumor cell culture and tumor therapy [1][2][3].
|
-
- HY-P10501A
-
|
|
Antifolate
|
Cancer
|
|
FRα-targeting peptide C7 (TFA) is a selective peptide ligand for folate receptor α (FRα) that has specific binding to FRα expressing cells and in vivo tumor targeting ability. FRα-targeting peptide C7 (TFA) can be used in the research of tumor diagnosis and treatment .
|
-
- HY-160449
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 10 (Example C-2) is a compound that targets the y220c mutant of p53. p53 Activator 10 activation is involved in the downstream effects of tumor suppression .
|
-
- HY-136201
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Sodium Glucoheptonate is used as a kit for radio-labeling with Tc-99m. Tc-99m glucoheptonate is kidney- and brain-imaging agent, and can be used in brain-tumor detection .
|
-
- HY-B0109
-
|
L671152; MK507
|
Carbonic Anhydrase
|
Cancer
|
Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
|
-
- HY-B0109A
-
|
L671152 hydrochloride; MK507 hydrochloride
|
Carbonic Anhydrase
|
Cardiovascular Disease
Others
|
Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
|
-
- HY-120515
-
|
|
PKC
|
Cancer
|
|
7-Oxostaurosporine is a potent protein kinase C (PKC) inhibitor that effectively inhibits tumor growth by inducing apoptosis and inhibiting the nuclear factor (NF)-κB/p-p65 pathway .
|
-
- HY-153272
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Antitumor agent-93 (compound 7D) is an anticancer agent that can effectively inhibit the growth of several tumor cell lines, such as MDA-MB-231 and HCT-116 cell lines .
|
-
- HY-19981B
-
|
ARQ-087 dihydrochloride
|
EGFR
|
Cancer
|
|
Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models .
|
-
- HY-136959
-
|
|
HDAC
|
Cancer
|
|
M133 is a HDAC1 and HDAC2 selective inhibitor which shows potent antiproliferative activity against diverse human tumor cell lines with IC50s of 0.75-1.94 μM. M133 can be used for cancer research .
|
-
- HY-160289
-
|
|
Proteasome
|
Cancer
|
|
ARI-3144 is an excellent substrate for fibroblast activation protein (FAP). ARI-3144 is a FAP-activated proteasome inhibitor that can be used for the research of solid tumors .
|
-
- HY-P990027
-
|
|
ADC Antibody
|
Cancer
|
|
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
|
-
- HY-P5126
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
|
DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis . DOTA-LM3 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-163001
-
|
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-164484
-
|
|
Raf
|
Cancer
|
|
IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities .
|
-
- HY-103711
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts .
|
-
- HY-P991178
-
|
|
TNF Receptor
|
Cancer
|
|
BMS-986156 is a fully humanized IgG1 agonist monoclonal antibody agonist corticosteroid-induced tumor necrosis factor receptor-related protein (GITR). BMS-986156 binds to GITR and promotes activation of T effector cells and inactivates T regulatory cells. BMS-986156 is indicated for use in advanced solid tumor studies .
|
-
- HY-147784
-
|
|
Btk
|
Cancer
|
|
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
|
-
- HY-162859
-
|
|
DNA/RNA Synthesis
|
Cancer
|
AB25583 is a Polθ helicase (Polθ-hel) small molecule inhibitor, with an IC50 value of 6 nM. AB25583 selectively kills BRCA1/2 deficient cells and works in synergy with Olaparib (HY-10162) in cancer cells carrying pathogenic BRCA1/2 mutations. AB25583 can be used for tumor research .
|
-
- HY-P10770
-
|
|
Peptide-Drug Conjugates (PDCs)
E-Selectin
|
Cardiovascular Disease
Cancer
|
|
P-ESBP-DOX is a HPMA copolymer-drug conjugate, which is consistituted of the E-selectin binding peptide and the Doxorubicin (HY-15142). P-ESBP-DOX exhibits cytotoxicity against TNFα-activated human vascular endothelial cells IVECs with an IC50 of 0.28 μM. P-ESBP-DOX can be used in research about tumor vasculature .
|
-
- HY-10824B
-
|
PT523 ammonium
|
Dihydrofolate reductase (DHFR)
Antifolate
|
Cancer
|
|
Talotrexin ammonium is a nonpolyglutamatable antifolate. Talotrexin ammonium improves antitumor activity in a broad spectrum of cancer models by targeting DHFR to inhibit tumor growth .
|
-
- HY-D1719
-
|
|
Fluorescent Dye
|
Others
|
|
Cypate, a cyanine dye, is a near infrared (NIR) fluorescent probe for in vivo tumor imaging .
|
-
- HY-153773
-
Z4P
3 Publications Verification
|
IRE1
|
Cancer
|
|
Z4P is a BBB-penatrable IRE1 inhibitor with an IC50 of 1.13 μM. Z4P in combination with Temozolomide (HY-17364) inhibits the growth and recurrence of glioblastoma and has anti-tumor activity .
|
-
- HY-147592
-
|
|
CD73
|
Inflammation/Immunology
Cancer
|
|
CD73-IN-11 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-11 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 24) .
|
-
- HY-147591
-
|
|
CD73
|
Inflammation/Immunology
Cancer
|
|
CD73-IN-10 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-10 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 4) .
|
-
- HY-168011
-
|
|
Ferroptosis
Glutathione Peroxidase
Reactive Oxygen Species
|
Cancer
|
|
GPX4-IN-14 (compound 2c) is an inhibitor of GPX4, with free radical scavenging activity (maximum scavenging rate is 72.52%) and anti-tumor proliferation activity in vitro. GPX4-IN-14 inhibits GPX4 protein, increases lipid peroxide levels and intracellular Reactive Oxygen Species (ROS) levels, thereby inducing ferroptosis and exerting anti-tumor proliferation effects .
|
-
- HY-147589
-
|
|
CD73
|
Cancer
|
|
CD73-IN-8 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-8 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022052886A1, compound 57) .
|
-
- HY-147590
-
|
|
CD73
|
Inflammation/Immunology
|
|
CD73-IN-9 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-9 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 2) .
|
-
- HY-147588
-
|
|
CD73
|
Cancer
|
|
CD73-IN-7 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-7 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022052886A1, compound 13) .
|
-
- HY-122590
-
|
|
Gli
|
Cancer
|
|
Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells .
|
-
- HY-126598
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Chaetoglobosin F is a cytochalasan-based alkaloid from Chaetomium globosum. Chaetoglobosin F exhibits cytotoxicity against human nasopharyngeal epidermoid tumor cell KB, with IC50 of 52.0 µM .
|
-
- HY-D1905
-
|
|
Fluorescent Dye
|
Cancer
|
|
ICG acid is a fluorescent dye used in medical diagnostics. ICG acid has absorption peaking at 800 nm and can absorb the near IR laser energy and release heat in the dyed tissue. ICG acid has been used in fluorescence-guided surgery to identify critical structures, including intra-abdominal tumors .
|
-
- HY-126906R
-
|
|
Antibiotic
P-glycoprotein
|
Cancer
|
|
Milbemycin A4 (Standard) is the analytical standard of Milbemycin A4. This product is intended for research and analytical applications. Milbemycin A4 inhibits P-glycoprotein activity, and reverses multidrug resistance of tumor cells. Milbemycins are a family of macrolide antibiotics with insecticidal and acaricidal activity sup> .
|
-
- HY-P991154
-
|
|
VEGFR
PD-1/PD-L1
|
Cancer
|
|
Pumitamig is a humanized bispecific immunoglobulin (H-γ1-VH_L-κ) dimer antibody targeting human vascular endothelial growth factor A (VEGFA) and human programmed death ligand 1 (PD-L1). Pumitamig is promising for research of various solid tumors .
|
-
- HY-129040AR
-
|
|
Adrenergic Receptor
|
Cancer
|
|
Iobenguane (sulfate) (Standard) is the analytical standard of Iobenguane (sulfate). This product is intended for research and analytical applications. Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation) .
|
-
- HY-N7507
-
|
|
Others
|
Cancer
|
|
Sempervirine is an indole alkaloid isolated from Gelsemium sempervirens with anti-tumor activities. Sempervirine is against sempervirine-sensitive tumor cells with EC50 values of 2.7 μM, 1.77 μM, and 1.96 μM for Raji, MDA-MB-231 and HeLa cells, respectively .
|
-
- HY-149517
-
|
|
EGFR
|
Cancer
|
|
E07 aptamer is an aptamer that targets human epidermal growth factor receptor (hEGFR). E07 aptamer can compete with EGF for binding, binds to a novel epitope on EGFR. E07 aptamer binds to cells expressing EGFR, blocks receptor autophosphorylation, and prevents proliferation of tumor cells in three-dimensional matrices. E07 aptamer can be used for tomor disease research .
|
-
- HY-148305
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-28 (compound 3) is an immune checkpoint inhibitor of PD-1/PD-L1 signaling pathway (IC50=0.744 µM). PD-1/PD-L1-IN-28 shows good research potential in tumor immunity .
|
-
- HY-119529
-
|
3,8-Quinolinediol
|
Tyrosinase
Bacterial
|
Cancer
|
|
Jineol is a cytotoxic alkaloid from the centipede Scolopendra subspinipes. Jineol exhibits modest cytotoxic activity in vitro against the growth of human tumor cell lines .
|
-
- HY-170806
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model .
|
-
- HY-117836
-
|
|
FAK
|
Cancer
|
|
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
|
-
- HY-101566A
-
|
BAY 1895344 hydrochloride
|
ATM/ATR
|
Cancer
|
|
Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity . Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas .
|
-
- HY-P5126A
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
|
DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis . DOTA-LM3 (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-170779
-
|
|
FAP
|
Cancer
|
|
DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([ 68Ga]Ga/DOTA-NI-FAPI-04 and [ 177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact .
|
-
- HY-164529
-
|
|
Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
|
-
- HY-163028
-
|
|
Tim3
|
Cancer
|
|
ML-T7 is a potent Tim-3 inhibitor. ML-T7 blocks Tim-3 interactions with PtdSer and CEACAM1.
ML-T7 not only enhances the antitumor activity of adoptive transfer therapy with cytotoxic T lymphocytes (CTLs) and CAR T cells but also increases the effector function of T cell. ML-T7 promotes NK cells’ killing activity against tumor cells and DC antigen-presenting capacity. ML-T7 directly exerts antitumor efficacy in preclinical tumor models either alone or in combination with Nivolumab (HY-P9903A). ML-T7 can be used for tumor immunotherapy research .
|
-
- HY-N0797
-
-
- HY-N3215
-
|
|
Others
|
Others
|
|
Nagilactone C is a diterpene dilactone compound isolated from Podocarpus neriifolius. Nagilactone C has potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines .
|
-
- HY-W008449
-
|
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
1-Methylxanthine, a caffeine derivative, is an essential human urinary metabolite of caffeine and theophylline (1,3-dimethylxanthine, TP) . 1-Methylxanthine enhances the radiosensitivity of tumor cells .
|
-
- HY-153432
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
TRV-7019 is a BBB-penetrable radioligand for brain imaging that target butyrylcholinesterase. TRV-7019 can be used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity .
|
-
- HY-P99217
-
|
AMG 102
|
c-Met/HGFR
|
Cancer
|
|
Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
|
-
- HY-117249
-
|
AK-2123
|
Apoptosis
Caspase
|
Cancer
|
|
Sanazole (AK-2123) is a hypoxic cell radiosensitizer. Sanazole enhances radiation-induced DNA strand breaks. In mouse fibroblast tumors, Sanazole increases nuclear condensation and fragmentation, as well as elevates caspase-3 activity, thereby enhancing radiation-induced apoptosis. These characteristics make Sanazole a promising candidate for research in tumor therapy .
|
-
- HY-148839
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research .
|
-
- HY-137206
-
|
|
Molecular Glues
Ligands for E3 Ligase
|
Cancer
|
|
ALV2 is a potent and selective Helios molecular glue degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment .
|
-
- HY-161373
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
|
-
- HY-101566
-
|
BAY 1895344
|
ATM/ATR
|
Cancer
|
|
Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity . Elimusertib can be used for the research of solid tumors and lymphomas .
|
-
- HY-B0919
-
|
CI-337; O-Diazoacetyl-L-serine; P-165
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Azazerine (CI-337) is a competitive inhibitor of glutamine amidotransferase. Azaserine is an antibiotic, it shows antibacterial activities. Azazerine shows anti-tumor activities and it may also act as a tumor inducer. Azazerine can be used for the research of cancer and infection .
|
-
- HY-145414
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
DYSP-C34 is a potent, biocompatible, and ultrasound (US)-triggered multifunctional molecular machine. DYSP-C34 has multiple favorable properties, such as improved lipophilic/hydrophilic balance, intensified US-induced ROS production capacity, and better cellular permeability, resulting in the excellent tumor target efficiency and notable sonodynamic therapy (SDT)-mediated tumor regression. DYSP-C34 exhibits mild immunogenicity by stimulating APCs directly .
|
-
- HY-149227
-
-
- HY-15866
-
|
|
Others
|
Cancer
|
|
FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research .
|
-
- HY-149482
-
LN5P45
1 Publications Verification
|
Cathepsin
|
Cancer
|
|
LN5P45 is an OTUB2 inhibitor (IC50: 2.3 μM). LN5P45 induces monoubiquitination of OTUB2 on lysine 31. LN5P45 can be used for research of tumor progression and metastasis .
|
-
- HY-131651
-
|
LTB4 ethanolamide
|
Endogenous Metabolite
Leukotriene Receptor
|
Cancer
|
|
Leukotriene B4 ethanolamide (LTB4 ethanolamide) is an antagonist and a partial agonist for Leukotriene B4 (LTB4) receptor 1 (BLTR1). Leukotriene B4 ethanolamide ameliorates the tumor progression, which is only asscociated with inflammation .
|
-
- HY-132979
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities .
|
-
- HY-162001
-
INX-315
1 Publications Verification
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-162865
-
|
|
FGFR
|
Cancer
|
FGFR2-IN-3 is an inhibitor of fibroblast growth factor receptor 2 (FGFR2). FGFR2-IN-3 has good binding properties, forming key interactions and inducing conformational changes in FGFR2. FGFR2-IN-3 can be used for research on tumors .
|
-
- HY-161661
-
|
|
Others
|
Cancer
|
|
Anticancer agent 223 (Compound V-d) is an anticancer agent that triggers cell death through caspase-dependent and caspase-independent mechanisms. Anticancer agent 223 inhibits tumor spheroid formation and resensitizes cisplatin (HY-17394)-resistant A2780 cells to cisplatin (HY-17394) treatment .
|
-
- HY-P991151
-
|
|
PD-1/PD-L1
TNF Receptor
|
Cancer
|
|
Opamtistomig is a humanized immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody targeting human programmed death ligand 1 (PD-L1), CD274 and tumor necrosis factor receptor superfamily member 9 (TNFRSF9). Opamtistomig is promising for research of various solid tumors and hematological malignancies .
|
-
- HY-116071
-
|
|
Autophagy
|
Cancer
|
|
Autophagy-IN-3 (Compound 6k) is an autophagy inhibitor. Autophagy-IN-3 promotes metabolic stress in the tumor microenvironment and enhances the effects of cytostatics in combined treatments .
|
-
- HY-114377
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
p-SCN-Bn-DOTA is a bifunctional chelating agent. p-SCN-Bn-DOTA can simultaneously chelate radionuclides and link monoclonal antibody for radioimmunoresearch of tumor .
|
-
- HY-128075
-
|
|
Herbicide
|
Cancer
|
|
Acifluorfen, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen causes strong photooxidative destruction of pigments and lipids in sensitive plant species .
|
-
- HY-141729
-
|
|
Fluorescent Dye
|
Cancer
|
|
Biotin-NH-PSMA-617 is a biotin-tagged PSMA-617. PSMA-617 is a small molecule targeting the prostate-specific membrane antigen (PSMA), which is directly expressed by the tumor cells .
|
-
- HY-146185
-
|
|
Molecular Glues
Bcl-2 Family
|
Cancer
|
|
CCT373566 is a potent and orally active molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo .
|
-
- HY-121452
-
|
|
nAChR
Calcium Channel
|
Cancer
|
|
Migrastatin is a typical Fascin1 inhibitor. Migrastatin is isolated from a cultured broth of Streptomyces sp. MK929-43F1. Migrastatin inhibits tumor cell migration .
|
-
- HY-114586
-
|
|
Angiotensin Receptor
|
Cancer
|
|
L-158809 is an angiotensin type 1 (AT1) receptor antagonist that prevents or ameliorates fractionated whole-brain irradiation-induced cognitive impairment. L-158809 is promising for research of brain tumor .
|
-
- HY-118985
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Acifluorfen sodium, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen sodium causes strong photooxidative destruction of pigments and lipids in sensitive plant species .
|
-
- HY-P991179
-
|
|
TNF Receptor
|
Cancer
|
|
MK-4166 is a humanized IgG1 agonist monoclonal antibody targeting GITR. MK-4166 enhances the proliferation of both naïve and tumor-infiltrating T lymphocytes .
|
-
- HY-16045
-
|
Hexyl 5-aminolevulinate hydrochloride; P-1206; 5-Aminolevulinic acid hexyl ester hydrochloride
|
Fluorescent Dye
|
Cancer
|
|
Hexaminolevulinate (Hexyl 5-aminolevulinate) hydrochloride, a porphyrin precursor, is a photosensitiser that can be used in photodynamic therapy (PDT) for certain tumor. Hexaminolevulinate hydrochloride can improve the visualisation of bladder tumours .
|
-
- HY-144443
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-16 (Compound M23) is a potent inhibitor of PD-1/PD-L1 with an IC50 value of 53.2 nM. PD-1/PD-L1-IN-16 has the potential for the research of tumor immunoresearch .
|
-
- HY-155747
-
|
|
Autophagy
Akt
mTOR
|
Cancer
|
|
FDW028 a potent and highly selective FUT8 inhibitor. FUT8 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. FDW028 can be used for metastatic colorectal cancer (mCRC) research .
|
-
- HY-103665
-
|
|
STING
|
Cancer
|
|
STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer .
|
-
- HY-P99100
-
|
CTL-002
|
PD-1/PD-L1
|
Cancer
|
|
Visugromab (CTL-002) is a GDF-15 neutralizing IgG4 mAb. Visugromab has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors .
|
-
- HY-144442
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-15 (Compound M17) is a potent inhibitor of PD-1/PD-L1 with an IC50 value of 60.1 nM. PD-1/PD-L1-IN-15 has the potential for the research of tumor immunoresearch .
|
-
- HY-139453
-
|
|
Drug Derivative
DNA Alkylator/Crosslinker
|
Cancer
|
|
LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
|
-
- HY-163658
-
|
|
PARP
|
Cancer
|
|
PARP-1-IN-23 (Compound I16 ) is an orally active and selective PARP-1 inhibitor with the IC50 of 12.38 nM. PARP-1-IN-23 inhibits tumor growth in vivo .
|
-
- HY-170393
-
|
|
JAK
STAT
|
Cancer
|
|
iBFAR2, a BFAR inhibitor, restores the CD8+ TRM cell subset against solid tumors. iBFAR2 promotes JAK2-STAT1 association and STAT1 phosphorylation .
|
-
- HY-P5910
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Azurin p28 peptide is a tumor-penetrated antitumor peptide. Azurin p28 peptide redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide induces apoptosis or cell cycle arrest. Azurin p28 peptide inhibits p53-positive tumor growths. Azurin p28 peptide shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
|
-
- HY-N1381
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Periplocin is a cardiotonic steroid isolated from root-bark Periploca sepium Bunge. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase .
|
-
- HY-169868
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
NOTA-FAPI-52 is a tracer with potent tumor uptake. NOTA-FAPI-52 can be radiolabeled to enable PET imaging or other bioimaging techniques. NOTA-FAPI-52 can be used to study diseases in which fibroblast activation protein (FAP) is overexpressed .
|
-
- HY-156680
-
|
|
Histone Methyltransferase
|
Cancer
|
|
TNG-462 is an orally active and selective PRMT5 inhibitor with anti-tumor activity against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation cancers .
|
-
- HY-135336A
-
-
- HY-149412
-
|
|
ERK
|
Cancer
|
|
MHJ-627 is a potent ERK5 (MAPK7) inhibitor (IC50: 0.91 μM). MHJ-627 promotes the mRNA expression of tumor suppressors and anti-metastatic genes, and promotes cancer cell death .
|
-
- HY-162599
-
|
|
TNF Receptor
|
Infection
Cancer
|
|
Spirohypertone B is a potent Tumor necrosis factor-α (TNF-α) inhibitor. Spirohypertone B protects L929 cells from death induced by co-incubation with TNF-α and Actinomycin D (HY-17559) .
|
-
- HY-B0754A
-
|
Hematoporphyrin IX dihydrochloride
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin dihydrochloride can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light .
|
-
- HY-N7486
-
|
|
Others
|
Cancer
|
|
Chamaejasmenin B can be extracted from Stellera chamaejasme L. Chamaejasmenin B suppresses cancer cells migration and invasion. Chamaejasmenin B inhibits tumor metastasis. Chamaejasmenin B can be used in the research of cancers, such as breast cancers .
|
-
- HY-B0754
-
|
Hematoporphyrin IX
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Hematoporphyrin (Hematoporphyrin IX), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light .
|
-
- HY-162567
-
|
|
HSP
|
Cancer
|
|
AP-4-139B is a heat shock protein 70 inhibitor (IC50=180 nM). HSP70 is a protein that is overexpressed in many types of cancer and is closely related to the survival and proliferation of tumor cells. AP-4-139B exhibits significant cytotoxicity to tumor cells, particularly in colorectal cancer cells. AP-4-139B can be used for cancer research .
|
-
- HY-16999
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
|
-
- HY-144184
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-6 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-6 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-6 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 18) .
|
-
- HY-144185
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-7 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-7 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-7 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 24) .
|
-
- HY-144181
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-5 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-5 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-5 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 1) .
|
-
- HY-125858
-
MI-1061
1 Publications Verification
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-P5128
-
|
Satoreotide tetraxetan
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
|
DOTA-JR11 is a somatostatin receptor 2 （SSTR2）antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research . DOTA-JR11 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-N2420
-
-
- HY-173268
-
|
|
TAM Receptor
|
Cardiovascular Disease
Cancer
|
|
UNC9426 (compound 12) is a potent, orally bioavailable and specific TYRO3 inhibitor with an IC50 of 2.1 nM. UNC9426 reduces platelet aggregation without increasing bleeding time. UNC9426 blocks TYRO3-dependent functions in tumor cells and macrophages .
|
-
- HY-149931
-
|
|
Fluorescent Dye
|
Cancer
|
|
BMV109 is a quenched probe that becomes fluorescent when cleaved and covalently bound by active cathepsin proteases. BMV109 can be exploited for tumor imaging .
|
-
- HY-P99785
-
|
HLX20
|
PD-1/PD-L1
|
Cancer
|
|
Opucolimab is an anti-PD-L1 recombinant human monoclonal antibody. Opucolimab can be used to synthesis antibody agent conjugates. Opucolimab can be used for the research of advanced solid tumors .
|
-
- HY-19095
-
|
|
Antifolate
|
Cancer
|
|
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo .
|
-
- HY-158062
-
|
|
PROTACs
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research . (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
|
-
- HY-P10563
-
|
BHV-1100
|
CD38
|
Cancer
|
|
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .
|
-
- HY-115908
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
|
-
- HY-P5910A
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Azurin p28 peptide TFA is a tumor-penetrated antitumor peptide. Azurin p28 peptide TFA redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide TFA induces apoptosis or cell cycle arrest. Azurin p28 peptide TFA inhibits p53-positive tumor growths. Azurin p28 peptide TFA shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
|
-
- HY-125858A
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-156109
-
|
|
PDHK
Mitochondrial Metabolism
|
Cancer
|
|
PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
|
-
- HY-N1839
-
|
|
Apoptosis
Glycosidase
|
Cancer
|
|
3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC) inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitory activity against α-glucosidase (IC50: 345 μM) .
|
-
- HY-P99007
-
|
BAY 1179470
|
FGFR
|
Cancer
|
|
Aprutumab (BAY 1179470) is a fully human FGFR2 monoclonal antibody, which binds to the FGFR2 isoforms FGFR2-IIIb and FGFR2-IIIc. Aprutumab has the potential for solid tumors research .
|
-
- HY-13554
-
|
|
Antibiotic
|
Infection
Cancer
|
|
Annamycin is an antibiotic, that has high affinity for lipid membranes and can bypass the multidrug resistance protein-1 (MDR-1 ) mechanism of cellular drug resistance. Annamycin exhibits antitumor efficacy in multilamellar vesicles against solid tumor .
|
-
- HY-143889
-
|
|
CDK
|
Cancer
|
|
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
|
-
- HY-139579
-
|
OTL 38
|
Fluorescent Dye
|
Cancer
|
|
Pafolacianine (OTL 38) is a fluorescent imaging agent made of near-infrared dye used in detecting tumor lesions during surgical procedures. Pafolacianine excites at 774 to 775 nm and emits at 794 to 796 nm .
|
-
- HY-N0247
-
|
|
Smo
|
Cancer
|
|
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri with anticancer activity. Saikosaponin B1 significantly inhibits tumor growth in Medulloblastoma (MB) model by inhibiting the Hedgehog pathway through targeting SMO .
|
-
- HY-161074
-
|
|
FAP
|
Cancer
|
|
PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors .
|
-
- HY-155602
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-18 (compound 8q) is a potent inhibitor of CDK2/E and CDK4/D1, with IC50s of 8 nM and 46 nM, respectively. CDK2-IN-18 inhibits the proliferation of tumor cells .
|
-
- HY-144029
-
|
|
RET
|
Cancer
|
|
RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research .
|
-
- HY-B0109AS
-
|
L671152-d3 hydrochloride; MK507-d3 hydrochloride
|
Carbonic Anhydrase
Isotope-Labeled Compounds
|
Others
|
Dorzolamide-d3 hydrochloride is deuterated labeled Dorzolamide hydrochloride (HY-B0109A). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
|
-
- HY-136201R
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Sodium Glucoheptonate (Standard) is the analytical standard of Sodium Glucoheptonate. This product is intended for research and analytical applications. Sodium Glucoheptonate is used as a kit for radio-labeling with Tc-99m. Tc-99m glucoheptonate is kidney- and brain-imaging agent, and can be used in brain-tumor detection[1][2].
|
-
- HY-125102
-
|
|
IGF-1R
|
Cancer
|
|
AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
|
-
- HY-P5608
-
|
|
Bacterial
|
Infection
|
|
Maximin 4 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 4 has cytotoxicity on tumor cells and spermicidal effect .
|
-
- HY-P5609
-
|
|
Bacterial
|
Infection
|
|
Maximin 5 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 5 has cytotoxicity on tumor cells and spermicidal effect .
|
-
- HY-P5604
-
|
|
Bacterial
|
Infection
|
|
Maximin 1 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 1 has cytotoxicity on tumor cells and spermicidal effect .
|
-
- HY-P5605
-
|
|
Bacterial
|
Infection
|
|
Maximin 2 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 2 has cytotoxicity on tumor cells and spermicidal effect .
|
-
- HY-16110
-
|
UFT; BMS-200604
|
Thymidylate Synthase
|
Cancer
|
|
Tegafur-Uracil (UFT; BMS-200604) is an effective oral chemotherapy drug based on fluoropyrimidine. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used in combination with leucovorin (LV) and polysaccharide K (PSK) for research on solid tumors .
|
-
- HY-129087
-
|
|
Apoptosis
|
Cancer
|
|
BC-1258，an F-box/LRR-repeat protein 2 (FBXL2) activator，can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells，and profoundly inhibits tumor formation in mice .
|
-
- HY-103711R
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Estramustine (Standard) is the analytical standard of Estramustine. This product is intended for research and analytical applications. Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].
|
-
- HY-D1464
-
CH1055
1 Publications Verification
|
Fluorescent Dye
|
Cancer
|
|
CH1055 is a NIR-II fluorophore based on a synthetic 970-Da organic molecule. CH1055 is a rapidly excreted dye (∼90% excreted through the kidneys within 24 h). CH1055 also allows targeted molecular imaging of tumors in vivo when conjugated with anti-EGFR Affibody .
|
-
- HY-N10390
-
|
|
Others
|
Cancer
|
|
3β-Hydroxylanosta-8,24-dien-21-al is a lanostane-type triterpene. 3β-Hydroxylanosta-8,24-dien-21-al can inhibit the tumor promotion, reducing the percentage of mice bearing papillomas .
|
-
- HY-143615
-
|
|
RET
|
Cancer
|
|
RET-IN-10 is a potent inhibitor of RET. RET loss of function mutations leads to Hirschsprung's disease, while its gain of function mutations is associated with a variety of human tumors. RET-IN-10 has the potential for the research of cancer diseases (extracted from patent WO2021135938A1, compound 18) .
|
-
- HY-117707
-
|
|
Raf
|
Cancer
|
|
EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
|
-
- HY-168088
-
|
|
HDAC
DNA Methyltransferase
|
Cancer
|
|
DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .
|
-
- HY-160708
-
|
|
Tie
|
Cancer
|
|
Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC50=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .
|
-
- HY-154850
-
|
|
STING
|
Cancer
|
|
F-CRI1 is a potent STING agonist with a Kd value of 40.62 nM. F-CRI1 is a radioactive probe with 18F-labeled modification. F-CRI1 can be used to study STING visualization in the tumor microenvironment .
|
-
- HY-N7623
-
|
|
Drug Derivative
|
Cancer
|
|
Ursonic acid methyl ester is an esterified derivative of Ursolic acid (HY-N0140). Ursonic acid methyl ester shows growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 µg/ml .
|
-
- HY-164547
-
|
|
Porcupine
Wnt
β-catenin
|
Cancer
|
WHN-88 is a Porcupine (PORCN) inhibitor. WHN-88 can eliminate the palmitoylation of Wnt ligands, preventing their secretion and subsequent Wnt/β-catenin signaling. WHN-88 can inhibit cancer cell stemness and suppress the occurrence and development of breast tumors in MMTV-Wnt1 transgenic mice .
|
-
- HY-122641
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Deltasonamide 1 is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
|
-
- HY-156996
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
AGI-134 is a fully synthetic alpha-Gal glycolipid. AGI-134 invokes CD8+ T cell-mediated immunity. AGI-134 induces tumor cell destruction and phagocytosis .
|
-
- HY-155645
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 15 (compound 2g) is a Topoisomerase II inhibitor. Topoisomerase II inhibitor 15 potently is an apoptotic inducer with greater selectivity against head and neck tumors .
|
-
- HY-109963
-
-
- HY-D2345
-
|
|
Fluorescent Dye
Carbonic Anhydrase
|
Cancer
|
|
GZ22-4 is a near-infrared (NIR) fluorescent probe. GZ22-4 shows high affinity for carbonic anhydrase IX (CAIX), with a Kd of 0.2 nM. GZ22-4 can be used for the research of visualize CAIX-positive tumors .
|
-
- HY-P99192
-
|
LY2875358
|
c-Met/HGFR
|
Cancer
|
|
Emibetuzumab (LY2875358) is a humanized bivalent MET antibody (IgG4 type). Emibetuzumab shows high neutralization and internalization activities, resulting in inhibition of both HGF-dependent and HGF-independent MET pathway activation and tumor growth. Emibetuzumab can be used in study of cancer .
|
-
- HY-115492
-
|
|
PKC
|
Cancer
|
|
NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis .
|
-
- HY-D0226
-
|
1,4-Dihydroxyanthraquinone
|
DNA/RNA Synthesis
Fungal
|
Infection
Cancer
|
|
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth .
|
-
- HY-160818
-
MC3138
1 Publications Verification
|
Sirtuin
|
Cancer
|
|
MC3138 is a selective SIRT5 activator. MC3138 has antitumor activity on human PDAC cells, with IC50 values of 25.4-236.9 μM. MC3138 combined with Gemcitabine (HY-17026) significantly inhibits tumor growth in mice .
|
-
- HY-152859
-
|
BI 907828
|
E1/E2/E3 Enzyme
MDM-2/p53
|
Cancer
|
|
Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research .
|
-
- HY-168022
-
|
|
Aurora Kinase
|
Cancer
|
CAM2602 is an Aurora A-TPX2 interaction inhibitor that has a binding affinity of 19 nM to Aurora A. CAM2602 can inhibit the growth of pancreatic cancer cells. In solid tumor transplant models, CAM2602 can increase the proportion of PH3 positive cells while reducing the proportion of P-Thr288 Aurora A positive cells, thereby inhibiting tumor growth .
|
-
- HY-122641D
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
|
-
- HY-100219
-
|
|
VD/VDR
|
Cancer
|
|
CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM .
|
-
- HY-164496
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KL-50 is a selective toxin toward tumors that lack the DNA repair protein O 6-methylguanine-DNA-methyltransferase (MGMT), which reverses the formation of O 6-alkylguanine lesions. KL-50 activates DNA damage response pathways and cycle arrest in MGMT-cells, independent of mismatch repair (MMR). KL-50 is promising for research of brain tumors that lack the DNA repair protein MGMT .
|
-
- HY-100433
-
|
|
PDI
|
Cancer
|
|
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues . PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-143869
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-28 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-28 enhances the body's anti-tumor immunity. HPK1-IN-28 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 1) .
|
-
- HY-143870
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-29 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-29 enhances the body's anti-tumor immunity. HPK1-IN-29 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 38) .
|
-
- HY-D1464A
-
|
|
Fluorescent Dye
|
Cancer
|
|
CH1055 triethylamine is a NIR-II fluorophore based on a synthetic 970-Da organic molecule. CH1055 triethylamine is a rapidly excreted dye (∼90% excreted through the kidneys within 24 h). CH1055 triethylamine also allows targeted molecular imaging of tumors in vivo when conjugated with anti-EGFR Affibody .
|
-
- HY-10058
-
|
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
|
AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo .
|
-
- HY-P3139
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 is a potent inhibitor of the?PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-116879
-
|
(2E)-4-Oxo-2-nonen-8-ynal; alkynyl-4-ONE
|
Biochemical Assay Reagents
|
Cancer
|
|
4-Oxo-2-Nonenal Alkyne ((2E)-4-Oxo-2-nonen-8-ynal; alkynyl-4-ONE) is a functionalized lipid electrophile that conjugated to the exosomes via the reaction of amino and aldehyde groups. 4-Oxo-2-Nonenal Alkyne can be used in tumor exosomes determination .
|
-
- HY-W005288
-
|
4-Hydroxystyrene
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
|
-
- HY-122856
-
|
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-101309A
-
|
|
5-HT Receptor
|
Cancer
|
|
5-(Nonyloxy)tryptamine oxalate, a high-affinity agonist for the 5-HTIDβ receptor, with an ED50 value of 68 nM. 5-(Nonyloxy)tryptamine oxalate, exhibits antitumor growth activity in vivo and enhances the ability of T cells to target tumor cells .
|
-
- HY-D0208
-
|
Uranine sodium
|
Fluorescent Dye
|
Cancer
|
|
Fluorescein (Uranine) sodium is widely used as a fluorescent tracer in medicinal and biological applications and tumor infected tissues tracer. Fluorescein (Uranine) sodium is a representative green fluorophore that has been widely used as a scaffold of practically useful green fluorescent probes .
|
-
- HY-119459
-
|
|
Succinate Dehydrogenase
Fungal
Constitutive Androstane Receptor
Caspase
NF-κB
|
Infection
Cancer
|
|
Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic .
|
-
- HY-145734A
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-145734
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-N1381R
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Periplocin (Standard) is the analytical standard of Periplocin. This product is intended for research and analytical applications. Periplocin is a cardiotonic steroid isolated from root-bark Periploca sepium Bunge. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase .
|
-
- HY-P4910
-
|
|
Proteasome
Apoptosis
|
Cancer
|
|
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .
|
-
- HY-P2251
-
|
|
HIV
Microtubule/Tubulin
|
Infection
Inflammation/Immunology
Cancer
|
|
T-peptide, a Tuftsin analog, can be used for the research of human immunodeficiency virus (HIV) infection. T-peptide prevents cellular immunosuppression and improves survival rate in septic mice. T-peptide also can inhibit the growth of residual tumor cells after surgical resection .
|
-
- HY-147567
-
|
|
ATM/ATR
DNA-PK
PI3K
|
Cancer
|
|
ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively .
|
-
- HY-15782
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
YH16899 binds Lysyl-tRNA synthetase (KRS), and inhibits membrane translocation of KRS. YH16899 impares the interaction of KRS with 67LR. YH16899 inhibits tumor metastasis in mouse models .
|
-
- HY-132173
-
|
|
Bcl-2 Family
|
Cancer
|
|
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo .
|
-
- HY-161821
-
|
|
Interleukin Related
TNF Receptor
MMP
|
Cancer
|
|
Antitumor agent-173 (Compound 4b) is a prodrug of Cycloicaritin (HY-N1940). Antitumor agent-173 is a substrate for OATP2B1. Antitumor agent-173 selectively inhibits the growth of tumor Antitumor agent-173 significantly increases the oral bioavailability of Cycloicaritin and exerts good antitumor activity and safety .
|
-
- HY-145406
-
|
|
Adenosine Receptor
HDAC
|
Inflammation/Immunology
Cancer
|
|
IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
|
-
- HY-B0392
-
-
- HY-101266B
-
|
DS-3032b; DS-3032 tosylate hydrate
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis .
|
-
- HY-101266
-
|
DS-3032
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis .
|
-
- HY-160047
-
|
|
PDGFR
|
Cancer
|
|
AX102 sodium is a 34 bp length nucleotide aptamer modified at the 5' end with a 40 kDa polyethylene glycol moiety. AX102 selectively binds platelet-derived growth factor B (PDGF-B) and causes tumor vessel regression .
|
-
- HY-149672
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
ABBV-467 is a selective MCL-1 inhibitor (Ki: <0.01 nM). ABBV-467 induces apoptosis. ABBV-467 induces cancer cell death and inhibits tumor growth in models of hematological malignancies, such as multiple myeloma .
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-
- HY-158251
-
|
|
Others
|
Cancer
|
|
BIBD-300 is a PARP-1 imaging agent with high affinity for PARP-1. BIBD-300 can accurately localize C6 and U87MG tumors, which can be used for research in the diagnosis of breast cancer, prostate cancer, glioma, and liver cancer .
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-
- HY-126856
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM . HC-Toxin induces tumor cell apoptosis and has anticancer effects .
|
-
- HY-128075R
-
|
|
Herbicide
|
Cancer
|
|
Acifluorfen (Standard) is the analytical standard of Acifluorfen. This product is intended for research and analytical applications. Acifluorfen, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen causes strong photooxidative destruction of pigments and lipids in sensitive plant species .
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-
- HY-128749A
-
|
Calcium D-glucarate tetrahydrate
|
Endogenous Metabolite
|
Cancer
|
|
D-Glucaric acid tetrahydrate is the end-products of the D-glucuronic acid pathway in mammals. D-Glucaric acid tetrahydrate is also found in fruits and vegetables. D-Glucaric acid tetrahydrate can be used to reduce cholesterol and inhibits tumor development. D-Glucaric acid tetrahydrate also enhances human immunity and reduce cancer risks .
|
-
- HY-126830
-
|
|
Antifolate
Apoptosis
|
Cancer
|
|
Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed .
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-
- HY-131904A
-
|
|
Enolase
Parasite
|
Infection
Cancer
|
|
Hex is an enolase inhibitor and antimalarial agent with Ki values of 74.4 nM and 269.4 nM for ENO2 and ENO1, respectively. Hex is a NfENO and TbENO inhibitor with IC50s value of 0.14 μM and 2.1 μM, respectively. Hex has antimalarial activity against Plasmodium falciparum 3D7, Naegleria fowleri trophozoites and Plasmodium berghei ANKA strain. Hex has anti-tumor effects against intracranial tumors .
|
-
- HY-100591
-
|
|
Sirtuin
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
|
-
- HY-137473
-
|
Pyropheophorbide-a methyl ester
|
Apoptosis
|
Cancer
|
|
Methyl pyropheophorbide-a (Pyropheophorbide-a methyl ester), a chlorophyll-a derivative, is a potent photosensitizer that can be used in photodynamic therapy (PDT) of cancer. Methyl pyropheophorbide-a has photodynamic activity and can induce apoptosis and inhibit tumor growth .
|
-
- HY-160169
-
-
- HY-P3333
-
|
|
MHC
|
Inflammation/Immunology
Cancer
|
|
KSPWFTTL is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes .
|
-
- HY-163099
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
P5(PEG24)-VC-PAB-Exatecan (LP5) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG24)-VC-PAB-Exatecan can be used for the research of tumor .
|
-
- HY-162382
-
|
|
PI3K
Akt
mTOR
|
Cancer
|
|
KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response .
|
-
- HY-W355129
-
|
2-Amino-3,8-dimethylimidazo[4,5-f]quinoxaline-2
|
Cytochrome P450
|
Cancer
|
|
MeIQx, a dietary aromatic amine, is mutagenic compound could be isolated from present in fried beef and beef extracts. MeIQx binds covalently to hemoglobin. MeIQx induces liver tumors .
|
-
- HY-P3139A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-P2615
-
|
|
Fluorescent Dye
|
Cancer
|
|
Ac-VDVAD-AFC is a caspase-specific fluorescent substrate. Ac-VDVAD-AFC can measure caspase-3-like activity and caspase-2 activity and can be used for the research of tumor and cancer .
|
-
- HY-161324
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
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-
- HY-N12141
-
|
|
Apoptosis
|
Inflammation/Immunology
|
|
Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome .
|
-
- HY-W034551
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Others
Cancer
|
|
DOTA-tri(t-butyl ester) belongs to the DOTA class of chelating agents. DOTA-tri(t-butyl ester) is a key raw material for synthesizing nanospherical magnetic resonance imaging (MRI) contrast agents, which are used in MR angiography and tumor angiogenesis imaging .
|
-
- HY-N10307
-
|
|
Fungal
Bacterial
Endogenous Metabolite
|
Infection
Cancer
|
|
Anserinone B is an antifungal and antibacterial benzoquinone. Anserinone B causes radial growth reductions of 50% and 37% against S.fimicola and A. furfuraceus, respectively. Anserinones B also displays moderate cytotoxicity in the NCI’s 60 human tumor cell line panel (GI50=4.4 µg/mL) .
|
-
- HY-W008449R
-
|
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
1-Methylxanthine (Standard) is the analytical standard of 1-Methylxanthine. This product is intended for research and analytical applications. 1-Methylxanthine, a caffeine derivative, is an essential human urinary metabolite of caffeine and theophylline (1,3-dimethylxanthine, TP) . 1-Methylxanthine enhances the radiosensitivity of tumor cells .
|
-
- HY-W009245
-
|
|
HIV
|
Infection
Cancer
|
|
Bz-RS-iSer(3-Ph)-OMe (compound 2), a Taxol derivative, inhibits HSV replication cycle at low cytotoxicity, blocks mitotic divisions of Vero cells, influences M-MSV induced tumor size and affects immune response by inhibiting PHA-induced T lymphocyte proliferation .
|
-
- HY-118893
-
|
|
Antibiotic
Bacterial
Fungal
Molecular Glues
|
Infection
Cancer
|
|
Asukamycin, a manumycin-type metabolite, could be isolated from Streptomyces nodosus subsp. asukaensis. Asukamycin is an antibiotic and has antimicrobial activity. Asukamycin inhibits growth of various tumor cell lines .
|
-
- HY-N1022
-
|
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
11-Hydroxytephrosin is a potent inhibitor of NF-kappaB. NF-kappaB is known to play a crucial role in the regulation of genes controlling the immune system, apoptosis, tumor cell growth, and tissue differentiation .
|
-
- HY-124056
-
|
|
CXCR
|
Cancer
|
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-124944
-
|
|
Ras
|
Cancer
|
|
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity .
|
-
- HY-P3333A
-
|
|
MHC
|
Inflammation/Immunology
Cancer
|
|
KSPWFTTL TFA is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL TFA can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes .
|
-
- HY-18933
-
|
|
Akt
|
Cancer
|
|
BI-69A11 is an AKT inhibitor that can effectively suppress the phosphorylation of AKT. BI-69A11 exhibits anticancer activity and can lead to the death of melanoma cells and prostate tumor cells .
|
-
- HY-160169A
-
-
- HY-134904
-
|
RM-006
|
mTOR
|
Cancer
|
|
RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors .
|
-
- HY-P99542
-
|
SAR-408701; HuMAb2-3-SPDB-DM4
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Tusamitamab ravtansine (SAR-408701) is a targeted ADC against tumor cells expressing CEACAM5, composed of a humanized anti-CEACAM5 monoclonal antibody covalently linked to the potent cytotoxic agent, maytansinoid DM4 (HY-12454), via a cleavable linker. Tusamitamab ravtansine has an average drug-to-antibody ratio (DAR) of 3.8 .
|
-
- HY-160597
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) is an exatecan (HY-13631) derivative that can be used as a payload in drug conjugates. Exatecan-amide-bicyclo[1.1.1]pentan-1-ol has significant inhibitory activity against a variety of tumor cell lines .
|
-
![Exatecan-amide-bicyclo[1.1.1]pentan-1-ol](//file.medchemexpress.com/product_pic/hy-160597.gif)
- HY-144671
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-N6578
-
|
|
Others
|
Cancer
|
|
3-epi-Isocucurbitacin B (Compound 5) is a cucurbitane triterpene derived from Trichosanthes kirilowii. 3-epi-Isocucurbitacin B shows significant cytotoxicity to human tumor cells A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT15 .
|
-
- HY-W008449S2
-
|
|
Drug Metabolite
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
|
1-Methylxanthine-d3 is deuterated labeled 1-Methylxanthine (HY-W008449). 1-Methylxanthine, a caffeine derivative, is an essential human urinary metabolite of caffeine and theophylline (1,3-dimethylxanthine, TP) . 1-Methylxanthine enhances the radiosensitivity of tumor cells .
|
-
- HY-144669
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-117563
-
|
SKI 5C
|
SphK
|
Cancer
|
|
CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research .
|
-
- HY-P0023
-
|
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM . Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface .
|
-
- HY-125664
-
|
|
Antibiotic
|
Cancer
|
|
Lucialdehyde B is a tetracyclic triterpene isolated from the substrates of Ganoderma lucidum with antiviral and cytotoxic activities. Lucialdehyde B has cytotoxic effects against Lewis lung cancer (LLC), T-47D, Sarcoma 180 and Meth-A tumor cell lines .
|
-
- HY-P5606
-
|
|
Bacterial
|
Infection
|
|
Maximin 3 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 3 has cytotoxicity on tumor cells and spermicidal effect. Maximin 3 has significant anti-HIV activity .
|
-
- HY-105155
-
|
RMP 7
|
Bradykinin Receptor
|
Cancer
|
|
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
|
-
- HY-P2615A
-
|
|
Fluorescent Dye
|
Cancer
|
|
Ac-VDVAD-AFC TFA is a caspase-specific fluorescent substrate. Ac-VDVAD-AFC TFA can measure caspase-3-like activity and caspase-2 activity and can be used for the research of tumor and cancer .
|
-
- HY-16726
-
|
CG100649
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-P0023A
-
|
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM . Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface .
|
-
- HY-169327
-
|
|
PROTACs
MDM-2/p53
|
Cancer
|
|
MD-265 is a PROTAC degrader that can break down MDM2, leading to activation of p53 in cancer cells carrying wild-type p53. MD-265 achieves complete tumor regression and improves long-term survival of mice with leukemia. (Pink: MI-1063 (HY-133754); Black: linker; Blue: Lenalidomide (HY-A0003) .
|
-
- HY-158050
-
|
|
c-Fms
|
Cancer
|
|
PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .
|
-
- HY-N2584A
-
|
|
HSV
|
Infection
Cancer
|
|
Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV) .
|
-
- HY-168094
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-30 (Compound 3) is a specific and potent PARP1 inhibitor with cytotoxicity. PARP1-IN-30 allows precise inhibition of PARP1 in tumor cells with breast cancer 1 protein (BRCA1) or BRCA2 deficiencies. PARP1-IN-30 is promising for research of cancers .
|
-
- HY-110201
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
|
-
- HY-P10052
-
|
|
VEGFR
|
Cancer
|
|
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. CBO-P11 is modified with a nearinfrared cyanine dye bearing an alkyne function, allowing both “click” coupling on azido-modified nanoparticles and fluorescence labelling .
|
-
- HY-W021040
-
|
CGA-173506
|
Fungal
Apoptosis
|
Infection
Cancer
|
|
Fludioxonil (CGA-173506) is a phenylpyrrole-type fungicide with oral activity that can inhibit the growth of S. sclerotiorum. Fludioxonil promotes tumor growth and metastasis, and induces cardiac toxicity. Fludioxonil causes cytoskeletal disruption, DNA damage, and apoptosis in mouse glioma cells .
|
-
- HY-132822
-
|
SBP-101
|
Others
|
Cancer
|
|
Ivospemin (SBP-101) is an antineoplastic spermine analog. Ivospemin has shown efficacy in slowing pancreatic and ovarian tumor progression in vitro and in vivo. Ivospemin shows modest induction of polyamine catabolism, but stronger repression of ornithine decarboxylase activity. Ivospemin is promising for research of cancers .
|
-
- HY-171281
-
|
MIR200C
|
MicroRNA
|
Cancer
|
|
Human microRNA 200c (MIR200C), a nucleotide small endogenous non-coding RNA, is an illustrious tumor suppressor. Human microRNA 200c is one of the highly studied miRNAs in terms of development, stemness, proliferation, epithelial-mesenchymal transition (EMT), therapy resistance, and metastasis .
|
-
- HY-156457
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
|
-
- HY-P2617
-
|
|
Caspase
|
Inflammation/Immunology
Cancer
|
|
Ac-WEHD-AFC is a fluorogenic caspase-1 substrate. Ac-WEHD-AFC can measure caspase-1 fluorogenic activity and can be used for the research of tumor and inflammation .
|
-
- HY-118269
-
|
|
c-Met/HGFR
|
Cancer
|
|
OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
|
-
- HY-164525
-
|
SC-81490; PF-02881307
|
MMP
|
Cancer
|
|
SD-7300 (SC-81490) is an orally active inhibitor of MMP-2, MMP-9, and MMP-13 with Ki values ??of 0.03, 0.01, and 0.03 nM, respectively. SD-7300 can reduce the degradation of extracellular matrix by tumor cells, thereby inhibiting the invasion and metastasis of tumor cells. In addition, SD-7300 is also a dose-dependent inhibitor of mouse corneal angiogenesis and an inhibitor of interleukin-1-induced bovine cartilage degradation. SD-7300 can be used in breast cancer research .
|
-
- HY-146323
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-58 (Compound C18) is an anti-tumor agent. Antitumor agent-58 effectively inhibits colony formation and cell migration of MGC-803 cells. Antitumor agent-58 induces apoptosis of MGC-803 cells through activation of the p38 and JNK signaling pathways. Antitumor agent-58 induces mitochondrial dysfunction of MGC-803 cells. Antitumor agent-58 effectively inhibits tumor growth of xenograft model bearing MGC-803 cells .
|
-
- HY-P99687
-
|
AMG 256
|
PD-1/PD-L1
|
Cancer
|
|
Latikafusp (AMG 256) is a bifunctional fusion protein comprising a PD-1-targeting antibody and IL-21 mutein designed to deliver IL-21 pathway stimulation to PD-1+ cells. Latikafusp is designed to prime and extend the activity of cytotoxic and memory T cells and induce anti-tumor immunity. Latikafusp has the potential for solid tumors research .Latikafusp may lead to the development of immunogenicity-mediated responses .
|
-
- HY-132192
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model .
|
-
- HY-132192A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model .
|
-
- HY-N5034
-
|
Monoaminoethyl phosphate; NSC 254167; O-Phosphoethanolamine
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Phosphorylethanolamine (Monoaminoethyl phosphate) is a membrane phospholipid and an important precursor of Phosphatidylcholine (HY-B2233B). It is found in most animal tissues and various human extracranial tumors, playing a critical role in membrane integrity, cell division, mitochondrial respiratory function, and more. Studies have shown that changes in the abundance of Phosphorylethanolamine are associated with Alzheimer's disease and Parkinson's disease. Lowering the ratio of Phosphorylethanolamine to Phosphatidylcholine in the liver can improve insulin signaling. Phosphorylethanolamine holds promise for research in the fields of cancer, neurodegenerative disorders, and metabolic diseases .
|
-
- HY-144070A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1) .
|
-
- HY-153935
-
-
- HY-50895B
-
|
ZD 1839 dihydrochloride
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
|
-
- HY-50895
-
|
ZD1839
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
|
-
- HY-142221
-
|
|
PD-1/PD-L1
|
Cancer
|
|
ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC50 value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections .
|
-
- HY-D0226R
-
|
|
DNA/RNA Synthesis
Fungal
|
Infection
Cancer
|
|
Quinizarin (Standard) is the analytical standard of Quinizarin. This product is intended for research and analytical applications. Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth .
|
-
- HY-135899
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway. .
|
-
- HY-123130
-
|
|
MMP
|
Cancer
|
|
ABT-770 (compound 11) is a highly selective and orally active MMP inhibitor, demonstrating over 1000-fold selectivity for MMP-2 (IC50=4 nM) compared to MMP-1 (IC50=4600 nM). ABT-770 can be utilized in studies related to tumor growth, invasion, and metastasis .
|
-
- HY-106168
-
|
NB1011
|
Thymidylate Synthase
|
Cancer
|
|
Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin) .
|
-
- HY-W018723
-
|
p-Aminobenzamidine dihydrochloride
|
Ser/Thr Protease
PAI-1
|
Cardiovascular Disease
Cancer
|
|
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor. 4-Aminobenzamidine dihydrochloride acts as an orally active urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine dihydrochloride can be used for cardiovascular diseases and anti-tumor study .
|
-
- HY-N0797R
-
|
|
P-glycoprotein
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
(20S)-Protopanaxadiol (Standard) is the analytical standard of (20S)-Protopanaxadiol. This product is intended for research and analytical applications. 20S-protopanaxadiol (aPPD) is a metabolite of ginseng saponins, inhibits Akt activity and induces apoptosis in various tumor cells .
|
-
- HY-171543
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-37 (Compound 8) is an orally active and selective poly(ADP-ribose) polymerase 1 and 2 (PARP1/2) inhibitor with an IC50 value of 24 nM for PARP1. PARP1-IN-37 inhibits PARP activity in cells with an EC50 value of 3.7 μM. PARP1-IN-37 is promising for research of BRCA-mutated tumors, such as breast and ovarian cancers .
|
-
- HY-133590
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Heliotrine N-oxide is the corresponding PA (pyrrolizidine alkaloid) N-oxide of Heliotrine (HY-126128). Heliotrine N-oxide leads to the formation of pyrrolic DNA adducts and potential initiation of PA-induced liver tumors in vivo .
|
-
- HY-108647
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation .
|
-
- HY-P99605
-
|
PRS 343
|
EGFR
TNF Receptor
|
Cancer
|
|
Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
|
-
- HY-N0815
-
|
Bufogenin; Recibufogenin
|
PI3K
Akt
NF-κB
AP-1
GSK-3
CDK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma .
|
-
- HY-P2617A
-
|
|
Caspase
|
Inflammation/Immunology
Cancer
|
|
Ac-WEHD-AFC TFA is a fluorogenic caspase-1 substrate. Ac-WEHD-AFC TFA can measure caspase-1 fluorogenic activity and can be used for the research of tumor and inflammation .
|
-
- HY-P99258
-
|
OMP 52M51; Anti-Human NOTCH1 Recombinant Antibody
|
Notch
|
Cancer
|
|
Brontictuzumab (OMP 52M51) is a monoclonal antibody (MAb) that inhibits Notch1 signal. Brontictuzumab selectively binds the negative regulatory region of the Notch1. Brontictuzumab inhibits tumor cell proliferation. Brontictuzumab can be used in the research of leukemia and lymphoma .
|
-
- HY-147696
-
|
|
HSP
AMPK
Reactive Oxygen Species
|
Cancer
|
|
SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells .
|
-
- HY-126034
-
|
|
Ser/Thr Protease
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
3,4-Dichloroisocoumarin is a potent serine-protease and SrLip inhibitor (Ki for SrLip: 26.6 μM). 3,4-Dichloroisocoumarin is opened by serine proteases and then undergoes acylation with the enzyme, thereby inhibiting protease activity. 3,4-Dichloroisocoumarin can induce DNA fragmentation and Apoptosis. 3,4-Dichloroisocoumarin can be used in the research of multiple fields such as tumors, cardiovascular disease and enzyme catalytic mechanisms .
|
-
- HY-155229
-
-
- HY-157317
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-126 (Compound II4) is a photoactive (IC50= 0.149) anticancer agent with significant near-infrared fluorescence emission at 650-760 nm. Antitumor agent-126 has antiproliferative activity and can induce apoptosis after laser irradiation. Antitumor agent-126 effectively inhibits tumor growth in mouse xenograft models exposed to 650 nm laser irradiation. Antitumor agent-126 can be used in cancer research .
|
-
- HY-157055
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1-IN-25 (compound 43) is a potent PD-1/PD-L1 interaction inhibitor with an IC50 value of 10.2 nM in the HTRF assay. PD-1-IN-25 can promote CD8+ T cell activation through inhibiting PD-1/PD-L1 cellular signaling. PD-1-IN-25 delays the tumor growth .
|
-
- HY-P2300
-
|
Cyclo(RGDfC)
|
Integrin
|
Cancer
|
|
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors .
|
-
- HY-115537
-
|
|
Apoptosis
|
Cancer
|
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo .
|
-
- HY-N0247R
-
|
|
Smo
|
Cancer
|
|
Saikosaponin B1 (Standard) is the analytical standard of Saikosaponin B1. This product is intended for research and analytical applications. Saikosaponin B1 is a bioactive constituent of Radix Bupleuri with anticancer activity. Saikosaponin B1 significantly inhibits tumor growth in Medulloblastoma (MB) model by inhibiting the Hedgehog pathway through targeting SMO .
|
-
- HY-126932
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites .
|
-
- HY-146540
-
|
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
MDM-2/p53
|
Cancer
|
|
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth .
|
-
- HY-117980
-
|
AB 132
|
DNA/RNA Synthesis
|
Cancer
|
|
Meturedepa (AB 132) functions as a radiation sensitizer, enhancing the biological effects of radiation. When combined with suboptimal doses of X-ray radiation, this combined therapy achieves better outcomes in terms of tumor shrinkage compared to Meturedepa used alone. Meturedepa is applicable in the research of bronchogenic carcinoma .
|
-
- HY-157793
-
|
|
Toll-like Receptor (TLR)
NF-κB
MAPKAPK2 (MK2)
|
Inflammation/Immunology
Cancer
|
|
SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4 + T and CD8 + T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases .
|
-
- HY-162010
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile.
MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors treatment research .
|
-
- HY-142452
-
|
|
Raf
|
Cancer
|
|
Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B) .
|
-
- HY-145441
-
|
|
Drug Derivative
|
Cancer
|
|
GEM–IB is the conjugate of gemcitabine (GEM)-5'-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS) .
|
-
- HY-119339
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity .
|
-
- HY-118837
-
|
|
ROCK
|
Cancer
|
|
WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer .
|
-
- HY-13062
-
|
Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride
|
Topoisomerase
DNA/RNA Synthesis
ADC Cytotoxin
Bacterial
Autophagy
Apoptosis
Antibiotic
|
Infection
Neurological Disease
Cancer
|
|
Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor .
|
-
- HY-13062A
-
|
Daunomycin; RP 13057; Rubidomycin
|
Topoisomerase
DNA/RNA Synthesis
ADC Cytotoxin
Autophagy
Bacterial
Antibiotic
Apoptosis
|
Infection
Neurological Disease
Cancer
|
|
Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor .
|
-
- HY-P10388
-
|
|
CD47
TGF-β Receptor
|
Cancer
|
|
TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
|
-
- HY-16405
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
|
-
- HY-155176
-
|
|
HDAC
|
Cancer
|
|
SP-2-225 is a selective HDAC6 inhibitor. SP-2-225 enhance the production of cancer-associated antigens and macrophage antigen cross-presentation to T cells. SP-2-225 reduces the tumor volume in a syngeneic SM1 melanoma model .
|
-
- HY-16406
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
|
-
- HY-169076
-
|
|
FLT3
HDAC
Apoptosis
|
Cancer
|
FLT3/HDAC-IN-1 is a dual inhibitor of FLT3/HDAC, with IC50 values of 30.4, 52.4, and 14.7 nM for FLT3, HDAC1, and HDAC3, respectively. FLT3/HDAC-IN-1 can induce apoptosis in MV-4-11 cells and has anti-proliferative effects on FLT3 mutant-transformed BaF3 cells. FLT3/HDAC-IN-1 is being researched for its potential in treating hard-to-treat solid tumors and hematological malignancies .
|
-
- HY-N13176
-
|
|
Autophagy
Apoptosis
PI3K
Akt
mTOR
FAK
|
Cancer
|
Stellettin B is a triterpenoid compound that can be isolated from the marine sponge Jaspis stellifera. Stellettin B induces G1 phase arrest, apoptosis, and autophagy in human non-small cell lung cancer A549 cells by blocking the PI3K/Akt/mTOR pathway. Stellettin B can reduce the migration and invasion of liver cancer cells by decreasing the activation of the MAPK and FAK/PI3K/AKT/mTOR signaling pathways. Stellettin B can be used in the study of various tumors .
|
-
- HY-19916A
-
|
BAL-101553 dihydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1 .
|
-
- HY-19916
-
|
BAL-101553
|
Microtubule/Tubulin
|
Cancer
|
|
Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1 .
|
-
- HY-P99475
-
|
MSB-2311
|
PD-1/PD-L1
|
Cancer
|
|
Betifisolimab (MSB-2311) is a humanized monoclonal antibody directed against the immunosuppressive ligand PD-L1. Betifisolimab has the potential for advanced solid tumors and hematological malignancies research .
|
-
- HY-149631
-
|
|
HDAC
|
Cancer
|
|
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models .
|
-
- HY-115581
-
|
Deoxythymidine 3′,5′-diphosphate; pdTp
|
Apoptosis
|
Cancer
|
|
Thymidine 3',5'-disphosphate (Deoxythymidine 3′,5′-diphosphate; pdTp) is a selective small molecule inhibitor of staphylococcal nuclease and tudor domain containing 1 (SND1, the miRNA regulatory complex RISC subunit) and inhibits SND1 activity. Thymidine 3',5'-disphosphate exhibits anti-tumor efficacy in vivo .
|
-
- HY-144670
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of ALDH3A1 with an IC50 of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination research with docetaxel .
|
-
- HY-121247
-
|
5-Bromotetrandrine; BrTet; W198
|
P-glycoprotein
Drug Derivative
|
Cancer
|
|
Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR). Bromotetrandrine shows significant MDR reversal activity in vitro and in vivo, which may be related to the inhibition of P-gp overexpression and the increase in intracellular accumulation of anticancer agents. Bromotetrandrine is a brominated derivative of tetrandrine, which is promising for MDR modulator for tumor assessment .
|
-
- HY-128749AR
-
|
|
Endogenous Metabolite
|
Cancer
|
|
D-Glucaric acid (tetrahydrate) (Standard) is the analytical standard of D-Glucaric acid (tetrahydrate). This product is intended for research and analytical applications. D-Glucaric acid tetrahydrate is the end-products of the D-glucuronic acid pathway in mammals. D-Glucaric acid tetrahydrate is also found in fruits and vegetables. D-Glucaric acid tetrahydrate can be used to reduce cholesterol and inhibits tumor development. D-Glucaric acid tetrahydrate also enhances human immunity and reduce cancer risks .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-128890
-
|
|
ADC Linker
|
Cancer
|
|
DOTA-NHS-ester is a linker for affibody molecules and is applied in small animals PET, SPECT, and CT. DOTA-NHS-ester can be used to label radiotherapeutic agents or imaging probes for the detection of tumors .
|
-
- HY-136220A
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39) .
|
-
- HY-144749
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
|
-
- HY-B0942
-
|
|
nAChR
Bacterial
Apoptosis
Caspase
|
Infection
Neurological Disease
Cancer
|
|
Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo .
|
-
- HY-157014
-
|
|
Tryptophan Hydroxylase
|
Cancer
|
|
TPT-004 is a TPH inhibitor. TPT-004 has superior pharmacokinetic and pharmacodynamic properties. TPT-004 also has good efficacy in preclinical models of peripheral serotonin attenuation and colorectal tumor growth .
|
-
- HY-101021
-
|
Ilicicolin D
|
STAT
Apoptosis
Antibiotic
|
Inflammation/Immunology
Cancer
|
|
Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity .
|
-
- HY-148569
-
|
|
TMV
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
TMV-IN-3, chalcone derivative, is a tobacco mosaic virus (TMV) inhibitor. TMV-IN-3 has antiviral activity against TMV with an EC50 value of 120.3 μg/mL. TMV-IN-3 can be used for the research of infection, inflammation and tumor .
|
-
- HY-148568
-
|
|
TMV
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
TMV-IN-2, chalcone derivative, is a tobacco mosaic virus (TMV) inhibitor. TMV-IN-2 has antiviral activity against TMV with an EC50 value of 89.9 μg/mL. TMV-IN-2 can be used for the research of infection, inflammation and tumor .
|
-
- HY-157157
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-3 (compound 4B) is a PAD4 inhibitor with antitumor activity in vitro and in vivo. PAD4-IN-3 was covalently linked to RGD sequence peptide-modified chitosan (K-CRGDV), resulting in an enhanced oxidative stress-responsive nanoagent. K-CRGDV-PAD4-IN-3 can actively target tumors, inhibit PAD4 activity, block the formation of neutrophil extracellular traps (NETs), and improve the tumor immune microenvironment in response to the tumor microenvironment .
|
-
- HY-147081
-
|
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
-
- HY-13589A
-
|
LU103793 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) hydrochloride is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin hydrochloride blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin hydrochloride can be used to research anticancer .
|
-
- HY-136220
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 μΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 .
|
-
- HY-16726R
-
|
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (Standard) is the analytical standard of Polmacoxib. This product is intended for research and analytical applications. Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-141464
-
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Fmoc-Asn(Ac3AcNH-beta-Glc)-OH
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Amino Acid Derivatives
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Cancer
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Fmoc-L-Asn(beta-D-GlcNAc(Ac)3)-OH (Fmoc-Asn(Ac3AcNH-beta-Glc)-OH) can be used in the synthesis of silicon-fluoride acceptor (SiFA) derivatized octreotate derivatives. SiFA-octreotate analogues, as tumor imaging agents, are useful tool for the research of positron emission tomography (PET) .
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- HY-160048
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PDGFR
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Cancer
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PEG40K unconjugated/naked AX102 sodium is AX102 without PEG40K conjugation. AX102 is a DNA oligonucleotide aptamer for platelet-derived growth factor PDGF-B. AX102 is 34 bases in length, selectively binds platelet-derived growth factor B (PDGF-B), and causes tumor vessel regression .
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- HY-N3737
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Aurora Kinase
PERK
Reactive Oxygen Species
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Cancer
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Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity .
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- HY-N2584AR
-
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HSV
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Infection
Cancer
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Isoxanthohumol (Standard) is the analytical standard of Isoxanthohumol. This product is intended for research and analytical applications. Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV) .
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- HY-W127505S
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Biochemical Assay Reagents
Isotope-Labeled Compounds
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Others
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trans-2-Undecenal-d5 is deuterated labeled 4-Vinylphenol (HY-W005288). 4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
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- HY-144256
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DNA/RNA Synthesis
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Cancer
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CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties .
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- HY-P99827
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TSR-022; GSK4069889
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Tim3
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Cancer
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Cobolimab (TSR-022) is an anti-TIM-3 monoclonal antibody. Cobolimab mediates the internalization of TIM3 with an IC50 value of 0.4464 nM. Cobolimab has potential application in solid tumors and non-small cell lung cancer (NSCLC) .
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- HY-139662
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E1/E2/E3 Enzyme
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Cancer
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HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers .
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- HY-123334
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Porcupine
Wnt
|
Cancer
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GNF-1331 (compound 19) is a potent, selective and orally bioavailable porcupine inhibitor (IC50=12 nM). GNF-1331 blocks Wnt ligand secretion and subsequent Wnt signaling activity, and induces significant antitumor effects in the mouse MMTV-WNT1 xenograft tumor model .
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- HY-152189
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Others
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Cancer
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S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC50 value of 3.04 nM. S19-1035 can be used for the research of tumor .
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- HY-123310
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Androgen Receptor
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Cancer
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JNJ-26146900 is a potent and orally active androgen receptor antagonist with a Ki value of 400nM for rat AR. JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand. JNJ-26146900 reduces prostate tumor size and prevents bone loss. JNJ-26146900 can be used in research of cancer .
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- HY-135199
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E1/E2/E3 Enzyme
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Cancer
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Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors .
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- HY-147041
-
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GB1211
|
Galectin
|
Inflammation/Immunology
Cancer
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Selvigaltin (GB1211) is an orally active galectin-3 small molecule inhibitor with an IC50 value of 12 nM in rabbits, showing anti-tumor activity. Selvigaltin decreases galectin-3 levels in the liver and reduces biomarkers of liver function (AST, ALT, bilirubin), inflammation (cells foci) and fibrosis (PSR, SHG), as well as decreasing the mRNA and protein expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen). Selvigaltin restores T-cell activity and induces less tumors and metastasis .
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-
- HY-173275
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PDGFR
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Cancer
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PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRα D842V kinase with IC50s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRα D842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study .
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- HY-144746
-
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PD-1/PD-L1
|
Cancer
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|
PD-1/PD-L1-IN-26 (Compound II-14) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 0.0380 μM. PD-1/PD-L1-IN-26 activates the immune microenvironment by promoting the infiltration of CD4+ T cells into tumor tissues. PD-1/PD-L1-IN-26 has the potential for the research of cancer diseases .
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-
- HY-134471
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TNF Receptor
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Inflammation/Immunology
Cancer
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TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis .
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- HY-143439
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Estrogen Receptor/ERR
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Cancer
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LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity .
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-
- HY-151289
-
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TGF-β Receptor
TGF-beta/Smad
|
Cancer
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ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
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- HY-145110
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IGF-1R
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Cancer
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IGF-1R inhibitor-2 (example 121) is an insulin-like growth factor-1 receptor (IGF-1R) inhibitor. Downregulation of IGF-1R can reverse the transformed phenotype of tumor cells and potentially render them susceptible to apoptosis .
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- HY-145688
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HDAC
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Cancer
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HDAC-IN-33 is a potent HDAC inhibitor with IC50s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
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- HY-108876
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Daunomycin(citrate); RP 13057(citrate); Rubidomycin(citrate)
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Topoisomerase
DNA/RNA Synthesis
ADC Cytotoxin
Autophagy
Bacterial
Antibiotic
Apoptosis
|
Infection
Neurological Disease
Cancer
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Daunorubicin (Daunomycin) citrate is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin citrate inhibits DNA and RNA synthesis. Daunorubicin citrate is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin citrate is also an anthracycline antibiotic. Daunorubicin citrate can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor .
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- HY-149410
-
|
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Topoisomerase
|
Cancer
|
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MSN8C, an analog of mansonone E, is a novel catalytic inhibitor of human DNA topoisomerase II. MSN8C induces cancer cell apoptosis. MSN8C shows significant anti-tumor cell proliferation activity in vitro .
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- HY-122912
-
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ALDH1Ai 673A
|
Aldehyde Dehydrogenase (ALDH)
Necroptosis
|
Cancer
|
|
ALDH1A inhibitor 673A is an ALDH1A inhibitor. ALDH1A inhibitor 673A inhibits all three ALDH1A family members (IC50: 246 nM, 230 nM, 348 nM for ALDH1A1, ALDH1A2, ALDH1A3 respectively. ALDH1A inhibitor 673A induces necroptotic cell death preferentially in CD133+ ovarian CSCs. ALDH1A inhibitor 673A also inhibits chemotherapy-resistant tumor growth .
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- HY-131347
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PD-1/PD-L1
|
Inflammation/Immunology
Cancer
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PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects .
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-
- HY-122720
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KL-1
|
Apoptosis
|
Cancer
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SEC inhibitor KL-1 (KL-1) is a peptide-like lead compound that is an effective selective SEC inhibitor. SEC inhibitor KL-1 promotes apoptosis and has anti-tumor activity. SEC inhibitor KL-1 doses dependently inhibits the AFF4-CCNT1 interaction, with a Ki value of 3.48 μM .
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- HY-P1022A
-
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Metastin(human) TFA
|
GnRH Receptor
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Endocrinology
Cancer
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Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion .
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- HY-19827
-
|
(+)-Aeroplysinin-1
|
Bacterial
HIV
Apoptosis
|
Infection
Cancer
|
|
Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells .
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- HY-139104
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DNA/RNA Synthesis
Apoptosis
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Cancer
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Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis .
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- HY-P99562
-
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XmAb-18087
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CD3
|
Cancer
|
|
Tidutamab (XmAb-18087) is a humanized and affinity-optimized bispecific antibody (bsAb) targeting SSTR2 binding domain and T-cell binding domain (CD3). Tidutamab possesses a full Fc domain to maintain long serum half-life.Tidutamab eliminates SSTR+ tumor cells by stimulating redirected T cellmediated cytotoxicity (RTcC) .
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-
- HY-145687
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HDAC
|
Cancer
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|
HDAC-IN-32 is a potent HDAC inhibitor with IC50s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
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- HY-144424
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Trk Receptor
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Cancer
|
|
Trk-IN-11 (Compound 14h) is a potent inhibitor of TRK (IC50 = 1.4, 1.8 nM, against TrkA, TrkA G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-11 has the potential for the research of cancer disease .
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- HY-18969
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CDK
|
Cancer
|
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LDC3140 is a selective CDK7 inhibitor (IC50<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment .
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-
- HY-P1654
-
|
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Integrin
|
Cancer
|
|
A20FMDV2 is a selective αvβ6 integrin inhibitor (IC50: 3 nM), with an activity 1,000-fold more selective for αvβ6 than for other RGD-directed integrins (αvβ3, αvβ5, and α5β1). A20FMDV2 can be derived from the foot-and-mouth disease virus. A20FMDV2 can be radiolabeled for the PET imaging of αvβ6 integrin-positive tumors .
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- HY-13580
-
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Glucocorticoid Receptor
ADC Cytotoxin
|
Inflammation/Immunology
Cancer
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|
Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma .
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- HY-108640
-
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MDM-2/p53
Parasite
Apoptosis
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Infection
Cancer
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HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents . Antimalarial activity .
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- HY-108640A
-
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MDM-2/p53
Parasite
Apoptosis
|
Infection
Cancer
|
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HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents . Antimalarial activity .
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- HY-18652A
-
|
Ro 5126766 potassium; CH5126766 potassium
|
Raf
MEK
|
Cancer
|
|
Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) .
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-
- HY-164493
-
|
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Ras
|
Cancer
|
|
KRASG12C IN-13 (LY3499446) is a potent KRAS G12C inhibitor. KRASG12C IN-13 is promising for research of advanced solid tumors including non-small cell lung cancer and colorectal cancer .
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-
- HY-119711
-
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MMP
|
Cancer
|
|
NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression .
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-
- HY-132229
-
|
|
Trk Receptor
|
Cancer
|
|
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkA G595R and TrkA G667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity .
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-
- HY-115581A
-
|
Deoxythymidine 3′,5′-diphosphate tetrasodium; pdTp tetrasodium
|
Apoptosis
MicroRNA
|
Cancer
|
|
Thymidine 3',5'-diphosphate (Deoxythymidine 3′,5′-diphosphate) tetrasodium is a selective inhibitor of staphylococcal nuclease and tudor domain containing 1 (SND1, the MicroRNA regulatory complex RISC subunit) and [3,5- 2H2] tyrosyl nuclease. Thymidine 3',5'-diphosphate tetrasodium has anti-tumor activity and can also be used as a catalyst in biochemical reactions .
|
-
- HY-131166
-
-
- HY-13062R
-
|
|
Topoisomerase
DNA/RNA Synthesis
ADC Cytotoxin
Bacterial
Autophagy
Apoptosis
Antibiotic
|
Infection
Neurological Disease
Cancer
|
|
Daunorubicin (hydrochloride) (Standard) is the analytical standard of Daunorubicin (hydrochloride). This product is intended for research and analytical applications. Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor .
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-
- HY-160045
-
|
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Cholecystokinin Receptor
|
Cancer
|
|
AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
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-
- HY-119217
-
AZ084
2 Publications Verification
|
CCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma . AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer .
|
-
- HY-144273
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. IDO1-IN-13 has cellular IDO1 inhibition (HeLa EC50= 30 nM). IDO1-IN-13 decreases 51% of the kyn/trp ratio in SK-OV-3 xenograft tumor tissues .
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-
- HY-W715630
-
|
|
Topoisomerase
|
Cancer
|
|
Salvicine is a DNA topoisomerase II inhibitor (IC50=3 μM). Salvicine increases the interaction between DNA and Topo II by interacting with the ATPase domain, inhibiting DNA degradation and ATP hydrolysis. Salvicine has anticancer activities, including inhibiting Topo II, causing DNA damage, overcoming multidrug resistance, and inhibiting tumor cell adhesion .
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-
- HY-157288
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
(R)-Phe-A110/B319, a hapten, is a selective binder to tumor-associated antigens. (R)-Phe-A110/B319 has a 20-fold higher affinity towards the H1047R mutant of p110α in the p110α/p85α PI3K complex. (R)-Phe-A110/B319 can be used for the research of conditional chimeric antigen receptor T (CAR-T) cell activation and tumor targeting .
|
-
- HY-W039442
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
2′-Deoxy-2′-fluoroadenosine can be used for the synthesis of 2′-Deoxy-2′-fluoro-modified oligonucleotides hybridized with RNA. 2′-Deoxy-2′-fluoroadenosine can be cleaved efficiently by E. coli purine nucleoside phosphorylase (PNP) to the toxic agent 2-fluoroadenine (FAde). 2′-Deoxy-2′-fluoroadenosine shows excellent in vivo activity against tumors expressing E. coli PNP .
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-
- HY-156130
-
|
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Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth .
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-
- HY-138742
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
|
-
- HY-144371
-
-
- HY-P2229
-
|
SDZ CO 611
|
Somatostatin Receptor
|
Cancer
|
|
Ilatreotide (SDZ CO61), glycated somatostatin derivative, is a highly potent glycated analog of somatostatin with improved oral activity. Ilatreotide can suppress the fasting level and postprandial release of several gastrointestinal and pancreatic hormones. Ilatreotide can be used for the research of gastroenteropancreatic tumors .
|
-
- HY-144638
-
|
|
Apoptosis
|
Cancer
|
|
JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity .
|
-
- HY-170919
-
|
|
FGFR
|
Cancer
|
|
FGFR2/3-IN-2 (compound 10) is an orally active FGFR2 and FGFR3 inhibitor. FGFR2/3-IN-2 inhibits FGFR2 and FGFR3 with IC50s of 3.7 nM and 31.2 nM (preincubation time 1 h), respectively. FGFR2/3-IN-2 spares FGFR1/4 and other kinases without causing diarrhea and serum phosphate elevation in vivo. FGFR2/3-IN-2 induces tumor stasis or regression in the SNU-16 gastric cancer model .
|
-
- HY-19542
-
|
C6-Cer; N-Hexanoylsphingosine
|
Apoptosis
|
Cancer
|
|
C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
|
-
- HY-144720
-
|
|
SWI/SNF Complex
|
Cancer
|
|
BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .
|
-
- HY-162730
-
|
|
Molecular Glues
Phosphodiesterase (PDE)
|
Cancer
|
|
OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor .
|
-
- HY-162589
-
|
|
PROTACs
HSP
Apoptosis
|
Cancer
|
|
Lw13 is a Hsp90-targeting PROTAC and achieves maximum degradation at a concentration of 0.05 μM in Siha cells. Lw13 induces cell apoptosis and exhibits potent anti-tumor activity both in vitro and in vivo(Sturcture Note:(Blue: Cereblon ligand (HY-A0003), Black: linker；Pink: Hsp90 inhibitor SNX-5422 (HY-10213)) .
|
-
- HY-P1022
-
|
Metastin(human)
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) inhibits tumor metastasis and stimulates the secretion of gonadotropin (LH) and testosterone .
|
-
- HY-162881
-
|
|
EGFR
|
Cancer
|
DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
|
-
- HY-134595
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
SENP1-IN-2 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 30. SENP1-IN-2 is developed for tumor radiosensitivity enhancement .
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-
- HY-134594
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement .
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-
- HY-134597
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
SENP1-IN-4 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 21. SENP1-IN-4 is developed for tumor radiosensitivity enhancement .
|
-
- HY-134596
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
SENP1-IN-3 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 17. SENP1-IN-3 is developed for tumor radiosensitivity enhancement .
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-
- HY-15888
-
|
|
BMI1
Autophagy
|
Cancer
|
|
PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment .
|
-
- HY-156578
-
|
|
DGK
HIV
|
Infection
Cancer
|
|
DGKα-IN-8 (Example 51) is a DGKα inhibitor (IC50=22.491 nM; EC50=0.256 nM). DGKα-IN-8 can be used to study cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection .
|
-
- HY-144169
-
|
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
|
Inflammation/Immunology
Cancer
|
|
DHODH-IN-19 is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-19 inhibits tumor growth. DHODH-IN-19 has the potential for the research of cancer and inflammation disease (extracted from patent WO2021238881A1, compound 1) .
|
-
- HY-106218
-
|
5-Fluorocyclocytidine; 5'-Fluorocyclocytidine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Flurocitabine (5-Fluorocyclocytidine) is a fluorinated anlydride analog of cytosine arabinoside, partially hydrolysecl in vivo into two active antitumor substances (arabinosyl-tluorocytosine (ara-FC) and arabinosyl-fluorouracil (ara-FU)). Flurocitabine (5-Fluorocyclocytidine) has antitumor activity during phase I studies in acute leukemia and solid tumors .
|
-
- HY-148567
-
|
|
TMV
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
TMV-IN-1, chalcone derivative, is a tobacco mosaic virus (TMV) inhibitor. TMV-IN-1 has good therapeutic activity and protective activity against TMV with EC50 values of 70.7 μg/mL and 60.8 μg/mL, respectively. TMV-IN-1 can be used for the research of infection, inflammation and tumor .
|
-
- HY-147783
-
|
|
MDM-2/p53
|
Cancer
|
|
Anticancer agent 68 is (Compound 12) is an anti-cancer agent. Anticancer agent 68 arrests the cells at the G2/M phase and induces programmed cell death. Anticancer agent 68 induces upregulation of tumor suppression via activation of p53 & PTEN .
|
-
- HY-103397
-
|
|
Antibiotic
DNA Methyltransferase
Parasite
|
Infection
Cancer
|
|
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells . Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM .
|
-
- HY-153900
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 6 (Compound A) is a TLR8 agonist, with an EC50 of 0.052 μM. TLR8 agonist 6 induces IL-12p40 production in human PBMC (EC50: 0.031 μM). TLR8 agonist 6 can be used in the research of virus resistance, infection resistance, autoimmunity, tumor, etc .
|
-
- HY-146497
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones .
|
-
- HY-135849
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
Catalase, Aspergillus niger is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors . Free oxygen radical scavenger.
|
-
- HY-160053
-
|
|
PDGFR
|
Cancer
|
|
Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM). Gint4.T aptamer sodium inhibits PDGFRβ heterodimerization and EGFR transactivation. It can significantly inhibit cell migration and proliferation, induce differentiation and prevent tumor growth in vivo. Gint4.T aptamer sodium specifically inhibits PDGFRβ-mediated tropism of mesenchymal stem cells (MSCs) toward the tumor microenvironment .
|
-
- HY-118925
-
|
|
Bcl-2 Family
HDAC
Phosphatase
|
Cancer
|
|
Holothurin A is a potent inhibitor against BCL2, HDAC1 and PTPN2 with an anticancer activity, which is derived from sea cucumber Holothuria scabra. Holothurin A plays an essential role in the process of apoptosis, cell cycle and suppressing tumor .
|
-
- HY-155959
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-33 (Compound N11) is a PD-1/PD-L1 inhibitor. PD-1/PD-L1-IN-33 inhibits PD-1 and PD-L1 interaction with an IC50: 6.3 nM. PD-1/PD-L1-IN-33 promotes T-cell proliferation, activation, and infiltration into tumor spheres. PD-1/PD-L1-IN-33 has immunomodulatory and anticancer activity .
|
-
- HY-124813
-
|
113B7
|
FAK
EGFR
MMP
|
Cancer
|
|
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion .
|
-
- HY-163534
-
|
|
PD-1/PD-L1
|
Cancer
|
PD-1/PD-L1-IN-43 (compound Z13) is a small-molecule inhibitors targeting the PD-1/PD-L1 interaction. PD-1/PD-L1-IN-43 exhibites potent in vivo antitumor efficacy against B16-F10 melanoma. PD-1/PD-L1-IN-43 inhibits tumor growth by blocking the interaction between PD-1 and PD-L1. PD-1/PD-L1-IN-43 can be used in anti-tumor studies .
|
-
- HY-108433
-
|
Carnitine palmitoyltransferase 2
|
Apoptosis
MDM-2/p53
|
Metabolic Disease
Cancer
|
|
CPT2 (Carnitine palmitoyltransferase 2), an enzyme that participates in fatty acid oxidation, also is a colorectal cancer (CRC) prognostic biomarker. CPT2 overexpression can activate p-p53 to increase p53 expression, thereby inhibiting tumor proliferation and promoting apoptosis. CPT2 deficiency results in the most common inherited disorder of long-chain fatty acid oxidation affecting skeletal muscle. Downregulation of CPT2 is also highly correlated with the progression of various cancers and has potential for cancer research .
|
-
- HY-154869
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
PD-1/PD-L1-IN-34 (Compound (1S,2S)-A25) inhibits PD-1/PD-L1 interaction (IC50=0.029 μM), with a selected binding affinity with PD-L1 (KD=0.1554 μM). PD-1/PD-L1-IN-34 inhibits tumor growth by activating the immune microenvironment .
|
-
- HY-15888A
-
|
|
BMI1
Autophagy
|
Cancer
|
|
PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment .
|
-
- HY-B0150A
-
|
Niacinamide Hydrochloride; Nicotinic acid amide Hydrochloride
|
Sirtuin
Endogenous Metabolite
HBV
|
Infection
Cancer
|
|
Nicotinamide Hydrochloride is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide Hydrochloride also inhibits SIRT1. Nicotinamide Hydrochloride increases cellular NAD+, ATP, ROS levels. Nicotinamide Hydrochloride inhibits tumor growth and improves survival. Nicotinamide Hydrochloride also has anti-HBV activity .
|
-
- HY-B0150
-
|
Niacinamide; Nicotinic acid amide
|
Organoid
Endogenous Metabolite
Sirtuin
HBV
|
Cancer
|
|
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity .
|
-
- HY-146384
-
|
|
CRM1
|
Cancer
|
|
CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer agent target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer .
|
-
- HY-114133
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
|
Depreotide is a nove tumor tarcer, can be complexed with technetium-99m ( 99mTc-depreotide) for optimal imaging properties. 99mTc-depreotide somatostain receptor imaging has been playing an important role in medical diagnosis research . Depreotide can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-40136R
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
cis-4-Hydroxy-L-proline (Standard) is the analytical standard of cis-4-Hydroxy-L-proline. This product is intended for research and analytical applications. cis-4-Hydroxy-L-proline is an orally active proline analog and collagen production inhibitor. cis-4-Hydroxy-L-proline inhibits cell growth by preventing the deposition of triple helical collagen on the cell layer. cis-4-Hydroxy-L-proline inhibits N-nitrosomethylurea-induced breast tumor growth. cis-4-Hydroxy-L-proline improves lung compliance and reduces prostate weight. cis-4-Hydroxy-L-proline can be used in the study of hypoxic pulmonary hypertension .
|
-
- HY-B0091A
-
|
CD 271 sodium salt
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity .
|
-
- HY-18953
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .
|
-
- HY-B0091
-
|
CD271
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
|
-
- HY-116683
-
|
MAL2-11B
|
HSP
DNA/RNA Synthesis
|
Infection
Cancer
|
|
116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70 .
|
-
- HY-115400
-
1V209
3 Publications Verification
TLR7 agonist T7
|
Toll-like Receptor (TLR)
|
Cancer
|
|
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity .
|
-
- HY-106031
-
|
|
Topoisomerase
|
Cancer
|
|
F-14512 is a targeted cytotoxic compound that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 combines an epipodophyllotoxin core that targets topoisomerase II with a spermine group that acts as a cell delivery vehicle, with improved selectivity for tumor cells. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and demonstrates high potency in multiple human cell lines (median IC50=0.18 μM). In the MX1 breast tumor xenograft model, F-14512 exhibits potent antitumor activity .
|
-
- HY-149540
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
|
-
- HY-156169
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX/XII-IN-7 (compound 3e) is a potent hCA IX and XII inhibitor with Kis of 3.2 nM, 9.2 nM, 503.7 nM and 59 nM for hCA I, hCA II, hCA IX and hCA XII, respectively. hCAIX/XII-IN-7 has the potential for hypoxic tumors research .
|
-
- HY-101870B
-
|
INCB053914 phosphate
|
Pim
|
Cancer
|
|
Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-101870
-
|
INCB053914
|
Pim
|
Cancer
|
|
Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-P99938
-
|
HX008
|
PD-1/PD-L1
|
Cancer
|
|
Pucotenlimab (HX008) is a humanized immunoglobulin G4 (IgG4) anti programmed cell death protein 1 (anti-PD-1) monoclonal antibody. Pucotenlimab can be used for the research of tumor .
|
-
- HY-101597
-
|
|
Apoptosis
|
Cancer
|
|
NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP .
|
-
- HY-162312
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-114357A
-
|
|
TAM Receptor
c-Met/HGFR
Trk Receptor
|
Cancer
|
|
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo .
|
-
- HY-155991
-
|
|
Apoptosis
|
Cancer
|
|
RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity .
|
-
- HY-16350
-
|
NKP-1339; IT-139; KP-1339
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu .
|
-
- HY-P99253
-
|
KW-0761
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Mogamulizumab (KW-0761) is a recombinant anti-CCR4 monoclonal antibody (MAb). Mogamulizumab can eliminate tumor cells by antibody-dependent cellular cytotoxicity (ADCC). Mogamulizumab can be used in the research of cancers, adult T-cell leukemia/lymphoma (ATLL), cutaneous T-cell lymphoma (CTCL) .
|
-
- HY-A0061
-
|
Trifluorothymidine; 5-Trifluorothymidine; TFT
|
Thymidylate Synthase
HSV
Nucleoside Antimetabolite/Analog
Orthopoxvirus
DNA/RNA Synthesis
Apoptosis
Autophagy
|
Cancer
|
|
Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .
|
-
- HY-P99233
-
|
HuMax-TAC
|
Interleukin Related
|
Cancer
|
|
Camidanlumab (HuMax-TAC) is a CD25 monoclonal antibody. Camidanlumab targets the cell-surface antigen CD25, which is over-expressed on a variety of hematological tumors and shows limited expression on normal tissues. Camidanlumab can be used for synthesis of antibody agent conjugates (ADCs) to research several diseases including lymphoma and leukemia .
|
-
- HY-10824
-
|
PT523
|
Antifolate
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth .
|
-
- HY-N15169
-
|
|
IFNAR
CD74
NO Synthase
Arginase
|
Cancer
|
|
BG-136 is an innate immune stimulant isolated from Durvillaea Antarctica that can simultaneously stimulate the activation of both innate and adaptive immune cells in the tumor microenvironment (TME), exerting a broad-spectrum antitumor effect .
|
-
- HY-144036
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4) .
|
-
- HY-W250111
-
|
|
Biochemical Assay Reagents
Apoptosis
Reactive Oxygen Species
Bcl-2 Family
Caspase
|
Cancer
|
|
Carboxymethyl chitosan is a derivative of chitosan. Carboxymethyl chitosan inhibits Apoptosis and ROS. Carboxymethyl chitosan increases the expression of Bcl-2 and reduces the expression of Bax, cytochrome c and caspase-3. Carboxymethyl chitosan inhibits the migration of various cells. Carboxymethyl chitosan exerts antitumor effects on Lewis tumors and hepatocarcinoma .
|
-
- HY-P99643
-
|
UCB6114
|
Dan family
|
Cancer
|
|
Ginisortamab (UCB6114) is a fully human IgG4P anti Gremlin-1 monoclonal antibody, with mean IC50 values of 8.2 nM and 9 nM against human and mouse gremlin-1, respectivly. Ginisortamab inhibits gremlin-1 antagonism of BMP signaling pathways. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors .
|
-
- HY-144657
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo .
|
-
- HY-149541
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
|
-
- HY-172820
-
|
DP303c
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab envedotin (DP303c) is a anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab envedotin is composed of the tubulin polymerization inhibitor Monomethyl auristatin E (MMAE) (HY-15162) to the anti-HER2 antibody DP001 via a cleavable linker. Trastuzumab envedotin can be used for the research of HER2-positive solid tumors, such as breast cancer, colorectal cancer, and gastric cancer .
|
-
- HY-114527
-
|
|
Apoptosis
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
TPMP-I-2 is an anticancer agent that induces cancer cell lines Apoptosis and decreases protein levels of stearoyl-CoA desaturase. TPMP-I-2 prolongs the survival time of nude rats in a simulated micrometastatic cervical cancer model and reduces tumor growth in a breast cancer model in nude mice combined with immunotoxins .
|
-
- HY-100388
-
|
|
SHP2
Phosphatase
|
Cancer
|
|
SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2 D61Y, SHP2E69K, SHP2 A72V, SHP2 E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth .
|
-
- HY-142682
-
|
|
Phosphatase
|
Neurological Disease
Cancer
|
|
SCP1-IN-1 (compound SH T-62) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-1 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-1 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
|
-
- HY-142683
-
|
|
Phosphatase
|
Neurological Disease
Cancer
|
|
SCP1-IN-2 (Compound SH T-65) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-2 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-2 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
|
-
- HY-164645
-
|
|
Ras
|
Cancer
|
|
pan-KRAS-IN-16 (Compound 3344) is an anti-RAS small molecule derived from an intracellular antibody fragment with pan-RAS-effector protein-protein interaction inhibitor properties. pan-KRAS-IN-16 binds to a hydrophobic pocket near to the effector-binding switch regions of RAS. pan-KRAS-IN-16 prevents endogenous RAS-dependent signaling in tumor cell lines .
|
-
- HY-P99386
-
|
MNRP-1685A
|
Complement System
EGFR
PDGFR
p38 MAPK
|
Cancer
|
|
Vesencumab (MNRP-1685A) is IG1 antibody against neuropilin-1 (NRP-1). Vesencumab binds to NRP-1 and prevents the subsequent coupling of NRP-1 to VEGFR-2. Vesencumab has anti-angiogenic and anti-neoplastic activities. Vesencumab can be used in the research of metastatic solid tumors, including ovarian cancer .
|
-
- HY-12168
-
|
BAY 12-9566
|
MMP
|
Cancer
|
|
Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
|
-
- HY-155653
-
|
|
BCRP
|
Cancer
|
|
ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) .
|
-
- HY-19577
-
|
PTT119
|
DNA Alkylator/Crosslinker
|
Infection
Cancer
|
|
Ambamustine (PTT119) is a new bifunctional alkylating agent and induces DNA damage by alkylating mechanisms. Ambamustine interferes with late steps in murine mammary tumor virus (MuMTV) processing and maturation and reduces production of the B-type retrovirus MuMTV. Ambamustine possesses cytolytic and antiviral activities .
|
-
- HY-136174
-
|
|
PARP
|
Cancer
|
|
RBN-2397 is a potent, accross species and orally active NAD + competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors .
|
-
- HY-P10762
-
|
LDC 10B
|
Peptide-Drug Conjugates (PDCs)
Folate Receptor (FR)
TRP Channel
|
Cancer
|
|
CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. CBP-1008 binds to FRα with high affinity and TRPV6 with low affinity. CBP-1008 has antitumor activity, and can be used in advanced solid tumor research (eg: colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma and follicular dendritic cell sarcoma) .
|
-
- HY-116191
-
|
|
PI3K
mTOR
|
Cancer
|
|
WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
|
-
- HY-103702
-
|
|
Proton Pump
|
Cancer
|
|
TIP48/49-IN-1 (Compound B) is an orally active and specific inhibitor of RUVBL1/2 ATPase, with an IC50 of 59 nM for purified RUVBL1/2. TIP48/49-IN-1 affects DNA replication process, and leads to S-phase arrest. TIP48/49-IN-1 induces apoptosis. TIP48/49-IN-1 inhibits tumor growth and radiosensitizes non-small cell lung cancer cells (NSCLC) .
|
-
- HY-151153
-
|
|
HDAC
Microtubule/Tubulin
Caspase
Apoptosis
|
Cancer
|
|
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
|
-
- HY-14389
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM . LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-114414
-
|
|
HDAC
mTOR
Apoptosis
|
Cancer
|
|
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
|
-
- HY-124689
-
|
|
Arp2/3 Complex
|
Metabolic Disease
Cancer
|
|
TR-100 is a small molecule inhibitor of tumor-associated troponin (Tpm). TR-100 affects the interaction of Tpm3.1 with actin filaments by binding to the C-terminal of Tpm3.1, thereby affecting the stability and function of the actin filaments. This mechanism of action allows TR-100 to specifically affect actin filaments in cancer cells without compromising heart muscle function. TR-100 can be used to study the role of Tpm3.1 in cancer cell proliferation and survival and the effects of Tpm3.1 on insulin-stimulated glucose uptake and insulin secretion .
|
-
- HY-144657A
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .
|
-
- HY-50896
-
|
CP-358774; NSC 718781; OSI-774
|
EGFR
Autophagy
|
Cancer
|
|
Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W001171
-
-
- HY-133016
-
|
|
MetAP
|
Cardiovascular Disease
Cancer
|
|
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
|
-
- HY-151277
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK5-IN-29 is an selective activin receptor-like kinase (ALK) inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC50 value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
|
-
- HY-139874
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3 + T lymphocytes into the Pan02 tumor tissues .
|
-
- HY-144423
-
|
|
Trk Receptor
|
Cancer
|
|
Trk-IN-10 (Compound 14j) is a potent inhibitor of TRK (IC50 = 0.86, 6.92 nM, against TrkA, TrkA G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) has a higher selectivity of Trk inhibition, which may be of great significance for reducing toxicity .
|
-
- HY-P99829
-
|
PF-06647020; ABBV-647; h6M24-vc0101
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cofetuzumab pelidotin (PF-06647020) is a PTK7-targeting ADC comprising a humanized anti-PTK7 mAb (hu6M024, IgG1) joined to an auristatin microtubule inhibitor payload, auristatin-0101 (Aur0101; HY-12522), by a cleavable valine-citrulline (vc)-based linker. Cofetuzumab pelidotin has a DAR of 4. Cofetuzumab pelidotin binds to cell-surface PTK7 with an EC50 of 1153 pM by flow cytometry. Cofetuzumab pelidotin has the potential for solid tumors research .
|
-
- HY-N9174
-
|
|
Others
|
Cancer
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
- HY-50683
-
|
|
c-Met/HGFR
|
Metabolic Disease
Cancer
|
|
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases . JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach .
|
-
- HY-103397R
-
|
|
Antibiotic
DNA Methyltransferase
Parasite
|
Infection
Cancer
|
|
Nanaomycin A (Standard) is the analytical standard of Nanaomycin A. This product is intended for research and analytical applications. Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells[1]. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM[2].
|
-
- HY-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-150190
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 methyltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo .
|
-
- HY-147165
-
|
|
YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-12168B
-
|
(Rac)-BAY 12-9566
|
MMP
|
Cancer
|
|
(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
|
-
- HY-P99172
-
|
|
CD47
Interleukin Related
|
Cancer
|
|
CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors .
|
-
- HY-147915
-
|
|
Carboxylesterase (CES)
Reactive Oxygen Species
|
Cancer
|
|
Benz-AP is a potent photosensitizer. Benz-AP produces singlet oxygen, with a negative correlation with hCES2 (Human carboxylesterase 2) activity. Benz-AP displays a higher photocytotoxicity potency in cancer cells under low hCES2 environments. Upon TPE (Two-photon excitation), Benz-AP produces ROS and kills cancer cells and tumor spheroids .
|
-
- HY-119616
-
|
|
Apoptosis
|
Cancer
|
|
Phenamet is an anti-tumor agent that can inhibit tumor growth and slow the progression of cancer. Phenamet prevents the reproduction of tumor cells by interfering with the growth and division of cancer cells. In addition, Phenamet can induce apoptosis in cancer cells, thereby eliminating tumor cells.
|
-
- HY-149521
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
|
-
- HY-100388R
-
|
|
SHP2
Phosphatase
|
Cancer
|
|
SHP099 (Standard) is the analytical standard of SHP099. This product is intended for research and analytical applications. SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth[1][2].
|
-
- HY-164490
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
|
-
- HY-A0061R
-
|
|
Thymidylate Synthase
HSV
Nucleoside Antimetabolite/Analog
Orthopoxvirus
DNA/RNA Synthesis
Apoptosis
Autophagy
|
Cancer
|
|
Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .
|
-
- HY-153856
-
|
|
EGFR
|
Cancer
|
|
TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations .
|
-
- HY-153856A
-
|
|
EGFR
|
Cancer
|
|
TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations .
|
-
- HY-134813
-
|
|
Ras
|
Cancer
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-12757
-
|
|
BCRP
|
Cancer
|
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
|
-
- HY-164492
-
|
|
Raf
|
Cancer
|
|
LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation .
|
-
- HY-151595
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome) .
|
-
- HY-121524
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
DJ101 is a potent and metabolically stable tubulin inhibitor. DJ101 targets the colchicine binding site and overcomes taxane resistance. DJ101 also inhibits melanoma tumor growth and lung metastasis. DJ101 can be used for prostate cancer research .
|
-
- HY-143321
-
|
|
STING
|
Cancer
|
|
STING agonist-13 is a stimulator of interferon genes (STING) agonist, for cancer immunity via STING-mediated immune activation. STING agonist-13 can stimulate STING downstream signaling and promoting type I interferon immune responses. STING agonist-13 significantly decreases tumor volume and shows immunological memory-derived cancer inhibition .
|
-
- HY-10252
-
|
ADW742; GSK 552602A; ADW
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells .
|
-
- HY-128350A
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
|
-
- HY-10824A
-
|
PT523 monoammonium
|
Dihydrofolate reductase (DHFR)
Antifolate
|
Cancer
|
|
Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic antifolate. Talotrexin monoammonium is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth .
|
-
- HY-144707
-
|
|
Apoptosis
|
Cancer
|
|
AK-778-XXMU is a potent inhibitor of DNA Binding 2 (ID2) antagonist with a KD of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and more importantly, slow down the tumor growth .
|
-
- HY-103190
-
|
|
Adenosine Receptor
|
Neurological Disease
Cancer
|
|
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system . MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo .
|
-
- HY-136244
-
|
|
TGF-β Receptor
|
Cancer
|
|
PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer .
|
-
- HY-159175
-
|
|
PROTACs
Deubiquitinase
Apoptosis
MDM-2/p53
|
Cancer
|
|
XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)) .
|
-
- HY-P99742
-
|
ADC-1013; JNJ-64457107
|
TNF Receptor
|
Cancer
|
|
Mitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment .
|
-
- HY-120241
-
|
K 251-1
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Reticulol (K 251-1) is an inhibitor of cyclic adenosine 3', 5'-monophosphate phosphodiesterase. Reticulol shows antitumor activity independent with cell cycle arrest or apoptosis. Reticulol inhibits cell growth of murine melanoma cells and human lung tumor cells. Reticulol protects its lung metastasis via the bloodstream by inhibiting the growth of B16F10 melanoma .
|
-
- HY-151873
-
|
|
RIP kinase
|
Inflammation/Immunology
Cancer
|
|
SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD) .
|
-
- HY-170842
-
|
|
Apoptosis
|
Cancer
|
|
TDK-HCPT is a small-molecule conjugate that links glutathione-sensitive thiamine disulfide to the chemotherapy drug 10-Hydroxycamptothecin (HY-N0095) via a thioketal bond. TDK-HCPT can target tumor cells and prolong the retention of chemotherapy agents within tumor cells. TDK-HCPT can inhibit tumor growth, induce apoptosis of tumor cells, and has anti-tumor activity .
|
-
- HY-50896R
-
|
|
EGFR
Autophagy
|
Cancer
|
|
Erlotinib (Standard) is the analytical standard of Erlotinib. This product is intended for research and analytical applications. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-101849
-
|
|
GLUT
TNF Receptor
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
|
-
- HY-D0085
-
|
|
Fluorescent Dye
|
Others
|
|
DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrial membrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumor cells .
|
-
- HY-162472
-
|
|
ATM/ATR
DNA-PK
|
Cancer
|
|
XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
|
-
- HY-145428
-
|
|
Notch
γ-secretase
|
Cancer
|
|
BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression .
|
-
- HY-110243
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
|
-
- HY-163642
-
|
|
Others
|
Cancer
|
|
TNF-α agonistic 1 (compound 22a) can repolarize tumor-associated macrophages (TAMs) in the tumor microenvironment (TME) from the M2 phenotype to the M1 anti-tumor phenotype .
|
-
- HY-128350
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
|
-
- HY-U00002A
-
|
|
VEGFR
|
Cancer
|
|
ZD-4190 hydrochloride is a potent VEGFR inhibitor with anti-tumor activity. ZD-4190 hydrochloride can delay the growth of MDA-MB-435 tumors by inhibiting tumor cell proliferation and angiogenesis .
|
-
- HY-146215
-
-
- HY-124179
-
|
|
NF-κB
|
Cancer
|
|
IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 μM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD) .
|
-
- HY-126287
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
|
-
- HY-169078
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
|
-
- HY-P10105
-
|
|
Akt
Apoptosis
|
Cancer
|
|
TCL1(10-24) is a encompassing the betaA strand of human TCL1. TCL1(10-24) is a Akt inhibitor. TCL1(10-24) interacts with the Akt PH domain prevented phosphoinositide binding and hence inhibits membrane translocation and activation of Akt. TCL1(10-24) inhibits cellular proliferation and anti-apoptosis. TCL1(10-24) has tumor growth in vivo .
|
-
- HY-124675
-
MYCMI-6
1 Publications Verification
NSC354961
|
c-Myc
Apoptosis
|
Cancer
|
|
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis .
|
-
- HY-120187
-
|
|
Others
|
Others
|
|
DDCPPB-Glu (compound 3a) is a compound with anti-tumor activity, which has the activity of inhibiting tumor cell growth and prolonging survival. DDCPPB-Glu has growth inhibition effect on various tumor cell lines, can increase the survival time of leukemia mice, and has inhibitory effect on tumors such as colon cancer and lung cancer.
|
-
- HY-122094
-
-
- HY-120793
-
|
TRB-N0224
|
Ras
Apoptosis
MMP
|
Inflammation/Immunology
Cancer
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
|
-
- HY-158138
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
|
-
- HY-108963
-
|
|
PKC
Leukotriene Receptor
|
Cancer
|
|
LY 170198 is a protein kinase C inhibitor and a LTD4 antagonist. LY 170198 is promising for research of tumor promotion, oncogene activation, protein phosphorylation, feedback mechanisms in signal transduction and cellular responses to growth factors .
|
-
- HY-155246
-
|
|
Apoptosis
PARP
|
Cancer
|
|
PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .
|
-
- HY-150298
-
|
CPI-818
|
Itk
|
Inflammation/Immunology
Cancer
|
|
Soquelitinib (CPI-818) is an orally active and highly selective covalent interleukin-2-inducible kinase (ITK) inhibitor. Soquelitinib is active in six different models of T cell-mediated inflammatory and immune disease, including acute and chronic asthma, pulmonary fibrosis, systemic sclerosis (scleroderma), psoriasis, and acute graft versus host disease with Th2 cytokine product inhibition. Soquelitinib increases tumor infiltration of normal CD8 + cells that possess enhanced T effector function .
|
-
- HY-145769
-
|
|
PD-1/PD-L1
|
Cancer
|
|
N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method .
|
-
- HY-119618
-
|
|
Endogenous Metabolite
|
Cancer
|
|
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
|
-
- HY-122724
-
|
|
Apoptosis
|
Cancer
|
|
IQDMA is an anti-tumor compound. IQDMA can induce apoptosis in tumor cells, such as K562 cells .
|
-
- HY-B0523B
-
|
|
Phosphodiesterase (PDE)
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Anagrelide hydrochloride monohydrate is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride monohydrate, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride monohydrate inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride monohydrate decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride monohydrate is a platelet-lowering agent and plays in the antithrombopoietic action .
|
-
- HY-W591818
-
|
|
Drug Derivative
|
Cancer
|
|
Sunitinib carboxylic acid is a carboxylic acid metabolite of Sunitinib (HY-10255A). Sunitinib is a multi-target tyrosine kinase inhibitor, mainly used to inhibit malignant tumors such as gastrointestinal stromal tumors, renal cell carcinoma, and pancreatic neuroendocrine tumors .
|
-
- HY-159190
-
|
|
MAPKAPK2 (MK2)
|
Cancer
|
|
HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
|
-
- HY-40136
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
cis-4-Hydroxy-L-proline is an orally active proline analog and collagen production inhibitor. cis-4-Hydroxy-L-proline inhibits cell growth by preventing the deposition of triple helical collagen on the cell layer. cis-4-Hydroxy-L-proline inhibits N-nitrosomethylurea-induced breast tumor growth. cis-4-Hydroxy-L-proline improves lung compliance and reduces prostate weight. cis-4-Hydroxy-L-proline can be used in the study of hypoxic pulmonary hypertension .
|
-
- HY-12678S1
-
|
NMS-E628-d8; RXDX-101-d8
|
Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
|
Cancer
|
|
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
|
-
- HY-P3448
-
|
CEND-1; iRGD; LSTA1
|
Integrin
Complement System
|
Cancer
|
|
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors .
|
-
- HY-163146
-
|
|
Fluorescent Dye
|
Cancer
|
|
TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
|
-
- HY-105129AS
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Pimonidazole-d10 is the deuterium labeled Pimonidazole. Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor[1]. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia [2].
|
-
- HY-B0523A
-
|
BL4162A
|
Phosphodiesterase (PDE)
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action .
|
-
- HY-A0096
-
-
- HY-171331
-
|
|
PD-1/PD-L1
Integrin
|
Cancer
|
|
AB-3PRGD2 is a radiotherapeutic agent targeting integrin αvβ3. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8 + T cells .
|
-
- HY-P10553
-
|
|
Apoptosis
|
Cancer
|
|
ARF(26–44), cell-permeable is a cell-penetrating peptide derived from a specific amino acid sequence of the p14ARF tumor suppressor protein. As a functional inhibitor of FoxM1, ARF(26–44) cell-permeable shows significant anti-tumor activity in the treatment of mouse hepatocellular carcinoma (HCC), significantly increasing tumor cell apoptosis and reducing tumor cell proliferation and angiogenesis. ARF(26–44), cell-permeable can be used in research on tumor therapy .
|
-
- HY-N0438
-
|
|
Apoptosis
|
Cancer
|
|
Pimpinellin is a constituent of Cyrtomium fortumei (J.). Pimpinellin inhibits the growth of tumor cells via the induction of tumor cell apoptosis .
|
-
- HY-113843
-
|
|
MDM-2/p53
|
Cancer
|
|
RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
|
-
- HY-156965
-
|
|
Fluorescent Dye
|
Metabolic Disease
Cancer
|
|
BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
|
-
- HY-18343
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
|
-
- HY-173630
-
|
|
Molecular Glues
IKZF Family
|
Cancer
|
|
BMS-986449 is a CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors .
|
-
- HY-148494
-
|
FLX475
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Tivumecirnon (FLX475) is an orally active, selective CCR4 antagonist. Tivumecirnon blocks the binding of CCR4 to its ligands, CCL17 and CCL22, thereby reducing Treg infiltration into the tumor microenvironment. Tivumecirnon has antitumor activity .
|
-
- HY-P0122
-
|
c(CRGDKGPDC)
|
Integrin
|
Cancer
|
|
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
|
-
- HY-105129R
-
|
|
Others
|
Cancer
|
|
Pimonidazole (hydrochloride) (Standard) is the analytical standard of Pimonidazole (hydrochloride). This product is intended for research and analytical applications. Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor[1]. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia [2].
|
-
- HY-105129AR
-
|
|
Others
|
Cancer
|
|
Pimonidazole (Standard) is the analytical standard of Pimonidazole. This product is intended for research and analytical applications. Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor[1]. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia [2].
|
-
- HY-142533
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
HL-PEG2k is a second near-infrared Ru(II) polypyridyl complex. HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors .
|
-
- HY-134813A
-
|
|
Ras
|
Cancer
|
|
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-N6843
-
-
- HY-D2203
-
|
|
Fluorescent Dye
|
Cancer
|
|
BODIPY BDP4 has ssuperb sonosensitivity and high SDT efficiency against cancer cells and tumors in tumor-bearing mice .
|
-
- HY-142950
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1) .
|
-
- HY-B2097
-
|
YM 175; Bisphonal
|
Farnesyl Transferase
|
Metabolic Disease
|
|
Incadronate disodium (YM 175) is a bisphosphonate with strong inhibitory activity on bone resorption. Incadronate disodium indirectly stimulates renal 25-hydroxyvitamin D-1-hydroxylase by increasing circulating parathyroid hormone. Incadronate disodium, a cholesterol-lowering agent, is a potent inhibitor of rat liver microsomal squalene synthase (Ki=57 nM). Incadronate disodium inhibits sterol biosynthesis in mouse macrophage J774 cells (IC50=64 μM). Incadronate disodium has the potential for malignant tumors research .
|
-
- HY-142949
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4) .
|
-
- HY-161694
-
|
|
DNA Methyltransferase
|
Cancer
|
|
DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
|
-
- HY-101849R
-
|
|
GLUT
TNF Receptor
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Fasentin (Standard) is the analytical standard of Fasentin. This product is intended for research and analytical applications. Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity[1][2][3].
|
-
- HY-159480
-
|
|
Src
ATM/ATR
Apoptosis
mTOR
AMPK
|
Cancer
|
|
AD1058 is an orally active, selective, and blood-brain barrier permeable inhibitor of ATR. AD1058 exhibits in vivo anticancer activity, inhibiting cell proliferation, disrupting the cell cycle, and inducing Apoptosis. AD1058 can be utilized in research on brain and central nervous system metastases stemming from advanced solid tumors .
|
-
- HY-W286059
-
|
|
Biochemical Assay Reagents
|
|
|
2-Aminohexadecanoic acid is a bioactive compound that has the activity of inhibiting tumor growth. 2-Aminohexadecanoic acid has been shown in studies to act on basic proteins and interfere with the proliferation of tumor cells. The uses of 2-Aminohexadecanoic acid include as a potential anti-tumor inhibitor.
|
-
- HY-135748
-
|
Poly(I:C) sodium
|
Toll-like Receptor (TLR)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis .
|
-
- HY-134958
-
|
Poly(I:C) potassium
|
Toll-like Receptor (TLR)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis .
|
-
- HY-75706
-
|
|
PARP
Ligands for Target Protein for PROTAC
|
Cancer
|
|
N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib (HY-10162) containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a PARP inhibitor used for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4 (HY-141481) . N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled with F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor .
|
-
- HY-108417
-
|
|
STAT
JAK
Bcr-Abl
|
Cancer
|
|
Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
|
-
- HY-145102
-
|
|
HSP
Apoptosis
|
Cancer
|
|
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
|
-
- HY-116624
-
MAZ51
4 Publications Verification
|
VEGFR
Apoptosis
|
Cancer
|
|
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity .
|
-
- HY-P99115
-
|
ASC 22; KN 035
|
PD-1/PD-L1
|
Cancer
|
|
Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC50 value of 5.25?nM. Envafolimab has the potential for the research of solid tumors .
|
-
- HY-P99024
-
|
RO7082859
|
CD20
CD3
|
Inflammation/Immunology
Cancer
|
|
Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on T cells. Glofitamab leads to T-cell activation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell non-Hodgkin lymphoma (B-NHL) .
|
-
- HY-17419S1
-
-
- HY-161248
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
E7130 is a microtubule inhibitor, which ameliorates the tumor microenvironment through suppression of cancer-associated fibroblasts (CAF) and promotion of tumor vasculature remodeling .
|
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-105129
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor . Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
|
-
- HY-105129A
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor . Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
|
-
- HY-P99547
-
|
(vic)-Trastuzumab duocarmazine
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) is a HER2-targeting ADC that is recognized and cleaved by histone B in tumor cells and selectively targets tumor cells. Trastuzumab duocarmazine has anti-tumor activity and can be used in cancer research related to uterine and ovarian sarcomas .
|
-
- HY-11080A
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo .
|
-
- HY-11080
-
PKI-179
1 Publications Verification
|
PI3K
mTOR
|
Cancer
|
|
PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo .
|
-
- HY-W272058
-
|
|
Others
|
Cancer
|
|
Isometronidazole is a hypoxic cell sensitizer. Isometronidazole (750 mg/kg) shows an efficacy as a hypoxic cell sensitizer in severely hypoxic FaDu tumors but not in less hypoxic GL tumors.
|
-
- HY-143407
-
|
|
FAK
|
Cancer
|
|
FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer .
|
-
- HY-160506
-
|
|
PROTACs
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .
|
-
- HY-B0523AR
-
|
|
Phosphodiesterase (PDE)
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Anagrelide (hydrochloride) (Standard) is the analytical standard of Anagrelide (hydrochloride). This product is intended for research and analytical applications. Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action .
|
-
- HY-13582A
-
|
|
Fungal
Parasite
|
Infection
Cancer
|
|
Carbendazim hydrochloride is a potent and orally active broad-spectrum?benzimidazole fungicide and can be acts as a pesticide for fungal diseases research, such as Seproria,?Fusarium?and?Sclerotina . Carbendazim hydrochloride is a benzimidazole (HY-Y1825) derivative with antitumor activity and used for cancer research, especially advanced solid tumors and lymphoma .
|
-
- HY-13582
-
|
|
Fungal
Parasite
|
Infection
Cancer
|
|
Carbendazim is a potent and orally active broad-spectrum benzimidazole fungicide and can be acts as a pesticide for fungal diseases research, such as Seproria, Fusarium and Sclerotina . Carbendazim is a benzimidazole (HY-Y1825) derivative with antitumor activity and used for cancer research, especially advanced solid tumors and lymphoma .
|
-
- HY-12564
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells .
|
-
- HY-169422
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 16 (Example 83) is an orally available WRN inhibitor. WRN inhibitor 16 did not induce tumor regression in the SW48 xenograft mouse tumor model.
|
-
- HY-N11638
-
|
|
Apoptosis
|
Cancer
|
|
Ganoderic acid R is a potent anticancer agent. Ganoderic acid R inhibits the growth by inducing apoptosis on tumor cell line. Ganoderic acid R possesses significant cytotoxicity on a multidrug resistance (MDR) tumor cell line (KB-A-1/Dox) and a sensitive tumor cell line (KB-A-1) .
|
-
- HY-155180
-
|
|
PI3K
|
Cancer
|
|
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
|
-
- HY-106033
-
|
DOTATOC; SDZ-SMT 487; SMT 487
|
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
Edotreotide is a ligand that selectively targets SSTR2 and can competitively bind to the receptor. Edotreotide mediates the targeted delivery, while modificated with radionuclides (such as 90Y, 177Lu, and 68Ga) to SSTR-positive tumors and induces tumor cell apoptosis by releasing β rays. Edotreotide has strong tumor targeting and precise killing activity. Edotreotide is used in the synthesis of radionuclide-drug conjugates (RDCs) and is widely used in the field of neuroendocrine tumors (such as metastatic carcinoids, lung and thymus NETs) .
|
-
- HY-16208
-
-
- HY-P991090
-
|
ABL105
|
EGFR
|
Cancer
|
|
YH32367 (ABL105) is a bispecific HER2 and 4-1BB antibody. YH32367 induces IFN-γ secretion and thereby eliciting tumor cell death in co-culture condition with hPBMC and HER2-expressing tumor cells. YH32367 has significant anti-tumor effects .
|
-
- HY-156110
-
|
|
Insulin Receptor
|
Cancer
|
|
IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
|
-
- HY-153341
-
|
|
PROTACs
Raf
|
Cancer
|
|
CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ) degrader of BRAF V600E with a DC50 of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. CFT1946 can be used in tumor research .
|
-
- HY-116604
-
|
PD 139530
|
PI3K
Akt
|
Cancer
|
|
RLX (PD 139530) is a PI3K/Akt/FoxO3a signaling inhibitor, possessing significant therapeutic potential in experimental colon cancer. RLX can effectively modulate the tumor microenvironment, enhancing the efficacy of cancer immunotherapy. RLX demonstrates the ability to improve the retention time of therapeutic agents within the tumor microenvironment by utilizing advanced nanoparticle delivery systems. RLX can be integrated with various treatment modalities, such as chemotherapy and radiotherapy, to enhance overall tumor therapy effectiveness. RLX highlights the necessity for further research into the tumor microenvironment’s dynamics to develop more tailored treatment approaches for diverse tumor types.
|
-
- HY-105098B
-
|
(±)-BMS-180194; SQ 33054
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
(±)-Lobucavir ((±)-BMS-180194) is a nucleoside analog with carcinogenic activity. In mice, chronic administration of (±)-Lobucavir resulted in tumor formation with a tumor spectrum similar to that observed after chronic administration of zidovudine or ganciclovir.
|
-
- HY-126730
-
|
|
Phosphatase
|
Cancer
|
|
Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts .
|
-
- HY-50914
-
|
|
CDK
|
Cancer
|
|
AZD5597 is an inhibitor of CDK with IC50 values of both 2 nM for CDK1 and CDK2. AZD5597 can inhibit the proliferation of tumor cells and has anti-tumor activity .
|
-
- HY-126954
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
13-Deoxycarminomycin is an antibiotic with antibacterial activity. 13-Deoxycarminomycin also exhibits cytotoxicity against tumor cells such as HeLa and P388, and can play an anti-tumor role .
|
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
- HY-143881
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-126617
-
|
NSC 258308
|
Others
|
Cancer
|
|
Duclauxin decreases proliferation of tumor cells in vitro and increases the lifespan of mice innoculated with Ehrlich ascitic tumor cells. Duclauxin (10-30 μg/mL) inhibits mitochondrial respiration of P-388 tumor cells and nucleic acid synthesis in cell culture of Ehrlich cancer, the lymphadenomas NK/LI and L 5178, and sarcoma 37. Duclauxin also inhibits growth of wheat coleoptile.
|
-
- HY-118184
-
|
|
PGE synthase
|
Cancer
|
|
AF3485 is a human mPGES-1 inhibitor that exhibits antitumor activity in vitro and in vivo. AF3485 inhibits tumor-associated angiogenesis by reducing PGE2 production, inhibiting EGFR signaling, and decreasing VEGF and FGF-2 expression. AF3485 reduced tumor growth in mice bearing human A431 xenograft tumors by subchronic administration.
|
-
- HY-120482
-
|
|
Microtubule/Tubulin
|
Others
|
|
CHM-1-P-Na is a sodium monophosphate salt of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one, which can be converted into CHM-1, a compound with a unique anti-tumor mechanism, in vitro and in vivo, and has excellent anti-tumor activity in tumor models and clear pharmacological effects on related enzymes.
|
-
- HY-N15054
-
|
|
Drug Derivative
|
Cancer
|
|
17-O-Demethylgeldanamycin is a secondary metabolite that can be isolated from Streptomyces. 17-O-Demethylgeldanamycin exhibits cytotoxicity against a variety of tumor cells and has anti-tumor activity .
|
-
- HY-121087
-
BCI-215
3 Publications Verification
|
Phosphatase
|
Cancer
|
|
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells .
|
-
- HY-118982
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
CT-2584 is a chemotherapeutic compound that reduces the expression of NKEF-B in several tumor cell types and kills tumor cells by inducing the production of ROS in mitochondria, commonly used in cancer research .
|
-
- HY-A0096R
-
|
|
Prostaglandin Receptor
Endogenous Metabolite
|
Endocrinology
Cancer
|
|
Iloprost (Standard) is the analytical standard of Iloprost. This product is intended for research and analytical applications. Iloprost (ZK 36374; Ciloprost) is a prostacyclin (PGI2) analogue, involves in embryo development and inflammation improvement, and inhibits tumor metastasis. Iloprost can be used for peripheral vascular research .
|
-
- HY-N8543
-
-
- HY-118899
-
|
|
Endogenous Metabolite
|
Cancer
|
|
XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
|
-
- HY-13646C
-
|
HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride
|
P-glycoprotein
|
Cancer
|
|
Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models .
|
-
- HY-155524
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 134 (compound 6a) is a environment-sensitive fluorescent probe and an apoptosis inducer, making a distinction between the tumor and normal tissues. Anticancer agent 134 localizes to the nuclear bodies in tumor slices .
|
-
- HY-P3099
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Uroguanylin (human) is a natural ligand for the Guanylyl Cyclase (GCC) receptor expressed in metastatic colorectal cancer tumors. Uroguanylin (human) has anti-tumor actions in an animal model for human colon cancer .
|
-
- HY-115760
-
|
|
Phosphatase
|
Neurological Disease
Cancer
|
|
Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation .
|
-
- HY-157231A
-
|
|
PERK
|
Cancer
|
|
HC-5404-Fu is a PERK inhibitor with an antitumor activity. HC-5404-Fu inhibits endoplasmic reticulum stress response signalling. HC-5404-Fu sensitizes renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). HC-5404-Fu is promising for research of renal cell carcinoma, gastric cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors .
|
-
- HY-13661
-
|
UCN-01; KRX-0601
|
Akt
PKC
CDK
Apoptosis
|
Cancer
|
|
7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinase AKT and calcium-dependent protein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependent kinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis .
|
-
- HY-128973
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
Pyropheophorbide-a (Ppa) is a photosensitizer used in photodynamic therapy (PDT) for tumors. Pyropheophorbide-a exhibits phototoxic effects on tumor cells, such as cervical cancer cells, and also has anti-lipogenesis activity. Pyropheophorbide-a shows potential for research in the fields of cancer and age-related macular degeneration (AMD). Pyropheophorbide-a derivatives also demonstrate inhibitory activity against tumor cells .
|
-
- HY-165740
-
|
Disialoganglioside GD2
|
Biochemical Assay Reagents
|
Cancer
|
|
Ganglioside GD2 (Disialoganglioside GD2), a member of the ganglioside family, is a tumor-associated antigen that is highly expressed in almost all neuroblastomas, as well as in most melanomas and retinoblastomas. Ganglioside GD2 contributes to tumor development by enhancing cell proliferation, motility, migration, adhesion, and invasion. Anti-Ganglioside GD2 strategies hold promise for research in the field of anti-tumor therapy .
|
-
- HY-P1828
-
|
|
EGFR
|
Cancer
|
|
EGFRvIII peptide (PEPvIII) is a tumor-specific mutation that is widely expressed in glioblastoma multiforme (GBM) and other neoplasms and its expression enhances tumorigenicity. EGFRvIII peptide represents a truly tumor-specific target for antitumor immunotherapy .
|
-
- HY-12628
-
GNE-618
1 Publications Verification
|
NAMPT
|
Cancer
|
|
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity .
|
-
- HY-144188
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
|
-
- HY-144187
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
|
-
- HY-P3099A
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Uroguanylin (human) (TFA) is a natural ligand for the Guanylyl Cyclase (GCC) receptor expressed in metastatic colorectal cancer tumors. Uroguanylin (human) (TFA) has anti-tumor actions in an animal model for human colon cancer .
|
-
- HY-P5520
-
|
|
Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
-
- HY-P10420
-
|
|
CD47
Interleukin Related
|
Cancer
|
|
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
|
-
- HY-N8430
-
|
|
Others
|
Cancer
|
|
Poricoic acid AM is a triterpenoid with ant-tumor activities .
|
-
- HY-146307
-
|
|
TrxR
|
Cancer
|
|
TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
|
-
- HY-W848341
-
|
NSC 338947; CIEtSoSo
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Clomesone (NSC 338947) is a compound with antitumor activity. Clomesone induces the formation of cross-links between DNA strands in cell lines. Clomesone is inactive against most human colorectal cancer solid tumor cell lines in vitro, has no significant activity against mouse tumors in vivo, and is accompanied by bone marrow suppression. Its pharmacokinetic behavior indicates that it cannot reach effective concentrations at the tumor site.
|
-
- HY-172495
-
|
|
Liposome
Integrin
|
Cancer
|
|
DSPE-PEG3000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG3000-iRGD can be used for drug delivery .
|
-
- HY-172493
-
|
|
Liposome
Integrin
|
Cancer
|
|
DSPE-PEG1000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG1000-iRGD can be used for drug delivery .
|
-
- HY-134463
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
- HY-172494
-
|
|
Liposome
Integrin
|
Cancer
|
|
DSPE-PEG2000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG2000-iRGD can be used for drug delivery .
|
-
- HY-114440
-
|
GR-MD-02
|
Galectin
Apoptosis
|
Cancer
|
|
Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM .
|
-
- HY-159641
-
|
BAY-3605349
|
Keap1-Nrf2
|
Cancer
|
|
VVD-130037 (BAY-3605349) is an orally active covalent activator of KEAP 1 (Kelch-like ECH-associated protein 1) with anti-tumor activity. VVD-130037 degrades NRF2 (nuclear factor-erythroid 2 p45-related factor 2), resulting in significant inhibition of tumor growth in advanced solid tumors .
|
-
- HY-168895
-
|
|
AP-1
ERK
Apoptosis
|
Cancer
|
|
c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC50: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth .
|
-
- HY-130612
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
|
-
- HY-149632
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
|
-
- HY-N11669
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Demycarosyl-3D-β-D-digitoxosylmithramycin SK is a Mithramycin analog with good anti-tumor activity, which can prevent the proliferation and growth of tumor cells by binding and inhibiting DNA-binding proteins .
|
-
- HY-106052
-
|
ICIG 1105; NSC 279194; RFCNU
|
DNA/RNA Synthesis
|
Cancer
|
|
Bofumustine (ICIG 1105) is a nitrosourea compound with antitumor activity. Bofumustine can interfere with the replication and division of tumor cell DNA through alkylation, leading to the death of tumor cells. Bofumustine can be used in the field of cancer research .
|
-
- HY-154944
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1) with an IC50 of 14.8 μM. JG-2016 can inhibit the growth of multiple tumor cells and has anti-tumor activity .
|
-
- HY-116399
-
|
|
MMP
|
Cancer
|
|
MMP-2/MMP-9-IN-1 is a highly selective, orally active and potent type IV collagenase (MMP-9 and MMP-2) inhibitor with IC50s of 0.24 and 0.31 μM for MMP-9 and MMP-2, respectively. MMP-2/MMP-9-IN-1 is orally active in animal models of tumor growth and metastasis. MMP-2/MMP-9-IN-1 can be used for the research of cancer .
|
-
- HY-144099
-
|
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity .
|
-
- HY-P4322
-
|
|
ERK
Akt
|
Neurological Disease
Cancer
|
|
H-Ile-Lys-Val-Ala-Val-OH is one of the most potent active sites of laminin-1. H-Ile-Lys-Val-Ala-Val-OH promotes cell adhesion, neurite outgrowth, and tumor growth. H-Ile-Lys-Val-Ala-Val-OH stimulates BMMSC population growth and proliferation by activating MAPK/ERK1/2 and PI3K/Akt signalling pathways .
|
-
- HY-16938
-
|
5'-(Methylthio)-5'-deoxyadenosine; 5'-Deoxy-5'-(methylthio)adenosine; 5'-S-Methyl-5'-thioadenosine
|
Endogenous Metabolite
Apoptosis
Parasite
|
Metabolic Disease
Cancer
|
|
5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
|
-
- HY-P10550
-
|
|
VEGFR
|
Cancer
|
|
VGB4 is a VEGF-A and VEGF-B antagonist peptide that duplicates two binding domains of VEGF-B (loop 1 and loop3) and are linked together by the receptor-binding domain of VEGF-A (loop3). VGB4 has significant anti-angiogenic and anti-tumor activities and can regulate tumor growth and metastasis through multiple mechanisms. VGB4 could be used in anti-tumor research .
|
-
- HY-114169
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .
|
-
- HY-164517
-
|
|
Trk Receptor
|
Cancer
|
|
ONO-7579 is an orally active TRKA inhibitor that suppresses tumor growth by inhibiting the phosphorylation of TRKA. In colorectal cancer cells KM12, its EC50 is 17.6 ng/g (meaning that when each gram of tumor tissue contains 17.6 ng of ONO-7579, the activity of phosphorylated TRKA in the tumor is inhibited by 50%). ONO-7579 can be used in cancer research .
|
-
- HY-156633
-
|
PC14586
|
MDM-2/p53
|
Cancer
|
|
Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation .
|
-
- HY-133935
-
|
|
Others
|
Others
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Benaxibine is an alkaloid belonging to the quinolone family of compounds. Benaxibine has a variety of biological activities, including anti-inflammatory, antioxidant, anti-tumor and immune-enhancing effects. Benaxibine can be used for screening and research of diseases such as inflammation and tumor .
|
-
- HY-P5020
-
|
|
Bacterial
|
Infection
Cancer
|
|
Crotalicidin is an antimicrobial peptide and anti-tumor peptide that can effectively inhibit the activity of Gram-negative bacteria and tumor cells. Crotalicidin can be obtained from rattlesnake venom. Crotalicidin can be used in the study of microbial infections and cancer .
|
-
- HY-P1828A
-
|
|
EGFR
|
Cancer
|
|
EGFRvIII peptide (PEPvIII) TFA is a tumor-specific mutation that is widely expressed in glioblastoma multiforme (GBM) and other neoplasms and its expression enhances tumorigenicity. EGFRvIII peptide TFA represents a truly tumor-specific target for antitumor immunotherapy .
|
-
- HY-14815
-
|
Combretastatin A4 phosphate
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Fosbretabulin (Combretastatin A4 phosphate) is a vascular disruptor with antitumor activity against atypical thyroid carcinoma (ATC) cell lines and xenografts. Fosbretabulin inhibits tumor growth by inhibiting microtubule polymerization, inducing apoptosis, and suppressing angiogenesis in tumors .
|
-
- HY-P99634
-
|
PankoMab
|
Mucin
|
Cancer
|
|
Gatipotuzumab (PankoMab) is a humanized monoclonal antibody which recognizes the tumor-specific epitope of mucin-1 (TA-MUC1). Gatipotuzumab reveals a potent tumor-specific antibody-dependent cell cytotoxicity (ADCC) .
|
-
- HY-13582R
-
|
|
Parasite
Fungal
|
Infection
Cancer
|
|
Carbendazim (Standard) is the analytical standard of Carbendazim. This product is intended for research and analytical applications. Carbendazim is a potent and orally active broad-spectrum benzimidazole fungicide and can be acts as a pesticide for fungal diseases research, such as Seproria, Fusarium and Sclerotina . Carbendazim is a benzimidazole (HY-Y1825) derivative with antitumor activity and used for cancer research, especially advanced solid tumors and lymphoma .
|
-
- HY-121659
-
|
|
PSMA
|
Cancer
|
|
DCFBC is a prostate-specific membrane antigen (PSMA) inhibitor that can be used for small animal positron emission tomography (PET) imaging. DCFBC labeled with F 18 ([18F]DCFBC) can images in severe combined immunodeficient mice. [18F]DCFBC uptake is higher in PIP tumors, but almost absent in FLU tumors. [18F]DCFBC uptake is also high in the kidney and bladder, but the radioactivity washout time is shorter than that in PIP tumors. Indicating that [18F]DCFBC can specifically localize to PSMA+ expressing tumors and is applicable to the study of prostate cancer .
|
-
- HY-118276
-
|
|
Drug Derivative
|
Cancer
|
|
Lithocholenic acid, a derivative of Lithocholic acid, possesses anti-tumor activity .
|
-
- HY-N15033
-
|
|
Others
|
Cancer
|
|
Ganoderic acid U is a natural product with anti-tumor activity .
|
-
- HY-N15011
-
|
|
Others
|
Cancer
|
|
Ganoderic acid W is a natural product with anti-tumor activity .
|
-
- HY-147682
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
|
-
- HY-172491
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG2000-ESBP is a PEG compound which composed of DSPE and a E-selectin-binding peptide (ESBP). As a tumor-targeting peptide, ESBP can specifically recognize and bind to receptors or markers on the surface of tumor cells .
|
-
- HY-P4111A
-
|
|
CXCR
|
Cancer
|
|
Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research .
|
-
- HY-124711
-
TBOPP
1 Publications Verification
|
DOCK
|
Cancer
|
|
TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors .
|
-
- HY-119823
-
|
|
P-glycoprotein
|
Cancer
|
|
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin .
|
-
- HY-107271
-
|
|
Others
|
Cancer
|
|
Imperialine 3-β-D-glucoside is the glycoside of Imperialine (HY-N0696). Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-agent resistant tumor cells .
|
-
- HY-135254
-
|
CP-46665-1
|
PKC
|
Cancer
|
|
CP-46665 dihydrochloride is an anticancer agent that inhibits the incorporation of tritiated thymidine into leukemia cells and human solid tumor cells in vitro. It can lead to the loss of surface characteristics in tumor cells and disrupt cell membranes, inhibiting cell proliferation .
|
-
- HY-145729
-
|
AZD9150
|
STAT
Apoptosis
|
Cancer
|
|
Danvatirsen is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth.
|
-
- HY-W272058R
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Isometronidazole (Standard) is the analytical standard of Isometronidazole. This product is intended for research and analytical applications. Isometronidazole is a hypoxic cell sensitizer. Isometronidazole (750 mg/kg) shows an efficacy as a hypoxic cell sensitizer in severely hypoxic FaDu tumors but not in less hypoxic GL tumors.
|
-
- HY-N5166
-
|
(-)-Ardeemin
|
P-glycoprotein
|
Cancer
|
|
Ardeemin ((-)-Ardeemin) binds to the P-glycoprotein, preventing anticancer agent from being pumped out of cells. Ardeemin reverses the multidrug resistance phenotype of tumor cells and increases the sensitivity of tumor cells to anticancer agent in mammary carcinoma xenografts .
|
-
- HY-145729A
-
|
AZD9150 sodium
|
Apoptosis
STAT
|
Cancer
|
|
Danvatirsen sodium is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen sodium binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth.
|
-
- HY-172490
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG1000-ESBP is a PEG compound which composed of DSPE and a E-selectin-binding peptide (ESBP). As a tumor-targeting peptide, ESBP can specifically recognize and bind to receptors or markers on the surface of tumor cells .
|
-
- HY-172492
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG5000-ESBP is a PEG compound which composed of DSPE and a E-selectin-binding peptide (ESBP). As a tumor-targeting peptide, ESBP can specifically recognize and bind to receptors or markers on the surface of tumor cells .
|
-
- HY-156677
-
|
|
METTL3
|
Cancer
|
|
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
|
-
- HY-P99041
-
|
ABX-EGF
|
EGFR
|
Cancer
|
|
Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer .
|
-
- HY-14919A
-
|
MN-029
|
Microtubule/Tubulin
|
Cancer
|
|
Denibulin (MN-029) hydrochloride is an anti-angiogenic agent with anticancer activity. It can cause rapid closure of blood vessels in solid tumors and lead to dose-dependent killing of tumor cells, effectively enhancing the antitumor effects of radiation and cisplatin chemotherapy .
|
-
- HY-128766A
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity .
|
-
- HY-149616
-
|
|
PROTACs
ERK
|
Cancer
|
|
PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .
|
-
- HY-128766
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity .
|
-
- HY-D1711
-
|
|
Fluorescent Dye
|
Cancer
|
|
MHI-148 is a near-infrared heptamethine cyanine dye with tumor-targeting properties for cancer detection, diagnosis and research. MHI-148 is immediately taken up and accumulated by lysosomes and mitochondria of tumor cells, but not in lysosomes and mitochondria of normal cells .
|
-
- HY-173145
-
|
|
Aminopeptidase
|
Cancer
|
|
CD13-IN-1 (Compound 5f) is a CD13 inhibitor with an IC50 of 1.71 μM. CD13-IN-1 can inhibit the proliferation of multiple tumor cells and has anti-tumor activity .
|
-
- HY-P10853
-
|
|
Autophagy
|
Cancer
|
|
Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity .
|
-
- HY-168933
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR095 is an orally active WRN inhibitor with an IC50 of 0.032 μM for WRN ATPase. KWR095 can impede the duplex unwinding activity of WRN and inhibit the proliferation of tumor cells. KWR095 has anti-tumor activity .
|
-
- HY-P3822
-
|
|
Histone Methyltransferase
|
Cancer
|
PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
|
-
- HY-168280
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
AS1411-C4-VH032 (AS1411-VH032) promotes tumor-selective degradation of MDM2, leading to tumor shrinkage without detectable toxicity .
|
-
- HY-170967
-
|
|
Apoptosis
Caspase
PARP
Reactive Oxygen Species
|
Cancer
|
|
IPH10 is an anti-cancer agent that exhibits a strong anti-tumor effect in vivo without hepatic and renal toxicity. IPH10 can significantly increase the content of ROS, decrease the mitochondrial membrane potential, and induce apoptosis in tumor cells .
|
-
- HY-17419
-
-
- HY-117841
-
-
- HY-132187
-
|
|
LPL Receptor
|
Cancer
|
|
Sphingosylphosphorylcholine is a bioactive sphingolipid. Sphingosylphosphorylcholine has anti-tumor activity .
|
-
- HY-N0156
-
-
- HY-N7753
-
|
|
Others
|
Cancer
|
|
Hydroxymethylenetanshiquinone is a abietane diterpene that can inhibit tumor cell proliferation .
|
-
- HY-Z17187
-
-
- HY-169002
-
|
|
Phosphatase
|
Cancer
|
|
PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
|
-
- HY-169075
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
|
-
- HY-P99746
-
|
3C23K; GM102
|
TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming .
|
-
- HY-P10894
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
mUNO is a tumor-homing peptide (mUNO, sequence: "CSPGAK") that specifically binds to mouse CD206, targeting tumor-associated macrophages that express CD206/MRC1. mUNO can interact with human recombinant CD206 .
|
-
- HY-P10705
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
KGFRWR is a short peptide sequence, belonging to self-assembling peptides (SAPs), which can self-assemble into functional nanostructures, typically nanofibers, under physiological conditions. KGFRWR can be used to target tumor cells and tumor vasculature, exhibiting antitumor activity .
|
-
- HY-133005
-
|
4-Desacetylvinblastine; Desacetylvincaleukoblastine
|
Drug Metabolite
|
Cancer
|
|
Desacetylvinblastine (4-Desacetylvinblastine) is the major metabolite of Vinblastine (HY-13780) and a cytotoxic agent. When used alone, desacetylvinblastine has poor anti-tumor effects, but it can exert significant anti-tumor activity when in the presence of specific conjugates .
|
-
- HY-P1728
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P5098
-
|
|
Integrin
|
Cancer
|
|
E(c(RGDfK)) is an αvβ3 integrin-specific binding moiety with tumor targeting properties. Increased uptake of E(c(RGDfK)) in human ovarian cancer OVCAR-3 xenograft tumors may be useful in cancer research .
|
-
- HY-106381
-
|
|
PKC
|
Inflammation/Immunology
Cancer
|
|
Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity .
|
-
- HY-164500
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
MC3629 is an inhibitor of histone methyltransferase (EZH2) with anti-tumor activity. MC3629 inhibits SHH MB cancer cell proliferation and self-renewal and induces apoptosis. MC3629 can be used to study drug resistance in tumor aggressiveness .
|
-
- HY-N0211
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .
|
-
- HY-N10534
-
|
Lewis X
|
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Lewis X trisaccharide (Lewis X, Le x) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis .
|
-
- HY-118819
-
-
- HY-147991
-
|
|
Phosphodiesterase (PDE)
HDAC
Apoptosis
|
Cancer
|
|
PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50 values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities .
|
-
- HY-170594
-
|
|
Atg7
Autophagy
|
Cancer
|
|
Antitumor agent-192 (Compound 2f) is a β-carboline antitumor agent. Antitumor agent-192 induces autophagy in HCT116 cells via the ATG5/ATG7 pathway. Antitumor agent-192 has an IC50 of less than 5 μM for human tumor cell lines and significantly inhibits tumor development and reduces tumor weight in a mouse colorectal cancer model transplanted with allografts [1].
|
-
- HY-N4225
-
-
- HY-P10131
-
|
|
Radionuclide-Drug Conjugates (RDCs)
FAP
|
Cancer
|
|
3BP-3940 is a highly potent and selective peptide inhibitor of FAP that targets cancer-associated fibroblasts (CAFs) in the tumor microenvironment. 3BP-3940 can be labeled with radionuclides (such as Ga-68) for precise tumor imaging or Lu-177 for the development of targeted anticancer technologies. 3BP-3940 accumulates in tumor lesions and can be used to diagnose and inhibit various solid cancers and CAFs-related diseases .
|
-
- HY-163683
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity .
|
-
- HY-156111
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
|
-
- HY-124632
-
WJ460
2 Publications Verification
|
Ferroptosis
Autophagy
|
Cancer
|
|
WJ460 is a potent inhibitor of myoferlin (MYOF) that interacts directly with MYOF. WJ460 inhibits the migration and growth, induces cell cycle arrest, mitochondrial autophagy, lipid peroxidation and ferroptosis in tumor cells. WJ460 has anti-tumor activity .
|
-
- HY-Y0520S
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Itaconic acid- 13C5 is the 13C labeled Itaconic acid. Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors[1][2].
|
-
- HY-126775
-
|
|
Mitochondrial Metabolism
Endogenous Metabolite
|
Cancer
|
|
Xenoclauxin is a secondary metabolite isolated from certain species of the Penicillium genus, which exhibits an inhibitory effect on the proliferation of tumor cells. Xenoclauxin affects cellular energy metabolism, particularly by inhibiting ATP synthesis in the mitochondria. Xenoclauxin can be used for anti-tumor research .
|
-
- HY-172253
-
|
|
Apoptosis
|
Cancer
|
|
(5R)-Dimethylbenzene-camptothecin (Compound 6a) is a camptothecin derivative. (5R)-Dimethylbenzene-camptothecin is cytotoxic to tumor cells and can induce apoptosis and cell cycle arrest. (5R)-Dimethylbenzene-camptothecin has anti-tumor activity .
|
-
- HY-156607
-
|
|
Phosphatase
|
Cancer
|
|
Anticancer agent 143 (compound 369) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 143 can be used in cancer research .
|
-
- HY-156706
-
|
|
JAK
|
Cancer
|
|
JAK-IN-31 (Example 75) is a JAK inhibitor with IC50 ranges of ≤0.01µM, ≤0.01µM, 0.01-0.1 µM and ≤0.01µM for JAK1, JAK2, JAK3 and Tyk2 respectively. JAK-IN-31 can be used in cancer research .
|
-
- HY-106921A
-
-
- HY-151580S
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-14-d3 is a potent and selective CDK2 inhibitor. CDK2-IN-14-d3 can be used in research of cancer[1].
|
-
- HY-18301
-
|
|
JAK
|
Cancer
|
|
JAK-IN-35 (compound TG46) is a JAK2 inhibitor that canb be used in cancer research .
|
-
- HY-169516
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-65 (Compound 07) is a VEGFR-2 inhibitor. VEGFR-2-IN-65 has H-bond interactions with Cys180. VEGFR-2-IN-65 inhibits tube formation in HUVECs .
|
-
- HY-160171
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-31 (Compound Z1) is a CDK9 inhibitor that inhibits cancer cell growth. CDK9-IN-31 has the potential to be developed as an anticancer agent .
|
-
- HY-157451
-
|
|
Others
|
Cancer
|
|
CBR1-IN-7 (Compound JV-2) is a human CBR1 inhibitor (IC50=8 μM). CBR1-IN-7 can be used in cancer research .
|
-
- HY-162007
-
|
|
CDK
|
Cancer
|
|
PYRA-2 is a CDC7 kinase inhibitor with potential for cancer research .
|
-
- HY-157822
-
-
- HY-101340A
-
|
CFI-402257 hydrochloride
|
Mps1
|
Cancer
|
|
CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity .
|
-
- HY-152196
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM .
|
-
- HY-106174
-
|
CS 891
|
5 alpha Reductase
|
Cancer
|
|
Lapisteride (CS 891) is an orally active 5α-reductase inhibitor. Lapisteride can be used in cancer research .
|
-
- HY-156705
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-25 (CY-16-1) is a CDK-7 inhibitor (IC50<1nM) that can be used in cancer research .
|
-
- HY-160171A
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-31 dimaleate (Compound Z1) is a CDK9 inhibitor that inhibits cancer cell growth. CDK9-IN-31 dimaleate has the potential to be developed as an anticancer agent .
|
-
- HY-106921
-
-
- HY-156715
-
|
|
MASTL
|
Cancer
|
|
MASTL-IN-1 is a MASTL (microtubule-associated serine/threonine kinase-like) inhibitor, which is involved in cell proliferation, migration, and invasion. MASTL-IN-1 has potential in cancer research .
|
-
- HY-12300
-
|
CFI-400945 free base
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
CFI-400945 free base is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.
|
-
- HY-156608
-
|
|
Phosphatase
|
Cancer
|
|
Anticancer agent 144 (compound 444) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 144 can be used in cancer research .
|
-
- HY-P10786
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. LinTT1 peptide targets peritoneal carcinoma (PC) by binding to the p32 (gC1qR) receptor. It can conjugate with iron oxide nanoworms (NWs) to form a nanocarrier. This nanocarrier is taken up by peritoneal carcinoma cells in vitro and enters the mitochondria; it also exhibits significant tumor targeting and penetration effects in mice. Moreover, LinTT1-functionalized nanocarriers, combined with the pro-apoptotic peptide [D(KLAKLAK)2], show significant tumor suppression in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery carrier for peritoneal cancer research .
|
-
- HY-U00337
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.
|
-
- HY-N11954
-
|
|
Others
|
Cancer
|
|
Schiarisanrin C is bioactive C19 homolignan with anti-tumor activities .
|
-
- HY-10249A
-
|
|
Akt
|
Cancer
|
|
AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity .
|
-
- HY-160263S
-
-
- HY-16509
-
-
- HY-N1977
-
|
|
Others
|
Cancer
|
|
Podophyllotoxin glucoside is a podophyllotoxin derivative, has anti-tumor effects .
|
-
- HY-142058
-
-
- HY-N11479
-
-
- HY-N12013
-
|
|
Others
|
Cancer
|
|
11-Oxomogroside IV A (compound 12) is a cucurbitane triterpene glycoside isolated from unripe fruits of Luo Han Guo. 11-Oxomogroside IV A has anti-tumor effects and is cytotoxic to tumor cells SMMC-772 (IC50: 288 μg/mL) .
|
-
- HY-N7000
-
-
- HY-15855
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Fosbretabulin (tromethamine), also known as combretastatin A4 phosphate (CA4P), is a vascular disrupting agent evaluated for its efficacy against anaplastic thyroid carcinoma (ATC). It targets tumor neovasculature, causing acute and reversible reductions in tumor blood flow and central necrosis .
|
-
- HY-139289S
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
ART899 is a highly specific allosteric inhibitor of the Polθ DNA polymerase domain. ART899 can effectively enhance the radiosensitivity of tumor cells, shows good tolerance when combined with fractionated radiation, and significantly reduces tumor growth compared to radiation alone .
|
-
- HY-164502
-
|
|
Akt
|
Cancer
|
|
NAP1051 is a biomimetic analog of lipin A4 that achieves anti-tumor effects by targeting the inflammatory tumor microenvironment. NAP1051 inhibits neutrophil chemotaxis to fMLP and stimulates macrophage efferocytosis by activating AKT. NAP1051 can be used in colorectal cancer research .
|
-
- HY-172692
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG1000-TH is a PEG compound which composed of DSPE and a pH-responsive cell penetrating peptide (TH). TH is activated in an acidic environment (such as the tumor microenvironment) and can selectively carry small molecules, oligonucleotides, proteins, etc. into tumor cells .
|
-
- HY-144125
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-41 (compound N-12), a potent antitumor agent, enhibits excellent antimigration and anti-invasion activity. Antitumor agent-41 (compound N-12) induces tumor inhibition via tumor necrosis and inflammatory response .
|
-
- HY-P10709
-
|
|
Biochemical Assay Reagents
|
Cardiovascular Disease
Cancer
|
|
CREKA peptide is a short peptide sequence, belonging to self-assembling peptides (SAPs), which can self-assemble into functional nanostructures, typically nanofibers, under physiological conditions. CREKA peptide can be used to target tumor cells and tumor vasculature, exhibiting antitumor activity .
|
-
- HY-N14752
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Hydroxymycotrienin A is an Ansa antibiotic. Hydroxymycotrienin A has the activity of inhibiting human neck tumor cell line, and its inhibitory effect on human papillomavirus (HPV) gene positive neck tumor cells (such as HeLa, CaSKi, SiHa, etc.) is stronger than HPV gene negative cells .
|
-
- HY-125443
-
|
|
Others
|
Cancer
|
|
Lucialdehydes A is a lanostante-type triterpene aldehydes, isolated from the fruiting bodies of Ganoderma lucidum. Lucialdehydes A shows cytotoxic effects on tumor cells, including Lewis lung carcinoma (LLC), T-47D, Sarcoma 180, and Meth-A tumor cell lines .
|
-
- HY-172694
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG5000-TH is a PEG compound which composed of DSPE and a pH-responsive cell penetrating peptide (TH). TH is activated in an acidic environment (such as the tumor microenvironment) and can selectively carry small molecules, oligonucleotides, proteins, etc. into tumor cells .
|
-
- HY-149298
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-2 is an inhibitor of PSMA with a Ki value of 1.07 nM. PSMA-IN-2 displays favorable in vivo NIR imaging (λEM = 1088 nm, λex = 808 nm), and can be used for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice .
|
-
- HY-120429
-
|
|
Apoptosis
|
Cancer
|
|
SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis .
|
-
- HY-172693
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG2000-TH is a PEG compound which composed of DSPE and a pH-responsive cell penetrating peptide (TH). TH is activated in an acidic environment (such as the tumor microenvironment) and can selectively carry small molecules, oligonucleotides, proteins, etc. into tumor cells .
|
-
- HY-130625
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model .
|
-
- HY-118138
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
NC-182 is an anti-tumor agent and DNA intercalator with a preference for B-form DNA. NC-182 can also promote the unwinding of Z-form DNA to B-form. NC-182 has a potent inhibitory effect on multidrug-resistant and sensitive tumors.
|
-
- HY-15701B
-
ADH-503
1 Publications Verification
(Z)-Leukadherin-1 choline
|
Complement System
|
Cancer
|
|
ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses .
|
-
- HY-120046
-
|
|
HDAC
|
Cancer
|
|
YF479 is a potent inhibitor of histone deacetylase. YF479 abates cell viability, suppresses colony formation and tumor cell motility. YF479 significantly inhibits breast tumor growth and metastasis. YF479 has the potential for the research of clinical trials for breast cancer .
|
-
- HY-16532
-
|
AEZS-108; AN-152
|
Peptide-Drug Conjugates (PDCs)
GnRH Receptor
|
Cancer
|
|
Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro .
|
-
- HY-16147
-
|
Oxi4503; CA1P; Combretastatin A1 diphosphate
|
Others
|
Cancer
|
|
Combretastatin A1 phosphate (Oxi4503; CA1P; Combretastatin A1 diphosphate) is a potent vascular disruptive agent. Combretastatin A1 phosphate exerts anti-angiogenic effects on tumors. Combretastatin A1 phosphate has the potential for the research of pancreatic neuroendocrine tumors .
|
-
- HY-153191
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-15 is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors .
|
-
- HY-153552
-
|
|
Drug Derivative
FAP
|
Cancer
|
|
NH2-UAMC1110 is a UAMC1110 (HY-100684) derivative that can be used in the synthesis of FAPI-QS. FAPI-QS is a chelating agent that can be used to manufacture high tumor selectivity and high dose radiotracers for the diagnosis and treatment of tumors .
|
-
- HY-P1728A
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-147204
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A) .
|
-
- HY-P99041A
-
|
|
EGFR
|
Cancer
|
|
Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer .
|
-
- HY-135217
-
|
|
Apoptosis
|
Cancer
|
|
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-P10884
-
-
- HY-112802A
-
|
|
c-Kit
|
Cancer
|
|
AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
|
-
- HY-15721
-
-
- HY-N15041
-
-
- HY-N10353
-
-
- HY-N8197
-
|
|
Others
|
Cancer
|
|
Epigambogic acid is a natural anti-tumor, antitussive, expectorant and anti-inflammatory compound .
|
-
- HY-N4124
-
|
|
Others
|
Cancer
|
|
Poricoic acid B, isolated from Poria cocos, possesses anti-tumor activity .
|
-
- HY-16114
-
BNC105
1 Publications Verification
|
Microtubule/Tubulin
|
Cancer
|
|
BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
|
-
- HY-N9400
-
-
- HY-N6988
-
|
|
Others
|
Cancer
|
|
Cimigenol is an active compound isolated from Cimicifuga, with potent anti-tumor activity .
|
-
- HY-113450
-
-
- HY-169100
-
|
|
VEGFR
PI3K
Akt
mTOR
p38 MAPK
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues .
|
-
- HY-148808
-
|
RXC007
|
ROCK
|
Cancer
|
|
Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma .
|
-
- HY-116217
-
|
FdCyd; NSC-48006
|
DNA Methyltransferase
|
Cancer
|
|
5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity .
|
-
- HY-10338A
-
|
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
Foretinib phosphate is an orally bioavailable small molecule with potential anti-tumor activity. Foretinib phosphate can selectively inhibit hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib phosphate shows different anti-cancer activity from cabozantinib in lung cancer cells and has stronger inhibitory effects on targets such as MEK1/2, FER and AURKB .
|
-
- HY-122703
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors .
|
-
- HY-118672
-
|
|
HDAC
MMP
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer .
|
-
- HY-10984A
-
|
(S)-CC-4047
|
Endogenous Metabolite
|
Cancer
|
|
(S)-Pomalidomide ((S)-CC-4047) is an angiogenesis-inhibiting drug with growth-inhibitory activity against B-cell tumors. (S)-Pomalidomide can induce complete tumor regression in BurKitt lymphoma cells. (S)-Pomalidomide serves as an immunomodulator with potential applications in inhibiting hematological malignancies .
|
-
- HY-162463
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Ir-UA is an usnic acid-derived iridium(III) complex that enhances PD-L1 expression and converts "cold tumors" into "hot tumors." Ir-UA stimulates PD-L1 expression by explicitly regulating the PD-L1 transcription factor .
|
-
- HY-172272B
-
|
|
Liposome
VEGFR
|
Cancer
|
|
DSPE-PEG5000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
|
-
- HY-N15103
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Hydroxymycotrienin B is an Ansa antibiotic. Hydroxymycotrienin B has the activity of inhibiting human neck tumor cell line, and its inhibitory effect on human papillomavirus (HPV) gene positive neck tumor cells (such as HeLa, CaSKi, SiHa, etc.) is stronger than HPV gene negative cells .
|
-
- HY-172272A
-
|
|
Liposome
VEGFR
|
Cancer
|
|
DSPE-PEG2000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
|
-
- HY-128749
-
|
Potassium D-glucarate
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
D-Glucaric acid potassium (Potassium D-glucarate) is an orally active end product of the D-glucuronic acid pathway in mammals. D-Glucaric acid potassium is present in a variety of fruits and vegetables. D-Glucaric acid potassium has cholesterol-lowering and anti-tumor activities. D-Glucaric acid potassium can inhibit tumor cell proliferation and inflammation, and induce apoptosis.
|
-
- HY-P99776
-
|
XmAb-13676
|
CD20
CD3
|
Cancer
|
|
Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 + expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .
|
-
- HY-135849B
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
Catalase, Human Erythrocyte is an important antioxidant enzyme. Catalase, Human Erythrocyte plays an important role in removing ROS and maintaining the balance of redox state. Catalase, Human Erythrocyte is closely related to the occurrence and development of tumors. Catalase, Human Erythrocyte has the potential to be used in tumor prevention research .
|
-
- HY-151508
-
|
|
Liposome
|
Cancer
|
|
Diamino lipid DAL4 is diamino lipid for the preparation of lipid nanoparticles (LNPs) encapsulated with mRNAs encoding cytokines including IL-12, IL-27 and GM-CSF. Diamino lipid DAL4 delivers mRNA to tumor cells to exert anti-tumor activity .
|
-
- HY-119767
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
Jolkinolide A is a diterpenoid, can be extracted from the roots of Euphorbia fischeriana Steud. Jolkinolide A exhibits anti-tumor activity, by affecting on angiogenesis of tumor tissues. Jolkinolide A significantly inhibits the Akt-STAT3-mTOR signaling pathway and reduces the expression of VEGF in A549 cells .
|
-
- HY-172272
-
|
|
Liposome
VEGFR
|
Cancer
|
|
DSPE-PEG1000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors .
|
-
- HY-12624
-
|
ON123300
|
CDK
AMPK
PDGFR
|
Cancer
|
|
Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
|
-
- HY-111965
-
-
- HY-149053B
-
|
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
(R)-OY-101 is an orally active and specific inhibitor of P-gp. (R)-OY-101 increases tumor sensitivity to anticancer agents. (R)-OY-101 has good activity in reversing tumor resistance and promoting apoptosis and can be used in cancer related research .
|
-
- HY-P99039
-
|
MEDI9447
|
CD73
|
Cancer
|
|
Oleclumab (MEDI9447) is a human IgG1λ monoclonal antibody targeting CD73 and inhibits the exonuclease activity of the extracellular enzyme CD73. Oleclumab can adjust the composition of bone marrow and lymphoid infiltrating leukocyte populations in the tumor microenvironment and has anti-tumor activity .
|
-
- HY-113003
-
|
γ-Glutamylglutamine; γ-Glu-Gln
|
Amino Acid Derivatives
|
Others
Cancer
|
|
H-γ-Glu-Gln-OH is a hydrophilic peptide and can be conjugated to drugs. The carrier composed of H-γ-Glu-Gln-OH has the characteristics of high water solubility and drug-loading capacity, good biocompatibility, low toxicity, improved tumor targeting ability, and anti-tumor efficacy .
|
-
- HY-155100
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
BI 7446 is a cyclic dinucleotide (CDN)-based potent and selective stimulator of interferon genes (STING) agonist. BI 7446 can activate all five STING variants in cells and induce tumor-specific immune-mediated tumor rejection. BI 7446 can be used for immuno-oncology research .
|
-
- HY-N10447
-
|
|
Apoptosis
|
Cancer
|
|
Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-B1250
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Acedoben is a biochemical agent. Acedoben and iron ions can construct a fast self-assembled coordination complex. The Fe-Ace coordination complex can not only serve as a carrier of tumor antigens, but also enhance antigen-specific anti-tumor immunity due to its inherent adjuvant properties .
|
-
- HY-106056
-
|
D 16726
|
Estrogen Receptor/ERR
|
Cancer
|
|
Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
|
-
- HY-N10355
-
|
|
Apoptosis
|
Cancer
|
27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent .
|
-
- HY-15701A
-
|
ADH-503 free base
|
Complement System
|
Cancer
|
|
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses .
|
-
- HY-B1250A
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Acedoben sodium is the sodium salt form of Acedoben. Acedoben and iron ions can construct a rapidly self-assembled coordination complex, and the Fe-Ace coordination complex can not only serve as a carrier of tumor antigens, but also enhance antigen-specific anti-tumor immunity due to its inherent adjuvant properties .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-126468
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Abieslactone is a compound with anti-tumor promoting activity, exhibiting significant potential for therapeutic applications in oncology.
|
-
- HY-19459
-
-
- HY-155445
-
|
|
Others
|
Cancer
|
|
di-DTPA TL is a hydrophilic bivalent DTPA hapten that can be used for tumor research .
|
-
- HY-114639
-
|
|
Others
|
Others
|
|
Maritinone is a compound with antiproliferative activity and exhibits strong cytostatic activity in various tumor cell lines.
|
-
- HY-N2596
-
-
- HY-106801
-
|
RP 49532
|
Others
|
Cancer
|
|
Girolline (RP 49532) can inhibit protein biosynthesis and has anti-tumor effect .
|
-
- HY-14947
-
|
MKI 833
|
MEK
|
Cancer
|
|
Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
|
-
- HY-16496
-
-
- HY-N0237
-
-
- HY-119169
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulozole is an orally active synthetic microtubule inhibitor. Tubulozole can be used for the research of tumor .
|
-
- HY-139858
-
-
- HY-N9390
-
|
|
Others
|
Cancer
|
|
Wilforlide B, a natural norditerpenoid, possesses anti-tumor activity in human cancer cells .
|
-
- HY-107226
-
|
|
Others
|
Cancer
|
|
Crovatin, isolated from the stem bark of C. oblongifolius, shows anti-tumor effect .
|
-
- HY-U00379
-
|
|
Others
|
Cancer
|
|
LM985 is one of a series of compounds based on the flavone ring structure, with anti-tumor activities.
|
-
- HY-13727A
-
|
BBR 2778
|
Topoisomerase
|
Cancer
|
|
Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
|
-
- HY-N0837
-
|
NSC17821; NSC23880
|
Others
|
Cancer
|
|
Veratramine(NSC17821; NSC23880) is useful as a signal transduction inhibitor for treating tumors.
|
-
- HY-N0517
-
-
- HY-147081A
-
|
AGRO-100 sodium
|
DNA/RNA Synthesis
|
Cancer
|
|
AS1411 sodium is a quadruplex-forming oligonucleotide aptamer that targets nucleolin. It has anti-tumor activity.
|
-
- HY-16212
-
-
- HY-172498
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG5000-CREKA is a PEG compound which composed of DSPE and a fibrin-targeting peptide (CREKA). CREKA peptide can be used to target tumor cells and tumor vasculature, exhibiting antitumor activity. DSPE-PEG5000-CREKA can be used for drug delivery .
|
-
- HY-172497
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG2000-CREKA is a PEG compound which composed of DSPE and a fibrin-targeting peptide (CREKA). CREKA peptide can be used to target tumor cells and tumor vasculature, exhibiting antitumor activity. DSPE-PEG2000-CREKA can be used for drug delivery .
|
-
- HY-172496
-
|
|
Liposome
|
Cancer
|
|
DSPE-PEG1000-CREKA is a PEG compound which composed of DSPE and a fibrin-targeting peptide (CREKA). CREKA peptide can be used to target tumor cells and tumor vasculature, exhibiting antitumor activity. DSPE-PEG1000-CREKA can be used for drug delivery .
|
-
- HY-11005
-
BX-912
4 Publications Verification
|
PDK-1
Apoptosis
|
Cancer
|
|
BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
|
-
- HY-139211
-
|
3,4-Difluorobenzylidene curcumin
|
Reactive Oxygen Species
|
Cancer
|
|
Difluorinated Curcumin (3,4-Difluorobenzylidene curcumin) is a fluorinated curcumin analog with high bioavailability and anticancer activity. Difluorinated Curcumin inhibits the self-renewal ability of tumor stem/stem-like cells, clonogenicity, invasiveness and angiogenesis of tumor cells. Difluorinated Curcumin also increases cell sensitivity to chemotherapy .
|
-
- HY-119505
-
|
|
HDAC
|
Others
|
|
Curcuphenol is a compound with histone deacetylase enhancing activity and has the activity of reversing immune escape. Curcuphenol can reverse the immune escape of tumors by restoring the expression of antigen presentation machinery. Its two synthetic analogs have histone deacetylase enhancing activity and play an important role in the immune recognition of metastatic tumors.
|
-
- HY-170565
-
|
|
Mitophagy
Apoptosis
|
Cancer
|
|
CHD-1 is a a hypoxia-activated antitumor prodrug. CHD-1 impairs mitochondrial morphology and membrane potential in hypoxic tumor cells, further triggering excessive mitophagy and inducing apoptosis. CHD-1 inhibits the growth of hypoxic tumor cells in vitro and the growth of HeLa xenograft in vivo .
|
-
- HY-16938R
-
|
5'-(Methylthio)-5'-deoxyadenosine (Standard); 5'-Deoxy-5'-(methylthio)adenosine (Standard); 5'-S-Methyl-5'-thioadenosine (Standard)
|
Endogenous Metabolite
Apoptosis
Parasite
|
Metabolic Disease
Cancer
|
|
5'-Methylthioadenosine (Standard) is the analytical standard of 5'-Methylthioadenosine. This product is intended for research and analytical applications. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
|
-
- HY-109139A
-
|
NIR178 mesylate; PBF509 mesylate
|
Adenosine Receptor
|
Cancer
|
|
Taminadenant mesylate (NIR178 mesylate) is a potent adenosine A2A receptor antagonist with potential anti-tumor activity. Taminadenant mesylate can selectively bind and inhibit A2AR on T lymphocytes, thereby releasing adenosine/A2AR-mediated inhibition of T lymphocytes and activating T cell-mediated immune responses against tumor cells. Taminadenant mesylate works by reducing the proliferation of susceptible tumor cells. Taminadenant mesylate also showed effectiveness in reversing dyskinesias in Parkinson's disease models and was able to inhibit dyskinesias caused by L-DOPA .
|
-
- HY-128946
-
|
|
Drug-Linker Conjugates for ADC
|
Inflammation/Immunology
Cancer
|
|
CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects .
|
-
- HY-16938S
-
|
5'-(Methylthio)-5'-deoxyadenosine-13C6; 5'-Deoxy-5'-(methylthio)adenosine-13C6; 5'-S-Methyl-5'-thioadenosine-13C6
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
Cancer
|
|
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
|
-
- HY-16938S1
-
|
5'-(Methylthio)-5'-deoxyadenosine-d3; 5'-Deoxy-5'-(methylthio)adenosine-d3; 5'-S-Methyl-5'-thioadenosine-d3
|
Apoptosis
Parasite
Endogenous Metabolite
|
Inflammation/Immunology
|
|
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
|
-
- HY-160015
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
CB07-Exatecan is an ADC drug-Linker conjugate that can be used for the synthesis of ADCs. ADC conjugated with CB07-Exatecan and trastuzumab inhibits the growth of HER2-positive cancer cells. CB07-Exatecan can be used in cancer research .
|
-
- HY-P99261
-
|
OMP 21M18
|
Notch
|
Cancer
|
|
Demcizumab (OMP 21M18) is an anti-DLL4 monoclonal antibody. Demcizumab is a potent inhibitor of the Notch pathway. Demcizumab alone or in combination with chemotherapy is effective in various cancer models .
|
-
- HY-129960
-
-
- HY-136979
-
|
|
PARP
|
Inflammation/Immunology
Cancer
|
|
RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants .
|
-
- HY-B1610
-
|
Trisodium citrate dihydrate; Citric acid trisodium salt dihydrate
|
Bacterial
Endogenous Metabolite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Sodium citrate dehydrate (Trisodium citrate dihydrate) is a natural product with oral activity that can be found in citrus fruits. Sodium citrate dehydrate can inhibit the proliferation of tumor cells and induce apoptosis. Sodium citrate dehydrate has antibacterial, anti-tumor and antioxidant activities. Sodium citrate dehydrate can be prepared as a cosolvent or buffer .
|
-
- HY-N11928
-
|
|
Others
|
Cancer
|
|
Changnanic acid (schisandrin) is a triterpene compound with potential anti-tumor effects. Changnanic acid exhibits moderate cytotoxic activity against human tumor cell lines Bel-7402, MCF-7 and HL-60, with IC50s of 100 μM, 100 μM and 50.51 μM respectively .
|
-
- HY-156568A
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-13659
-
|
NSC 650426
|
Antibiotic
Bcl-2 Family
Apoptosis
|
Infection
Cancer
|
|
KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice .
|
-
- HY-168901
-
|
|
Src
|
Cancer
|
|
Hck-IN-2 (Compound 8e) is an HCK inhibitor. Hck-IN-2 is cytotoxic to tumor cells, with IC50 values of 19.58 μM and 1.42 μM against MDA-MB231 and MCF-7, respectively. Hck-IN-2 has anti-tumor activity .
|
-
- HY-153306
-
|
|
PI3K
|
Cancer
|
|
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
|
-
- HY-119866
-
-
- HY-100693
-
-
- HY-16503
-
|
NSC 39069; Treosulphan
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Treosulfan (NSC 39069) is a bifunctional alkylating agent with activity in ovarian cancer and other solid tumor types.
|
-
- HY-N0184
-
-
- HY-19601
-
|
U 80244
|
Drug Intermediate
|
Cancer
|
|
Carzelesin is a cyclopropylpyrroloindole precursor molecule and effectively inhibits tumor growth. Carzelesin may be used in cancer research.
|
-
- HY-127005
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Ritrosulfan is a member of the alkylating sugar alcohol. Ritrosulfan is a hydrolyzing alkylating agent with anti-tumor activity .
|
-
- HY-N14995
-
-
- HY-123380
-
|
Methyl bruneomycin; NSC-45384
|
Drug Derivative
|
Cancer
|
|
Methyl streptonigrin (Methyl bruneomycin) is a derivative of streptonigrin. Methyl streptonigrin has anti-tumor activity .
|
-
- HY-N1550
-
|
Norsalvioxide
|
Others
|
Cancer
|
|
Przewalskin (Norsalvioxide) is a natural product found in Salvia yunnanensis. Przewalskin shows anti-tumor activity .
|
-
- HY-13742
-
|
IPdR
|
HSV
|
Cancer
|
|
Ropidoxuridine (IPdR) is a novel orally available, halogenated thymidine analog and is a potential radiosensitizer for use in human tumors.
|
-
- HY-123190
-
-
- HY-156982
-
|
|
Others
|
Cancer
|
|
Parpi is a PET radioactive tracer with low lipotropy. Parpi can be used as a tumor imaging agent .
|
-
- HY-N8840
-
|
|
Others
|
Cancer
|
|
Laricitrin (compound 4) is an O-methylated flavonol, a type of flavonoid, that has anti-tumor effect .
|
-
- HY-N14025
-
-
- HY-142965
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-28, a novel HDAC inhibitor, shows potent activities against tumor growth and metastasis
|
-
- HY-153863
-
|
|
PROTACs
MEK
Raf
|
Cancer
|
|
MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078)) .
|
-
- HY-159803
-
|
6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin
|
Endogenous Metabolite
|
Cancer
|
|
IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitory activity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitory activity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
|
-
- HY-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
|
-
- HY-149053
-
|
|
P-glycoprotein
|
Cancer
|
|
OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764) .
|
-
- HY-P99934
-
|
ABBV-621
|
Apoptosis
|
Cancer
|
|
Eftozanermin alfa (ABBV-621) is a second-generation tumor necrosis factor-related apoptosis-inducing ligand receptor (TRAIL-R) agonist. Eftozanermin alfa induces apoptosis in tumor cells by activation of death receptors 4/5. Eftozanermin alfa can be used for the research of multiple solid and heme malignancies .
|
-
- HY-50895A
-
|
ZD-1839 hydrochloride
|
EGFR
|
Cancer
|
|
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .
|
-
- HY-N3181
-
-
- HY-136404
-
|
|
Fluorescent Dye
|
Cancer
|
|
Melanin probe-1 is an 18F-picolinamides based PET probe. Melanin probe-1 can be used for PET imaging of malignant melanoma. Melanin probe-1 exhibits high tumor targeting efficiency, excellent tumor imaging contrasts, desirable biodistribution patterns, and good in vivo stability .
|
-
- HY-149886
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-9 (compound 35r) is an inhibitor ofHIF-2α. HIF-2α-IN-9 inhibits VEGF-A (IC50=305 nM), and regulates growth-promoting genes in tumor cells, reactivates macrophage-mediated tumor immunity .
|
-
- HY-N7223
-
|
|
YAP
Apoptosis
|
Cancer
|
|
Lappaol F, a lignin, is an anticancer agent. Lappaol F inhibits YAP mRNA and protein level. Lappaol F inhibits tumor cell growth by inducing cell cycle arrest. Lappaol F induces cancer cell apoptosis, and inhibits tumor growth. Lappaol F can be isolated from Arctium lappa Linne (Asteraceae) .
|
-
- HY-42484
-
|
Eribulin intermediate
|
Microtubule/Tubulin
|
Cancer
|
|
ER-076349 (Eribulin intermediate) is an inhibitor of tubulin polymerization, induces G2-M cell cycle arrest, and disrupts mitotic spindles. ER-076349 inhibits cancer cell growth, and inhibits tumor growth in several human tumor xenografts. ER-076349 is an analog of Halichondrin B .
|
-
- HY-13561
-
|
M475271
|
Src
|
Cancer
|
|
AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.0 8 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro an vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026) .
|
-
- HY-155995
-
|
MK-905
|
Biochemical Assay Reagents
|
Cancer
|
|
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
|
-
- HY-107513
-
|
|
mGluR
|
Neurological Disease
Cancer
|
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
|
-
- HY-N5112B
-
|
Isoarnebin I
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
Notch
NO Synthase
Bcl-2 Family
|
Cancer
|
|
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
|
-
- HY-W654139
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Parasite
Apoptosis
|
Metabolic Disease
|
|
5'-Deoxy-5'-(methylthio)adenosine-d3 is deuterium labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis.
|
-
- HY-156124
-
|
|
Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
|
-
- HY-162415
-
|
|
c-Fms
Apoptosis
|
Cancer
|
|
CSF1R-IN-22 (Compound C19) is an orally effective CSF-1R selective inhibitor (IC50<6 nM). CSF1R-IN-22 enhances the secretion of CXCL9 from M2 macrophages, increases CD8 + T cell infiltration. CSF1R-IN-22 boosts anti-tumor immune responses of anti-PD-1, and induces apoptosis in tumor cells. CSF1R-IN-22 can effectively reprogram M2-like TAMs (tumor-associated macrophages) to the M1 phenotype and reshape the TME by inducing the recruitment of CD8 + T cells into tumors and reducing the infiltration of immunosuppressive Tregs and MDSCs .
|
-
- HY-19471
-
|
|
Drug Isomer
CDK
VEGFR
Survivin
Apoptosis
|
Cancer
|
|
(rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET .
|
-
- HY-N15104
-
-
- HY-N3512
-
|
|
Others
|
Cancer
|
|
Wilfornine A is a natural product that can be isolated from Schisandra sphenanthera. Wilfornine A has anti-tumor effect .
|
-
- HY-N0370
-
|
5-Methoxypsoralen
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
|
-
- HY-103471
-
|
|
FAK
|
Cancer
|
|
Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth .
|
-
- HY-10247
-
|
|
Raf
|
Cancer
|
|
BRAF inhibitor (Compound P-0850) is a B-Raf inhibitor with anti-tumor activity .
|
-
- HY-164827
-
|
|
CDK
|
Cancer
|
|
CDK2 degrader 3 can selectively degrade CDK2 and has anti-tumor activity .
|
-
- HY-N10602
-
|
|
Others
|
Cancer
|
|
Caryatin is a natural product found in Rhododendron simiarum, and Aeonium decorum. Caryatin shows anti-tumor activity .
|
-
- HY-128939
-
|
|
Antifolate
|
Cancer
|
|
EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities .
|
-
- HY-N3988
-
|
|
Others
|
Cancer
|
|
Hannokinol is a potent anti-tumor agent. Hannokinol shows antiproliferative activity. Hannokinol shows antioxidant activities .
|
-
- HY-44680
-
|
|
Drug Intermediate
|
Cancer
|
|
L-Cystine N-carboxyanhydride can be used for synthesis of polyamino acid carrier for anti-tumor agent delivery .
|
-
- HY-118327
-
|
N-carbamylmaleamic acid
|
DNA/RNA Synthesis
|
Cancer
|
|
Maleuric acid has cytotoxicity on Ehrlich ascites tumor cells by preventing the entry of preprophase cells into mitosis[1].
|
-
- HY-143510
-
|
|
mTOR
|
Cancer
|
|
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
|
-
- HY-N4255
-
|
|
Others
|
Cancer
|
|
Resibufagin is a kind of bufadienolide isolated from the venom of Bufo bufo gargarizans, has anti-tumor activities .
|
-
- HY-N1128
-
|
(-)-Trichorabdal A
|
Bacterial
|
Cancer
|
|
Trichorabdal A is a diterpenoid compound isolated from Rabdosia trichocarpa. Trichorabdal A has potent anti-tumor activity .
|
-
- HY-13551B
-
|
m-AMSA (gluconate); Acridinyl anisidide (gluconate)
|
Topoisomerase
Autophagy
|
Cancer
|
|
Amsacrine gluconate is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
|
-
- HY-N15026
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
13-Hydroxyglucopiericidin A is an antibiotic. 13-Hydroxyglucopiericidin A has strong anti-tumor cell activity .
|
-
- HY-122532
-
|
|
Histone Methyltransferase
|
Cancer
|
|
Fagaronine chloride is an alkaloid with inhibitory activity against reverse transcriptase and topoisomerase I. Fagaronine chloride can effectively inhibit the reverse transcriptase of RSii tumor virus at a concentration of 6-60 μg/mL. Fagaronine chloride rapidly blocks the synthesis of DNA polymerase by interacting with the template primer. Fagaronine chloride has shown anti-tumor potential, especially in the study of retroviral infection .
|
-
- HY-100443
-
|
PX-102
|
FXR
|
Cancer
|
|
PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy .
|
-
- HY-162958
-
|
|
Apoptosis
TrxR
|
Cancer
|
|
Photosensitizer-6 (Compound 4) is a gold (I) complex and exhibits inhibitory activity against TrxR. Photosensitizer-6 induces apoptosis in 4T1 cell, targets and eradicates tumors through chemo-phototherapy and immunogenic cell death under light exposure. Photosensitizer-6 can be used for tumor imaging .
|
-
- HY-128776
-
|
|
TNF Receptor
|
Cancer
|
|
Antitumor agent-19 is an antitumor agent that targets tumor-associated macrophages (TAMs) and can be used as a potent TAMs modulator. Antitumor agent-19 can increase TNF-alpha levels in tumor cells with EC50 values???of 17.18 μM and 18.87 μM in RAW 264.7 cells and BMDM cells, respectively .
|
-
- HY-100765
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis .
|
-
- HY-10964
-
|
DMXAA; ASA-404
|
STING
IFNAR
Influenza Virus
|
Infection
Cancer
|
|
Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities.
|
-
- HY-W021377C
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 4 dihydrochloride is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
|
-
- HY-124484
-
|
|
Notch
|
Cancer
|
|
JI130 (JI051 derivative?) is a stabilizer for the?Hes1-PHB2?interaction. JI130 inhibits?the ability of Hes1 to repress transcription. JI130?significantly reduces the tumor growth in a murine pancreatic tumor model and has the potential for ?managing pancreatic cancer .
|
-
- HY-107999
-
CADD522
4 Publications Verification
|
Reactive Oxygen Species
|
Cancer
|
|
CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer .
|
-
- HY-149297
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer .
|
-
- HY-148669
-
|
JNJ-75276617; Menin-MLL inhibitor 24
|
Apoptosis
Histone Methyltransferase
FLT3
|
Cancer
|
|
Bleximenib (JNJ-75276617) is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib can be used in the research of tumors such as leukemia .
|
-
- HY-N6046
-
|
|
NF-κB
Apoptosis
Caspase
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
Cancer
|
|
Kamebakaurin is an orally active diterpenoid compound that can be isolated from Isodon excia (Maxin.). Kamebakaurin can inhibit NF-κB activation by directly targeting the DNA-binding activity of p50. Kamebakaurin can induce apoptosis and cell cycle arrest in tumor cells. Kamebakaurin has anti-inflammatory and anti-tumor activities .
|
-
- HY-N12978
-
|
|
Others
|
Cancer
|
|
Benzyl β-gentiobioside is a phenyl alcohol glycoside found in peach kernels (Prunus persica seeds). Benzyl β-gentiobioside has anti-tumor promoting activity by inhibiting TPA (12-O-tetradecanoylphorbol 13-acetate, a tumor promoter)-induced Epstein-Barr virus early antigen (EBV-EA) activation .
|
-
- HY-172395
-
|
|
Microtubule/Tubulin
Topoisomerase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
TopoII/tubulin-IN-1 (Compound 1B8) is a TopoII/tubulin inhibitor. TopoII/tubulin-IN-1 can inhibit the proliferation and the level of ROS of tumor cells, induce apoptosis and cell cycle arrest of tumor cells, but has no significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 has antitumor activity .
|
-
- HY-P991087
-
|
|
FAP
|
Cancer
|
|
RO7122290 is a bispecific fusion protein carrying a split trimeric 4-1BB (CD137) ligand and a fibroblast activation protein α (FAP) binding site. O7122290 is a FAP-α-targeted 4-1BB agonist that costimulates T cells for improved tumor cell killing in FAP-expressing tumors .
|
-
- HY-N0211R
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone (Standard) is the analytical standard of Cyasterone. This product is intended for research and analytical applications. Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .
|
-
- HY-154857
-
|
|
Scavenger Receptor Class B type I (SR-BI）
|
Cancer
|
|
1-Palmitoyl-2-succinyl-sn-glycerophosphorylcholine is a glycerophosphorylcholine, consisting of glycerol phosphate, choline and palmitic acid. It accumulates in vivo at sites of oxidative stress. 1-Palmitoyl-2-succinyl-sn-glycerophosphorylcholine may be a ligand of scavenger receptors class B, while oxidized phospholipids oxPC(CD36) are potent ligands of scavenger receptors class B (CD36 and SR-BI). Oxidized phospholipids (oxPLs) also play an important role in tumor apoptosis, may be elevated in malignant biliary strictures .
|
-
- HY-13727
-
|
BBR 2778 free base
|
Topoisomerase
|
Cancer
|
|
Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
|
-
- HY-13725
-
-
- HY-117515
-
|
|
Apoptosis
|
Cancer
|
|
YLT205 is an anticancer agent and induces cell apoptosis. YLT205 inhibits tumor growth in vivo and in vitro .
|
-
- HY-13656
-
|
KOS-1803
|
Microtubule/Tubulin
|
Cancer
|
|
Isofludelone (KOS-1803) is a potential microtubule stabilizer for the treatment of solid tumors. Isofludelone has antitumor activity .
|
-
- HY-122097
-
|
|
Others
|
Cancer
|
|
M7594_0037 is a potent inhibitor of human peptide deformylase (HsPDF) that has anti-tumor activity .
|
-
- HY-150266
-
|
|
Bcl-2 Family
|
Cancer
|
|
A-1293102 is a potent and selective BCL-XL inhibitor that kills BCL-XL-dependent tumor cells .
|
-
- HY-15449A
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(S)-Kaempferide (ZINC167686681) is a DNA methyltransferase (DNMT) inhibitor. (S)-Kaempferide can be used in tumor research .
|
-
- HY-163668
-
|
|
STING
|
Cancer
|
|
MK-2118 is a GMP-synthesized STING agonist with the potential to inhibit advanced/metastatic solid tumors or lymphomas. .
|
-
- HY-N8204
-
-
- HY-153661
-
-
- HY-162587
-
|
|
Topoisomerase
|
Cancer
|
|
Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors .
|
-
- HY-137724A
-
|
Cyclic-di-IMP disodium
|
STING
|
Cancer
|
|
C-di-IMP disodium is a STING agonist. C-di-IMP disodium can be used in tumor research .
|
-
- HY-18985
-
|
Phorbol dibutyrate; PDBu
|
PKC
|
Cancer
|
|
Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter .
|
-
- HY-N0140
-
|
Prunol; Urson; Malol
|
Autophagy
Endogenous Metabolite
|
Cancer
|
|
Ursolic acid (Prunol) is a natural pentacyclic triterpenoid carboxylic acid, exerts anti-tumor effects and is an effective compound for cancer prevention and therapy.
|
-
- HY-157562
-
|
|
Phospholipase
|
Cancer
|
|
DS68591889 is an inhibitor of phosphatidylserine synthase 1 (PTDSS1). DS68591889 can be used in tumor research .
|
-
- HY-N8091
-
|
|
Bacterial
|
Infection
Cancer
|
|
Lehmannine is a quinolizidine bioalkaloid isolated from S. alopecuroides L, has antibacterial, anti-inflammatory and anti-tumor activities .
|
-
- HY-13725A
-
-
- HY-U00155
-
|
NSC172112; NSC268497
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
|
-
- HY-122760
-
-
- HY-125670
-
-
- HY-N8131
-
|
|
Bacterial
|
Infection
Cancer
|
|
Pangelin is a coumarin that can be found in Ducrosia anethifolia. Pangelin exhibits anti-mycobacterial and anti-tumor activities .
|
-
- HY-N2242
-
|
|
Others
|
Cancer
|
|
Hosenkoside G, a baccharane glycoside isolated from the seeds of Impatiens Balsamina L., possesses anti-tumor activity .
|
-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-131257
-
|
|
Drug Metabolite
|
Others
Cancer
|
|
Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
|
-
- HY-N15380
-
|
|
PARP
Reactive Oxygen Species
Caspase
Apoptosis
Pyroptosis
|
Cancer
|
|
4,4′-Secalonic acid D (Compound 12) is a PARP1 inhibitor. 4,4′-Secalonic acid D induces the accumulation of ROS and DNA damage, activates the caspase-3/GSDME pathway, and triggers apoptosis and pyroptosis of tumor cells by inhibiting PARP1. 4,4′-Secalonic acid D has anti-tumor activity .
|
-
- HY-135217R
-
|
|
Apoptosis
|
Cancer
|
|
Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-W021377
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 2 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
|
-
- HY-148669A
-
|
JNJ-75276617 oxalate; Menin-MLL inhibitor 24 oxalate
|
Apoptosis
Histone Methyltransferase
FLT3
|
Cancer
|
|
Bleximenib (JNJ-75276617) oxalate is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia .
|
-
- HY-129762
-
|
NSC-102627
|
DNA/RNA Synthesis
|
Cancer
|
|
Yoshi-864 (NSC-102627) is an alkylsulfonate DNA crosslinker with anticancer activity. Yoshi-864 extends markedly the survival times of mice bearing L1210 leukemia or Ehrlich ascites carcinoma. Yoshi-864 also has a persistent reduction in ability to synthesize DNA in tumor cells from mice bearing the Ehrlich tumor .
|
-
- HY-123733A
-
|
RPS-001 TFA
|
PSMA
|
Cancer
|
|
MIP-1095 (RPS-001) TFA is a potent inhibitor of PSMA with good biodistribution and efficient targeting of tumor lesions. In applications, MIP-1095 TFA will be isotopically labeled ( 131I labeled) as an imaging probe to indicate tumor progression. And 131I-MIP-1095 showed higher renal uptake in mice .
|
-
- HY-159934
-
|
|
FAP
|
|
|
QI-18 is a fibroblast activation protein (FAP) inhibitor with the IC50 of 0.50 nM, which is a 6.5-fold increase in potency over that of UAMC-1110 (HY-100684，IC50 of 3.25 nM). QI-18 can be used to synthesize high tumor selectivity and high dose radiotracers for the diagnosis and treatment of tumors .
|
-
- HY-133779
-
|
|
Drug Metabolite
|
Others
Cancer
|
|
Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
|
-
- HY-W021377A
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 2 hydrochloride (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
|
-
- HY-116269
-
|
|
Ras
Apoptosis
PAK
ERK
|
Cancer
|
|
AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts .
|
-
- HY-N6790
-
-
- HY-151425
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo .
|
-
- HY-W021377B
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 4 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
|
-
- HY-156871
-
|
|
CaMK
|
Cancer
|
|
CAMK1D-IN-1 (compound I) is an inhibitor of CAMK1D, targeting cytotoxic T lymphocyte (CTL)-resistant tumor cells. CAMK1D impairs CTL-induced death receptor signaling and apoptosis by inhibiting caspases, making it a key and effective target for PD-L1-refractory tumors .
|
-
- HY-B1247
-
|
|
Endogenous Metabolite
|
Others
|
|
Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .
|
-
- HY-B1247A
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Protoporphyrin IX disodium is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX disodium also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX disodium is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX disodium causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX disodium is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .
|
-
- HY-147834
-
|
|
STING
|
Cancer
|
|
STING agonist-9 (Compound 45) is a potent STING agonist with an EC50 of 1.2 nM and 32.82 μM against h-STING and m-STING, respectively. STING agonist-9 shows antitumor activity .
|
-
- HY-N2604
-
-
- HY-149328
-
|
|
PROTACs
|
Cancer
|
|
phoBET1 is a photocaged-PROTAC. phoBET1 can achieve BRD4 degradation and effectively suppress tumor growth .
|
-
- HY-163093
-
|
|
Others
|
Cancer
|
|
ATX inhibitor 24 is a potent ATX inhibitor with IC50 of 7.51±0.72 nM that has anti-tumor effect .
|
-
- HY-161731
-
|
|
EGFR
|
Cancer
|
|
DS08701581 is an inhibitor of FER tyrosine kinase with IC50. DS08701581 has anti-tumor activity and oral activity .
|
-
- HY-17419A
-
|
|
Others
|
Cancer
|
|
(R)-Ifosfamide is a chemotherapeutic agent primarily used in the treatment of aggressive tumors such as rhabdomyosarcoma, exhibiting alkylating activity that interferes with DNA replication.
|
-
- HY-P10137
-
|
JR11
|
Somatostatin Receptor
|
Cancer
|
|
Satoreotide (JR11) is a SSTR2 antagonist. Satoreotide is usually conjugated with radiolabeled chelators used in neuroendocrine tumor imaing .
|
-
- HY-N14429
-
|
|
Bacterial
Fungal
|
Infection
|
|
Fredericamycin A has anti-Gram-positive bacterial and fungal activity, and shows strong anti-tumor effect in vivo and in vitro .
|
-
- HY-N15082
-
|
|
Bacterial
Fungal
|
Infection
Cancer
|
|
Hypnophilin has a variety of activities, including anti-Gram-positive bacteria, negative bacteria, yeast, mold and tumor activities .
|
-
- HY-121649
-
|
|
Topoisomerase
|
Cancer
|
|
AQ4 is a topoisomerase II inhibitor and DNA intercalator as a chemically stable cytotoxic agent in many human tumor lines .
|
-
- HY-N13259
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Fluopsin C is a copper-containing antibiotic with strong anti-Gram-positive and negative bacteria activity and anti-tumor activity .
|
-
- HY-N0183
-
|
Biochanin B; Flavosil; Formononetol
|
FGFR
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth .
|
-
- HY-N2570
-
|
|
Others
|
Cancer
|
|
Corytuberine is an aporphine alkaloid found in Dicranostigma leptopodum. Corytuberine displays cytotoxicity against SMMC-7721 tumor cells .
|
-
- HY-B0984A
-
-
- HY-N2542
-
-
- HY-P3025
-
-
- HY-N6075
-
|
Nuezhenide
|
Others
|
Cancer
|
|
Specneuzhenide (Nuezhenide) is a phenol glycoside isolated from Ligustrum sinense. Specneuzhenide (Nuezhenide) possesses anti-tumor activity .
|
-
- HY-163724
-
|
|
TrxR
Apoptosis
|
Cancer
|
|
LW-216 is a TrxR1 inhibitor that induces Apoptosis. LW-216 has anti-tumor activity .
|
-
- HY-16674
-
|
Docetaxel Impurity 1
|
Microtubule/Tubulin
|
Cancer
|
|
10-Oxo Docetaxel (Docetaxel Impurity 1) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
|
-
- HY-114824
-
|
|
Bacterial
|
Others
|
|
Streptovitacin A is a compound with antibacterial and antiproliferative activities isolated from microorganisms, which has inhibitory effects on a variety of bacteria and tumor cells.
|
-
- HY-111070
-
|
|
Drug Derivative
|
Cancer
|
|
Karavilagenin D, a cucurbitane-type triterpene isolated from Japanese bitter melon leaves, is a potential tumor-promoting inhibitor .
|
-
- HY-148482
-
|
|
Deubiquitinase
|
Cancer
|
|
USP7-IN-11 is a potent ubiquitin-specific protease 7 (USP7) (Deubiquitinase) inhibitor with an IC50 of 0.37 nM. USP7-IN-11 has anticancer effects (WO2022048498A1; Example 187) .
|
-
- HY-P10058
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
cpm-1285m is a cell-permeable mutated peptide analogue of cpm-1285 (Bcl-2 inhibitory peptide). cpm-1285m contains a single substitution of alanine for Leu-151, and exhibits a decrease in Bcl-2 binding affinity with a reduction in IC50 of ∼15-fold. cpm-1285m can be used as a control of cpm-1285 .
|
-
- HY-170996
-
|
|
ROR
|
Cancer
|
|
ROR1 ligand-1 (9-1) is a ligand for PROTACT ROR1 degrader-1 (HY-170995). ROR1 ligand-1 connects with VHL-type or CRBN ligand to design and synthesize the first selective and potent of ROR1 PROTACs .
|
-
- HY-135176
-
|
|
Endogenous Metabolite
|
Cancer
|
|
13-Dihydrocarminomycin (compound D788-12) is the major metabolite of the antitumor antibiotic Carminomycin (HY-B2171). 13-Dihydrocarminomycin has weak antitumor activity .
|
-
- HY-P5023
-
-
- HY-153546
-
|
|
STING
|
Cancer
|
|
STING agonist-31 is a STING agonist, with EC50 values of 0.24 and 39.51 μM for h-STING and m-STING. STING agonist-31 has antitumor efficiency .
|
-
- HY-N2322R
-
|
|
Others
|
Cancer
|
|
Khasianine (Standard) is the analytical standard of Khasianine. This product is intended for research and analytical applications. Khasianine is a steroidal glycoalkaloid which is obtained from black nightshade (Solanum Nigrum L.), which displays antitumor activity.
|
-
- HY-P4992
-
|
|
Somatostatin Receptor
|
Cancer
|
|
Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) is a somatostatin agonist that can be used in cancer research .
|
-
- HY-115729A
-
-
- HY-W478102
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-13 (Compound 15) is a CDK2 inhibitor with an IC50 of 12 µM. CDK2-IN-13 can be used in research of cancer .
|
-
- HY-P1344
-
|
|
DAPK
|
Cancer
|
|
DAPK Substrate Peptide is a synthetic peptide substrate for death associated protein kinase (DAPK), with a Km of 9 μM .
|
-
- HY-122568
-
|
|
STING
|
Cancer
|
|
STING agonist-15 (Compound STING agonist-C11) Is a STING agonist. STING agonist-15 can be used for research of cancer and immune response .
|
-
- HY-118263
-
|
PF-00299804 hydrate; PF-299804 hydrate
|
EGFR
|
Cancer
|
|
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC) .
|
-
- HY-P4978
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. CBP501 Affinity Peptide can be used in cancer research .
|
-
- HY-P99577
-
|
|
CD19
|
Cancer
|
|
Taplitumomab is an anti-CD19 monoclonal antibody. Taplitumomab paptox can be used in cancer research.
|
-
- HY-128758
-
|
|
DYRK
|
Cancer
|
|
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity .
|
-
- HY-158135
-
|
|
ADC Linker
|
Cancer
|
|
Val-Cit-PAB-DEA-COOH (compound 17) is an ADC linker that can be used in the synthesis of ADCs .
|
-
- HY-P5023A
-
-
- HY-160094
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
BCN-sulfonamide-PEG2-sulfonamide-N-bis ethanol (compound 71) is a Ligands for Target Protein for PROTAC that contains a sulfonamide linker to increase the solubility of the linker-conjugate. BCN-sulfonamide-PEG2-sulfonamide-N-bis ethanol can be used to synthesize PROTACs with antitumor activity .
|
-
- HY-P1344A
-
|
|
DAPK
|
Cancer
|
|
DAPK Substrate Peptide TFA is a synthetic peptide substrate for death associated protein kinase (DAPK), with a Km of 9 μM .
|
-
- HY-130797
-
-
- HY-128758A
-
|
|
DYRK
|
Cancer
|
|
DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity .
|
-
- HY-N2322
-
|
|
Others
|
Cancer
|
|
Khasianine is a steroidal glycoalkaloid which is obtained from black nightshade (Solanum Nigrum L.), which displays antitumor activity.
|
-
- HY-157447
-
|
|
Others
|
Cancer
|
|
CBR1-IN-4 (Compound 13p) is a human carbonyl reductase 1 (CBR1) inhibitor (IC50=0.09 μM). CBR1-IN-4 can be used in cancer research .
|
-
- HY-N7761
-
|
Tetrahydro tanshinone I
|
Others
|
Cancer
|
|
Trijuganone B (Tetrahydro tanshinone I) can be extracted from from the roots of Salvia miltiorrhiza f. alba. Trijuganone B inhibits the proliferation of leukemia cells .
|
-
- HY-P4979
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclin D1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research .
|
-
- HY-141601
-
|
ABBV-399
|
Antibody-Drug Conjugates (ADCs)
c-Met/HGFR
|
Cancer
|
|
Telisotuzumab vedotin (ABBV-399) is an antibody-drug conjugate (ADCs) targeting c-Met. Telisotuzumab vedotin consists of Monomethyl Auristatin E (MMAE), Telisotuzumab antibody and a cleavable mc-val-cit-PABC type linker. Telisotuzumab vedotin can be used to study non-small cell lung cancer expressing c-Met protein .
|
-
- HY-159489
-
|
|
SHP2
|
Cancer
|
|
SDUY038 is a SHP2 allosteric inhibitor, with an IC50 of 1.2 μM and KD of 0.29 μM, respectively. SDUY038 exhibits pan-antitumor activity (IC50 = 7-24 μM) by suppressing pERK expression. SDUY038 exhibits t1/2 of 3.95 h by oral administration .
|
-
- HY-153221
-
|
|
CDK
|
Cancer
|
|
QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC50 values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer .
|
-
- HY-156590
-
|
|
Raf
|
Cancer
|
|
B-Raf IN 16 (Compound I) is a BRAF inhibitors that belongs a cyclic iminopyrimidine derivative. B-Raf IN 16 can be used for cancer research .
|
-
- HY-115579
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
|
-
- HY-W158030
-
|
2GBI
|
NOD-like Receptor (NLR)
|
Cancer
|
|
2-Guanidinobezimidazole is a selective agonist of NLRP3, with a KD value of 1.29 μM to His-GFP-NLRP3. 2-Guanidinobezimidazole binds directly to the LRR domain of NLRP3, promoting inflammasome assembly and activation. 2-Guanidinobezimidazole promotes anti-tumor immunity, inhibits tumor growth, and overcome immune checkpoint blockade (ICB) resistance .
|
-
- HY-139643A
-
|
|
CXCR
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
CXCR7 antagonist-1 hydrochloride is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 hydrochloride is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases .
|
-
- HY-126850
-
|
|
EGFR
|
Cancer
|
|
4-Epidoxycycline is a liver metabolite of the antibiotic doxycycline (doxycycline, HY-N0565) and doesn't have antibiotic properties in mice. 4-Epidoxycycline’s ability to regulate HER2 gene expression in vitro and in live mouse models is similar to that of doxycycline, and it shows comparable high efficacy in tumor tissues, achieving over 95% tumor regression rates .
|
-
- HY-400685
-
|
|
Drug Intermediate
|
Cancer
|
|
SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-126193
-
|
|
NO Synthase
Apoptosis
Autophagy
Reactive Oxygen Species
|
Cancer
|
|
JS-K is a NO donor that reacts with glutathione to generate NO at physiological pH. JS-K induces reactive oxygen species (ROS) to mediate apoptosis. JS-K induces autophagy. JS-K inhibits invasion. JS-K has a broad spectrum anti-proliferative activity in cancer cells. JS-K reduces tumor volume and causes necrosis of implanted tumors in mice .
|
-
- HY-170554
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
ABBV-706 is a SEZ6 targeting ADC, which is composed of the Linker-Payload conjugation (HY-148820) and the Anti-SEZ6 Antibody (SC17) (HY-P991041). ABBV-706 exhibits high efficacy against small cell lung cancer (SCLC), neuroendocrine tumors (NENs) and central nervous system (CNS) tumors .
|
-
- HY-141677B
-
|
|
Histone Demethylase
|
Cancer
|
|
INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes .
|
-
- HY-N0093A
-
|
Cyclocytidine; Cyclo-CMP
|
DNA/RNA Synthesis
CMV
Autophagy
|
Cancer
|
|
Ancitabine is the precursor of the anticancer agent Cytarabine (HY-13605), which targets targets related to cell metabolism and proliferation. Ancitabine can inhibit tumor cell proliferation, interfere with the DNA synthesis process of tumor cells, and prevent cell division. Under alkaline pH conditions, Ancitabine can be quantitatively converted into Cytarabine and can be used in the study of cancers such as colorectal cancer .
|
-
- HY-170954
-
|
|
Apoptosis
c-Met/HGFR
TAM Receptor
|
Cancer
|
|
C-Met/Axl-IN-1 (Compound 22a) is an orally active and selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. C-Met/Axl-IN-1 can inhibit proliferation, induce cell cycle arrest and apoptosis of tumor cells. C-Met/Axl-IN-1 has strong anti-tumor activity .
|
-
- HY-P10759
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
- HY-139643
-
|
|
CXCR
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
CXCR7 antagonist-1 is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases .
|
-
- HY-N7271
-
|
|
RAD51
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
|
Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice .
|
-
- HY-N0093
-
|
Cyclocytidine hydrochloride; Cyclo-CMP hydrochloride; Cyclo-C
|
Autophagy
CMV
DNA/RNA Synthesis
|
Cancer
|
|
Ancitabine hydrochloride is the precursor of the anticancer agent Cytarabine (HY-13605), which targets targets related to cell metabolism and proliferation. Ancitabine hydrochloride can inhibit tumor cell proliferation, interfere with the DNA synthesis process of tumor cells, and prevent cell division. Under alkaline pH conditions, Ancitabine hydrochloride can be quantitatively converted into Cytarabine and can be used in the study of cancers such as colorectal cancer .
|
-
- HY-B1250R
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Acedoben (Standard) is the analytical standard of Acedoben. This product is intended for research and analytical applications. Acedoben is a biochemical agent. Acedoben and iron ions can construct a fast self-assembled coordination complex. The Fe-Ace coordination complex can not only serve as a carrier of tumor antigens, but also enhance antigen-specific anti-tumor immunity due to its inherent adjuvant properties .
|
-
- HY-158166
-
|
|
DNA-PK
|
Inflammation/Immunology
Cancer
|
|
DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies .
|
-
- HY-114169S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
WRG-28-d5 is the deuterium labeled WRG-28(HY-114169).WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic
|
-
- HY-173178
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes .
|
-
- HY-172201
-
|
|
NF-κB
Reactive Oxygen Species
Autophagy
Apoptosis
HIF/HIF Prolyl-Hydroxylase
Akt
STAT
PI3K
|
Inflammation/Immunology
Cancer
|
|
NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity .
|
-
- HY-169674
-
-
- HY-149694
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-12 (Compound 1a ) is the inhibitor of aurora kinase which is a key enzyme that is implicated in tumor growth .
|
-
- HY-144875
-
|
|
CDK
|
Cancer
|
|
CTX-712 is an orally effective CLK 2 inhibitor, with an IC50 of 1.4 nM, showing anti-tumor activity .
|
-
- HY-124584
-
|
|
Apoptosis
|
Cancer
|
|
Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis .
|
-
- HY-168633
-
|
|
Bombesin Receptor
PSMA
|
Cancer
|
|
PSMA/GRPR ligand 1 (compound 3 ) is a bispecific PSMA/GRPR ligand that shows dual targeting for PSMA(+) and GRPR(+) tumors .
|
-
- HY-124252
-
|
ETI
|
Lipoxygenase
|
Cancer
|
|
5,8,11-Eicosatriynoic acid (ETI) is a lipoxygenase inhibitor that blocks LTC4 biosynthesis in mast cell tumor cells .
|
-
- HY-W011845
-
|
7,12-DMBA; 7,12-Dimethylbenzanthracene
|
c-Myc
|
Cancer
|
|
DMBA has carcinogenic activity as a polycyclic aromatic hydrocarbon (PAH). DMBA is used to induce tumor formation in various rodent models .
|
-
- HY-14941
-
|
CP 4055
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Elacytarabine (CP 4055) is a lipid-conjugated derivative of the nucleoside analog cytarabine. Elacytarabine (CP 4055) is an antineoplastic agent with cytotoxicity in solid tumors.
|
-
- HY-111213
-
-
- HY-112181
-
KO-947
4 Publications Verification
|
ERK
|
Cancer
|
|
KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
|
-
- HY-13551
-
|
m-AMSA; acridinyl anisidide
|
Topoisomerase
Autophagy
|
Cancer
|
|
Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
|
-
- HY-130995
-
|
|
Antibiotic
ADC Cytotoxin
|
Infection
|
|
Agrochelin, an alkaloid cytotoxic antibiotic, is produced by the fermentation of a marine Agrobacterium sp. Agrochelin has cytotoxic activity in tumor cell lines .
|
-
- HY-N0834
-
|
SB365; Hederacolchiside A
|
Apoptosis
|
Cancer
|
|
Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla chinensis, is an anti-tumor agent .
|
-
- HY-151590
-
|
|
HDAC
|
Cancer
|
|
DKFZ-748 is a selective HDAC10 inhibitor (pIC50=7.66), and shows anti-tumor activity .
|
-
- HY-132234
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression .
|
-
- HY-P0073
-
|
Met-Enkephalin; Methionine enkephalin; Metenkefalin
|
Opioid Receptor
|
Neurological Disease
Cancer
|
|
Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
|
-
- HY-13727B
-
|
BBR 2778 hydrochloride
|
Topoisomerase
|
Cancer
|
|
Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity .
|
-
- HY-168374
-
-
- HY-111786
-
-
- HY-W698254
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Fluopsin F is an antibiotic containing metallic iron with strong anti-Gram-positive and negative bacteria activity and anti-tumor activity .
|
-
- HY-N8449
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Ailanthoidol is a natural occurring neolignan, with anti-inflammatory and antitumor activities. Ailanthoidol has chemopreventive activity against tumor promotion .
|
-
- HY-A0128
-
-
- HY-13551A
-
|
m-AMSA hydrochloride; acridinyl anisidide hydrochloride
|
Topoisomerase
Autophagy
|
Cancer
|
|
Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
|
-
- HY-A0128A
-
-
- HY-13648
-
|
CMT-3; COL-3
|
MMP
|
Cancer
|
|
Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
|
-
- HY-N14859
-
-
- HY-162101
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase inhibitor 3 (compound 9) is a potent Topoisomerase inhibitor. Topoisomerase inhibitor 3 shows antiproliferative and anti-tumor activity .
|
-
- HY-N0400
-
-
- HY-129125
-
|
|
STAT
|
Cancer
|
|
YMU1 is a selective inhibitor of human thymidylate kinase (hTMPK) with an IC50 of 610 nM. YMU1 inhibits tumor proliferation .
|
-
- HY-105061
-
|
Ro 7-0582; SR 1354
|
Bacterial
Parasite
|
Infection
Cancer
|
|
Misonidazole (Ro 7-0582; SR 1354) is a hypoxic tumor cell radiosensitizer . Misonidazole also has antimicrobial effects .
|
-
- HY-13730
-
|
N-Methylmitomycin C; NSC-56410; U-14743
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Porfiromycin (N-Methylmitomycin C) is a bioreductive alkylating agent that preferentially kill hypoxic tumor cells relative to other aerobic counterparts .
|
-
- HY-W520748
-
|
|
FKBP
|
Cancer
|
|
MJC13 is an FKBP52-targeted agent with anti-tumor activity that can be used in prostate cancer research .
|
-
- HY-W008253
-
-
- HY-161853
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
TX-2552 is an orally active tyrosine DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 value of 0.62 μM. TX-2552 can enhance the clastogenic activity of Topotecan (HY-13768) in mouse bone marrow cells, as well as the anti-tumor effect of Topotecan (HY-13768) in Krebs-2 ascites tumor mice .
|
-
- HY-162867
-
|
|
Ferroptosis
|
Cancer
|
Photosensitizer-5 is a photosensitizer. Photosensitizer-5 has cytotoxicity against HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. Photosensitizer-5 can lead to lipid peroxidation and induces cell death through an iron-independent ferroptosis-like pathway. Photosensitizer-5 shows anti-tumor activity in HeLa tumor-bearing mice .
|
-
- HY-107458
-
|
|
c-Kit
|
Cancer
|
|
AP23848 is an ATP-dependent kinase inhibitor that effectively and selectively targets the Kit activation loop mutation both in vitro and in vivo, showing anti-tumor activity. AP23848 can inhibit the phosphorylation of the activated Kit mutation and tumor growth in mice, making it suitable for targeting diseases with the D816V mutation, such as systemic mastocytosis (SM) and acute myeloid leukemia (AML) research .
|
-
- HY-100663
-
|
|
EGFR
|
Others
Cancer
|
|
Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
|
-
- HY-156112
-
|
|
Ser/Thr Protease
|
Cancer
|
|
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
|
-
- HY-N0591
-
-
- HY-50895S1
-
|
ZD1839-d6
|
EGFR
Autophagy
|
Cancer
|
|
Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
|
-
- HY-143432A
-
|
|
CDK
|
Cancer
|
|
(S)-Cdc7-IN-18 is a potent inhibitor of CDC7. Overexpression of huCdc7 promotes overactivation of MCM2, an important marker of tumor cells, and thus promotes aberrant proliferation of tumor cells. (S)-Cdc7-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2020239107A1, compound 1-1) .
|
-
- HY-10330S
-
|
|
Isotope-Labeled Compounds
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
Toceranib-d8 is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1][2].
|
-
- HY-172155
-
|
|
MEK
|
Cancer
|
|
MEK1-IN-1 (Compound M15) is a MEK1 inhibitor with an IC50 of 10.29 nM. MEK1-IN-1 can inhibit the proliferation and migration, induce apoptosis of tumor cells. MEK1-IN-1 has good liver microsomal stability. MEK1-IN-1 can be used for the research of solid tumors .
|
-
- HY-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-171183
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
AB8939 is an effective small moleculeMicrotubule/Tubulin polymerization inhibitor with anti-tumor activity (it inhibits tumor cell proliferation with an IC50 of less than 10 nM). AB8939 can effectively evade resistance mechanisms mediated by things like P-glycoprotein and myeloperoxidase. AB8939 can induce G2/M phase cell cycle arrest and apoptosis in cells .
|
-
- HY-42487B
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
(R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer .
|
-
- HY-170971
-
|
|
Apoptosis
Src
|
Cancer
|
|
Src Inhibitor 4 (Compound 18) is a derivative of KX-01 and an Src inhibitor. Src Inhibitor 4 can inhibit tumor cells, disrupt microtubules, and induce cell cycle arrest, apoptosis, and immunogenic cell death. After the introduction of phenolic or aniline functionality, Src Inhibitor 4 can serve as a payload attachment site for antibody-drug conjugates and has anti-tumor activity .
|
-
- HY-42487A
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
(rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer .
|
-
- HY-164427
-
|
|
SHP2
ERK
|
Cancer
|
|
SHP2-IN-31 is a SHP2 inhibitor, with IC50s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models .
|
-
- HY-B1247R
-
|
|
Endogenous Metabolite
|
Others
|
|
Protoporphyrin IX (Standard) is the analytical standard of Protoporphyrin IX. This product is intended for research and analytical applications. Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .
|
-
- HY-170935
-
|
|
SRPK
|
Cancer
|
|
SRSF1-IN-1 (STP2) is a SRSF1 inhibitor that regulates the splicing of Bcl-x precursor mRNA by inhibiting SRSF1 expression. SRSF1-IN-1 exhibits anti-tumor activity both in vitro and in vivo, with IC50 values ranging from 0.33 to 6.93 μM against tumor cells such as HepG2 and MCF7. In mice, SRSF1-IN-1 demonstrates good safety, as intraperitoneal injection at 1 g/kg does not cause death or pathological damage. SRSF1-IN-1 holds promising potential for research in the field of anti-tumor therapy .
|
-
- HY-P99682
-
|
hLIV22
|
ADC Antibody
|
Cancer
|
|
Ladiratuzumab (hLIV22) is a humanized monoclonal antibody against zinc transporter LIV-1/ZIP6. Ladiratuzumab is conjugated to MMAE (HY-15162) via a cleavable dipeptide linker to synthesize an antibody-drug conjugate (ADC) Ladiratuzumab vedotin (HY-P99683). Ladiratuzumab vedotin selectively targets LIV-1 protein overexpressed on the surface of tumor cells, enters cells through antibody-mediated receptor endocytosis, releases MMAE to inhibit microtubule polymerization, and kills adjacent tumor cells with a bystander effect. Ladiratuzumab can be used in the study of solid tumors such as metastatic triple-negative breast cancer (mTNBC) .
|
-
- HY-153039
-
|
|
Drug Intermediate
|
Others
Cancer
|
|
Anhydroleucovorin is a form of tetrahydrofolate and is a substrate for cyclohydrolase, which converts it to 10-formyltetrahydrofolate. Anhydroleucovorin can be used for research in the field of tumors .
|
-
- HY-160160
-
|
|
PPAR
|
Cancer
|
|
BAY-5516 is a inverse-agonist o PPARG, with the IC50 value of 6.1±3.6 nM that has anti-tumor effect .
|
-
- HY-111634
-
|
|
Constitutive Androstane Receptor
|
Cancer
|
|
Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats .
|
-
- HY-47979A
-
|
|
FAP
|
Others
Cancer
|
|
FAP-IN-2 TFA is a 99mTc-labeled isonitrile-containing FAP inhibitor derivative that can be used for tumor imaging .
|
-
- HY-101570
-
|
Peposertib; M3814
|
DNA-PK
|
Cancer
|
|
Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity .
|
-
- HY-153364
-
|
|
PPAR
|
Cancer
|
|
FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models .
|
-
- HY-10822A
-
|
BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
|
Thymidylate Synthase
|
Cancer
|
|
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .
|
-
- HY-124624
-
-
- HY-N4189
-
|
|
Others
|
Cancer
|
|
Isocucurbitacin B is a potent cytotoxic compound isolated from Helicteres rswa L. (Sterculiaceae). Isocucurbitacin B possesses anti-tumor acticity .
|
-
- HY-N14840
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
1-Hydroxysulfurmycin A is an anthracycline antibiotic. 1-Hydroxysulfurmycin A has anti-Gram-positive bacteria and anti-tumor cell activity .
|
-
- HY-169023
-
|
|
Apoptosis
|
Cancer
|
|
Antiangiogenic agent 6 (Pt-1) can inhibit angiogenesis. Antiangiogenic agent 6 can induce necroptosis in tumor cells .
|
-
- HY-126330
-
|
AVS100
|
HDAC
|
Cancer
|
|
SS-208 is a selective HDAC6 inhibitor, with an IC50 of 12 nM. SS-208 possesses anti-tumor activity in melanoma .
|
-
- HY-P1009
-
|
|
Caspase
|
Cancer
|
|
Z-YVAD-FMK is a cell-permeable caspase-1 and -4 inhibitor with anti-inflammatory and anti-tumor activities .
|
-
- HY-114535
-
|
|
EGFR
|
Cancer
|
|
Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities .
|
-
- HY-108491
-
|
|
SphK
|
Cancer
|
|
N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines .
|
-
- HY-B1436
-
|
|
STAT
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity. Nifuroxazide is an orally active nitrofuran antibiotic.
|
-
- HY-N4139
-
|
|
Others
|
Cancer
|
|
Protohypericin is a naturally occurring naphthodianthrone derived from plant Hypericum perforatum. Radioiodinated protohypericin is used in Tumor necrosis targeted radiotherapy .
|
-
- HY-N14849
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
1-Hydroxyauramycin A is an anthracycline antibiotic. 1-Hydroxyauramycin A has anti-Gram-positive bacteria and anti-tumor cell activity .
|
-
- HY-122997
-
|
|
Others
|
Others
|
|
Acetylaleuritolic acid is a triterpenoid isolated from Jatropha curcas that exhibits tumor suppressive properties against the P-388 lymphocytic leukemia test system.
|
-
- HY-132922
-
|
APG-5918
|
Histone Methyltransferase
|
Cancer
|
|
EEDi-5273 is an exceptionally potent and orally efficacious EED inhibitor (IC50 = 0.2 nM) capable of achieving complete and persistent tumor regression.
|
-
- HY-18310
-
|
|
PI3K
|
Cancer
|
|
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth .
|
-
- HY-145668
-
|
|
Others
|
Cancer
|
|
Cyclopentenyl uracil, a non-cytotoxic inhibitor of uridine kinase, effectively blocks the salvage of circulating uridine by host and tumor tissues in the intact mouse .
|
-
- HY-N8207
-
|
|
Apoptosis
MicroRNA
|
Cancer
|
|
Gypenoside LI, a gypenoside monomer, possesses anti-tumor activity. Gypenoside LI induces cell apoptosis, cell cycle and migration .
|
-
- HY-147317
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity .
|
-
- HY-110203
-
|
TNF-α Antagonist III
|
TNF Receptor
|
Cancer
|
|
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
|
-
- HY-N15106
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
11-Deoxy-13-deoxodaunorubicin is an anthracycline antibiotic with anti-Gram-positive bacteria, negative bacteria and tumor activity .
|
-
- HY-14808
-
|
ST1926
|
Apoptosis
|
Cancer
|
|
Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
|
-
- HY-102001
-
|
|
ADC Cytotoxin
|
Cancer
|
|
Tomaymycin DM, a DNA alkylator, is a derivative of Tomaymycin, it is a PBD dimer, which is attached to tumor targeting antibodies to create antibody-drug conjugates (ADCs).
|
-
- HY-163644
-
|
|
YAP
|
Cancer
|
|
VT-105 is a potent and selective TEAD autopalmitoylation inhibitor that inhibits proliferation and tumor growth in NF2-deficient mesothelioma.
|
-
- HY-105416
-
|
UCN-1028C
|
Antibiotic
PKC
Apoptosis
|
Metabolic Disease
Cancer
|
|
Calphostin C is a highly selective PKC inhibitor (IC50=0.05 μM) and tumor apoptosis inducer. Calphostin C competitively binds to PKC and inhibits PKC-mediated phosphorylation signal transduction. Calphostin C restores Na+/K+ ATPase activity in the sciatic nerve of diabetic mice and improves neuropathy. Calphostin C can be used in the study of anti-tumor and diabetic complications .
|
-
- HY-A0084A
-
|
Procaine amide; SP 100
|
DNA Methyltransferase
Potassium Channel
|
Cardiovascular Disease
Cancer
|
|
Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research .
|
-
- HY-P991180
-
|
|
TNF Receptor
|
Cancer
|
|
TRX-518 is a humanized agonist antibody targeting glucocorticoid-induced tumor necrosis factor receptor (GITR). TRX-518 specifically targets GITR⁺ Tregs and CD45RA⁻Foxp3⁺ effector Tregs (eTregs) among regulatory T cells (Tregs), reducing the number of Tregs in circulation and within tumors. TRX-518 is promising for research of cancers .
|
-
- HY-121410
-
|
|
Bacterial
Apoptosis
Parasite
NF-κB
Antibiotic
|
Infection
Cancer
|
|
Narasin is a cationic ionophore antibiotic and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin has antimicrobial, antiviral anticancer activity. Narasin inhibits tumor metastasis and growth of ERα‑positive breast cancer cells by inactivation of the TGF-β/SMAD3 and IL‑6/STAT3 signaling pathways .
|
-
- HY-170490
-
|
|
Photosensitizer
Apoptosis
|
Cancer
|
|
TTQ-SA is a near-infrared (NIR) spiro-AIEgen (aggregation-induced emission luminogen), that converts near-infrared light (NIR) into thermal energy, causing thermal damage and death of tumor cells. TTQ-SA exhibits cellular uptake and targeting ability in cancer cell MF-7. TTQ-SA silences the expression of survivin gene with combination of DNAzyme, enhances the sensitivity of tumor cells to photothermal therapy .
|
-
- HY-152963
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Inflammation/Immunology
Cancer
|
|
Tisotumab vedotin is an antibody drug conjugate (ADC) targeting tissue factor (TF), formed by covalently linking a fully human monoclonal antibody (TF-011) against TF with the microtubule disruptor Monomethyll Auristatin E (MMAE) (HY-15162). Tisotumab vedotin has immunomodulatory and anti-tumor activities, and can be used in the study of advanced or metastatic solid tumors such as cervical cancer .
|
-
- HY-149830
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-L1-IN-2 is a potential tumor immunological agent by inhibiting PD-L1. PD-L1-IN-2 is a Naamidine J derivative and exerts antitumor effects in vivo by reducing PD-L1 expression and enhancing tumor-infiltrating T-cell immunity. PD-L1-IN-2 is used for colorectal cancer research .
|
-
- HY-A0084
-
|
Procaine amide hydrochloride; SP 100 hydrochloride
|
DNA Methyltransferase
Potassium Channel
|
Cancer
|
|
Procainamide hydrochloride (Procaine amide hydrochloride) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide hydrochloride induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide hydrochloride relaxes airway smooth muscle by activating potassium channels. Procainamide hydrochloride can be used in cancer and arrhythmia research .
|
-
- HY-161886
-
|
|
SWI/SNF Complex
Epigenetic Reader Domain
|
Cancer
|
|
SMARCA2-IN-7 (compound 12), a dual inhibitor of BRM and BRG1 (IC50 < 0.005 for both), has an anti-tumor proliferation effect that inhibits BRG1-deleted SKMEL5 tumor proliferation with a cell proliferation activity AAC50 of 13 nM in SKMEL5. The cell proliferation activity AAC50 of KRT880 in H1299 cells was 42 nM .
|
-
- HY-P990710
-
|
AFM13
|
TNF Receptor
|
Cancer
|
|
Acimtamig (AFM13) is a CD30/CD16A bispecific innate cell engager. Acimtamig binds to the CD16A expressed on natural killer (NK) cells and binds to CD30 on CD30-expressing tumor cells, thereby selectively cross-linking tumor and NK cells. Acimtamig can be used for the study of eripheral T-cell lymphoma (PTCL) .
|
-
- HY-B1610R
-
|
|
Bacterial
Endogenous Metabolite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Sodium citrate (dihydrate) (Standard) is the analytical standard of Sodium citrate (dihydrate). This product is intended for research and analytical applications. Sodium citrate dehydrate (Trisodium citrate dihydrate) is a natural product with oral activity that can be found in citrus fruits. Sodium citrate dehydrate can inhibit the proliferation of tumor cells and induce apoptosis. Sodium citrate dehydrate has antibacterial, anti-tumor and antioxidant activities. Sodium citrate dehydrate can be prepared as a cosolvent or buffer .
|
-
- HY-156773
-
|
|
Apoptosis
METTL3
|
Cancer
|
|
STM3006 is a highly potent, selective, and orally active inhibitor of METTL3 (IC50: 5 nM). STM3006 can reduce the m6A level, promote the formation of dsRNA, trigger a cell-intrinsic interferon response, and enhance the killing effect of T cells on tumors. STM3006 has anti-tumor activity, and its combination with anti-PD-1 immunotherapy yields better results .
|
-
- HY-N6004
-
|
Shikalkin
|
Others
|
Cancer
|
|
(Rac)-Shikonin (Shikonin) possesses anti-tumor activity. (Rac)-Shikonin (Shikonin) circumvents cancer agent resistance by induction of a necroptotic death .
|
-
- HY-N3065
-
|
|
Others
|
Cancer
|
|
Pierreione B is a pyranoisoflavone, that can be isolated from the leaves and twigs of Antheroporum pierrei. Pierreione B demonstrates solid tumor selectivity with minimal cytotoxicity .
|
-
- HY-160070
-
|
|
HIV
|
Cancer
|
|
Phorbol-12,13-didecanoate is an anti-viral TPA compound and a tumor promoter. It can cause changes in actin-containing structures [1] .
|
-
- HY-N4109
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity .
|
-
- HY-138134
-
-
- HY-P6083
-
|
|
Biochemical Assay Reagents
|
Others
Cancer
|
|
RTSPSSR is synthesized peptide, which binds specifically to claudin-1 and visulizes the CRC tumor in mice, through near-infrared fluorescence imaging .
|
-
- HY-101120
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model .
|
-
- HY-139719
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
IMD-biphenylC is a novel imidazoquinolinone-NF-κB immunomodulator dimer that inhibits tumor proliferation while induces low systemic inflammation and reduces adjuvant toxicity.
|
-
- HY-50909
-
|
KRX-0401; NSC 639966; D21266
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
|
-
- HY-13468
-
KW-2478
3 Publications Verification
|
HSP
|
Cancer
|
|
KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
|
-
- HY-145726
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
ISIS 104838 is an antisense oligonucleotide agent that reduces the production of tumor necrosis factor (TNF-alpha), a substance that contributes to joint pain and swelling in rheumatoid arthritis.
|
-
- HY-163841
-
|
|
Others
|
Cancer
|
|
Antitumor agent-181 (HJ1) is an anticancer agent. Antitumor agent-181 inhibits tumor cell growth in vivo and in vitro .
|
-
- HY-N2997
-
|
|
Others
|
Cancer
|
|
Ganoderic acid LM2 is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid LM2 possesses potential anti-tumor activity .
|
-
- HY-171218
-
|
|
Src
|
Cancer
|
|
CGP062464 is an inhibitor of the tyrosine kinase c-Src (IC50: < 50 nM). CGP062464 can be used for research of osteoporosis and tumor-induced hypercalcemia .
|
-
- HY-157302
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-21 (compound 54) is a c-met inhibitor with an IC50 value of 0.45? nM, and shows anti-tumor efficacy in vivo .
|
-
- HY-N0669
-
-
- HY-156673
-
|
|
c-Myc
|
Cancer
|
|
m-Se3 is a potent and selective c-MYC transcription inhibitor that can inhibit tumor growth and has anti-cancer activity .
|
-
- HY-N0156R
-
|
|
MAP3K
Autophagy
Endogenous Metabolite
HIV
|
Cancer
|
|
Oleanolic acid (Standard) is the analytical standard of Oleanolic acid. This product is intended for research and analytical applications. Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
|
-
- HY-147894
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
PCAF-IN-1 is a highly selective PCAF inhibitor. PCAF-IN-1 is a antitumor agents, which can be used in tumor research research .
|
-
- HY-U00095
-
|
NCI 329680; ZINC01574758
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
|
-
- HY-115453
-
|
|
Sirtuin
Autophagy
|
Cancer
|
|
UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM .
|
-
- HY-162976
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-35 (compound 72) is a KRAS inhibitor, with IC50 of 2 nM. KRAS inhibitor-35 can be used in tumor research .
|
-
- HY-137301
-
|
|
Drug Metabolite
|
Cancer
|
|
Mycophenolic acid glucuronide is a metabolite of the immunosuppressant mycophenolic acid (MPA). Mycophenolic acid glucuronide shows anti-tumor activity and can be used in adenocarcinoma research .
|
-
- HY-139718
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
IMD-biphenylB is a potent imidazoquinolinone-NF-κB immunomodulator dimer that inhibits tumor proliferation while induces low systemic inflammation and reduces adjuvant toxicity.
|
-
- HY-17419R
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Ifosfamide (Standard) is the analytical standard of Ifosfamide. This product is intended for research and analytical applications. Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.
|
-
- HY-129407A
-
|
|
Ser/Thr Protease
Apoptosis
|
Cancer
|
|
AAF-CMK is a TPPII (tripeptidylpeptidase II) inhibitor, shows anti-tumor activity and induces apoptosis. AAF-CMK can be used in leukemia research .
|
-
- HY-132980
-
|
KRAS G12C inhibitor 19
|
Ras
|
Cancer
|
|
Olomorasib is a potent inhibitor of KRAS G12C. Olomorasib significantly inhibits tumor growth (extracted from patent WO2021118877A1) .
|
-
- HY-145726A
-
|
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
ISIS 104838 sodium is an antisense oligonucleotide agent that reduces the production of tumor necrosis factor (TNF-alpha), a substance that contributes to joint pain and swelling in rheumatoid arthritis.
|
-
- HY-P1727
-
|
|
YAP
|
Cancer
|
|
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-N2632
-
|
|
Apoptosis
|
Cancer
|
|
Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation .
|
-
- HY-N0429
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Diosbulbin B is a diterpene lactone isolated from D. bulbifera L., with anti-tumor activity. Diosbulbin B can induce liver injury .
|
-
- HY-W754718
-
|
|
Others
|
Cancer
|
|
Azepinomycin is found in the strain of Streptomyces toyokaensis MF71803. Azepinomycin can inhibit guanine deaminase (IC50 of 4.9 μM) and tumor cell .
|
-
- HY-160419
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-8 is a Mps1 inhibitor. Mps1-IN-8 can be used in the study of various tumors .
|
-
- HY-122486
-
|
Lophirochalcone
|
EBV
|
Cancer
|
|
Lophirachalcone (Lophirochalcone) is an inhibitor of the activation of EB virus (EBV) induced by tumor promoter teleocidin B-4. Lophirachalcone has antitumor activity .
|
-
- HY-136718
-
|
|
Apoptosis
|
Cancer
|
|
CLEFMA is a curcuminoid with antitumor activity. CLEFMA inhibits tumor growth is associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects .
|
-
- HY-153110A
-
|
|
EGFR
IRAK
Btk
|
Cancer
|
|
Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM .
|
-
- HY-153110
-
|
|
EGFR
IRAK
Btk
|
Cancer
|
|
Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM .
|
-
- HY-148669B
-
|
(S)-JNJ-75276617 oxalate; (S)-Menin-MLL inhibitor 24 oxalate
|
Apoptosis
Histone Methyltransferase
FLT3
|
Cancer
|
|
(S)-Bleximenib (oxalate) is a S-Enantiomer of Bleximenib oxalate (HY-148669A). Bleximenib (JNJ-75276617) oxalate is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia .
|
-
- HY-156649
-
|
CR6086
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
|
Vorbipiprant (CR6086) is an EP4 receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a potential immune checkpoint inhibitor, to turn cold tumors into hot tumors. Vorbipiprant also antagonizes PGE2-stimulated cAMP production (IC50=22 nM). Vorbipiprant exhibit striking DMARD effects in rodents, and anti-inflammatory activity to inhibt immune-mediated inflammatory diseases .
|
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
HSP
|
Cancer
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-P2088
-
|
Des-N-tetramethyltriostin A
|
Antibiotic
|
Cancer
|
|
TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
|
-
- HY-138071
-
|
8αTGH
|
STAT
Pyroptosis
Apoptosis
Reactive Oxygen Species
c-Myc
Bcl-2 Family
TrxR
|
Cancer
|
|
8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo .
|
-
- HY-155062
-
|
|
Mitochondrial Metabolism
Reactive Oxygen Species
β-catenin
Fluorescent Dye
PPAR
|
Cancer
|
|
IR-251 is a mitochondrion-targeting NIR fluorescent probe. IR-251 targets mitochondria via OATPs and causes mitochondrial damage in tumor cells. IR-251 IR-251 induced ROS overproduction by inhibiting PPARγ, and then inhibiting the β-catenin signaling pathway and downstream protein molecules related to the cell cycle and metastasis. IR-251 inhibits tumor proliferation and metastasis .
|
-
- HY-156737
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-49 (compound 12d) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-49 bound to colchicine site on tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-49 induces cell cycle arrest at G2/M phase and apoptosis. Tubulin polymerization-IN-49 has anticancer active and prevents tumor generation, inhibits tumor proliferation and angiogenesis .
|
-
- HY-121372
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
|
-
- HY-13735H
-
|
Acriquine acetate
|
Parasite
Sodium Channel
DNA Stain
Apoptosis
|
Cancer
|
|
Quinacrine (Acriquine) acetate is a small molecule modulator of the cGAS-STING-TBK1 signaling pathway, possessing immune stimulatory activity. Quinacrine acetate has been explored for its potential therapeutic applications in enhancing anti-tumor immunity. Quinacrine acetate can improve the effectiveness of cancer immunotherapies by addressing the poor immunogenicity of various tumors. Quinacrine acetate also presents a promising strategy for overcoming the limitations associated with immune checkpoint inhibitors in cancer treatment.
|
-
- HY-W019815
-
|
ENU; N-Nitroso-N-ethylurea
|
DNA/RNA Synthesis
|
Neurological Disease
Cancer
|
|
N-Ethyl-N-nitrosourea (ENU) is a DNA alkylating agent. N-Ethyl-N-nitrosourea induces leukemia by alkylating nucleobases, disrupting DNA, and resulting in bone marrow suppression and the formation of leukemic cells. N-Ethyl-N-nitrosourea is teratogenic in vivo, inducing tumor formation and paw malformations in pregnant rats. N-Ethyl-N-nitrosourea cause central nervous system (CNS) tumors and genetic disorders .
|
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-13016A
-
|
XL184 hydrochloride; BMS-907351 hydrochloride
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-164546
-
|
|
STAT
Apoptosis
|
Cancer
|
WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
|
-
- HY-N15066
-
-
- HY-P99707
-
|
HH1
|
Apoptosis
|
Cancer
|
|
Lilotomab (HH1) is a murine anti-CD37 monoclonal antibody. Lilotomab reduces clonogenic survival. Lilotomab shows anti-tumor activity .
|
-
- HY-123360
-
|
BIBW22BS
|
Others
|
Cancer
|
|
BIBW 22 (BIBW22BS) is a dipyridamole analogue. BIBW 22 is a potent bifunctional modulator that affects p-glycoprotein and nucleoside transport in tumor cells .
|
-
- HY-16516
-
|
|
Others
|
Cancer
|
|
Vitamin CK3 is the combination of Vitamin C and vitamin K3 (100:1 ratio) and has been shown to inhibit tumor growth and lung metastasis.
|
-
- HY-U00337A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Datelliptium chloride hydrochloride is a DNA-intercalating agent derived from Ellipticine (HY-15753). Datelliptium chloride hydrochloride is effective in vivo against a variety of murine solid tumors .
|
-
- HY-N0714
-
|
|
NF-κB
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Berbamine is a natural compound extracted from traditional Chinese medicine Phellodendron amurense Rupr. with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
|
-
- HY-W100403
-
|
Choline p-toluenesulfonate
|
Phospholipase
|
Cancer
|
|
Choline tosylate is a nucleophilic compound that inhibits phospholipase A2 and phospholipase C. Choline tosylate inhibits tumor growth in mice by inhibiting the formation of diacylglycerol (DAG) .
|
-
- HY-130996
-
|
|
ADC Cytotoxin
|
Cancer
|
|
Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines .
|
-
- HY-N9350
-
|
|
Others
|
Cancer
|
|
Ganoderic acid ε is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid ε exhibits an ED50 of 12.2 μg/mL in Meth-A tumor cells
|
-
- HY-N15035
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Bis(N-methylthioformohydroxamate)nickel (II) is an antibiotic containing metallic nickel with strong anti-Gram-positive and negative bacteria activity and anti-tumor activity .
|
-
- HY-159154
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
PSS-II promotes the production of ROS under light, thereby killing cancer cells and inhibiting tumor growth without damaging important organs of the body .
|
-
- HY-117260
-
-
- HY-N14893
-
|
|
Others
|
Cancer
|
|
Cetoniacytone B can inhibit the growth of HEPG2 and MCF7 human tumor cell lines, with GI50 values of 4.4 μM .
|
-
- HY-143655
-
|
|
BMI1
Autophagy
|
Cancer
|
|
QW24 exerts potent anti-tumor activity by down-regulating BMI-1 and is used as an effective therapeutic agent for clinical colorectal cancer research.
|
-
- HY-151620
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-80 (compound 11) is an orally active and potent antitumor agent. Antitumor agent-80 induces apoptosis in tumor cells .
|
-
- HY-156602
-
|
OKI-179
|
HDAC
|
Cancer
|
|
Bocodepsin (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin can be used for suppression on solid tumor and hematologic malignancies .
|
-
- HY-112225
-
-
- HY-B1436S
-
|
|
STAT
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Nifuroxazide-d4 is the deuterium labeled Nifuroxazide. Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
|
-
- HY-N6653
-
-
- HY-157215
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-66 (compound 2F) is a selective HDAC inhibitor and Pomalidomide (HY-10984) derivative that potently inhibits hematological tumor cells .
|
-
- HY-P99026
-
|
TJ011133; TJC4
|
CD47
|
Cancer
|
|
Lemzoparlimab (TJ011133; TJC4) is a humanized anti-CD47 IgG4 antibody. Lemzoparlimab has a strong anti-tumor activity .
|
-
- HY-47979
-
|
|
FAP
|
Others
Cancer
|
|
FAP-IN-2 is a derivative of 99mTc-labeled isonitrile-containing fibroblast activation protein (FAPI) inhibitor, that can be used for tumor imaging .
|
-
- HY-12444
-
|
FAK Inhibitor 14
|
FAK
|
Cancer
|
|
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
|
-
- HY-119589
-
|
Dactylarin
|
Antibiotic
|
Others
|
|
Altersolanol B (Dactylarin), a compound isolated from fungi, is structurally related to antibiotics and has been shown to induce ATP catabolism in Ehrlich ascites tumor cells.
|
-
- HY-141896
-
|
|
RET
|
Cancer
|
|
RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
|
-
- HY-N14603
-
|
|
Fungal
|
Infection
|
|
Chandrananimycin A has anti-mucor activity, as well as anti-tumor cell activity such as CCL HT29, MFXF 529L, MACL McF-7 .
|
-
- HY-137573
-
|
CC-90010
|
Epigenetic Reader Domain
|
Cancer
|
|
CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors .
|
-
- HY-120864
-
|
|
Wnt
|
Cancer
|
|
SEN461 is a potent and orally active Wnt pathway inhibitor. SEN461 shows effective anti-tumor activity and can be used for GBM research .
|
-
- HY-162974
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-34 (compound 27) is a KRAS inhibitor, with IC50 of 6.4 nM. KRAS inhibitor-34 can be used in tumor research .
|
-
- HY-138269A
-
|
CHX-A''-DTPA-NCS hydrochloride
|
Biochemical Assay Reagents
|
Others
|
|
Barzuxetan (hydrochloride)is a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DPTA derivative used for tumor pre-targeting. Barzuxetan (hydrochloride) can be used for conjugation of peptides and radionuclides.
|
-
- HY-N2104
-
|
|
Others
|
Cancer
|
|
Daurinoline is an alkaloid that can be isolated from the roots of Menispermum dauricum. Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC research .
|
-
- HY-107720
-
|
|
NO Synthase
|
Cancer
|
|
ARL-17477 is a dual inhibitor of NOS1and the autophagy-lysosomal system with anticancer activity and can inhibit tumor growth in KRAS-mutated cancers .
|
-
- HY-161179
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-27 (Compound 14q) is a potent TRK inhibitor with good kinase selectivity. TRK-IN-27 effectively inhibits tumor growth .
|
-
- HY-135533
-
|
Aburamycin A
|
Autophagy
|
Cancer
|
|
Chromomycin A2 (Aburamycin A) has cytotoxicity and induces autophagy. Chromomycin A2 has anti-tumor activity and can be used in cancer research .
|
-
- HY-129181
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-4 (compound 693) is a FGFR4 inhibitor with anti-tumor activity, extracted from patent WO2018113584A1 .
|
-
- HY-157122
-
VJDT
2 Publications Verification
|
Transmembrane Glycoprotein
|
Cancer
|
|
VJDT is a TREM1 small molecule inhibitor that effectively blocks TREM1 signaling. VJDT inhibits tumor growth and can be used in cancer research .
|
-
- HY-N14616
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Reumycin is a 7-azapteridine antibiotic. Reumycin is toxic to Airy carcinoma, sarcoma-180, sarcoma-37, lymphosarcoma and other tumor cells .
|
-
- HY-134418A
-
-
- HY-N1168
-
|
|
Aurora Kinase
|
Cancer
|
|
Tenacigenin B is a steroid that can be isolated from the genus Alocasia. Tenacigenin B has anti-tumor effects on lymphoma via regulation of Aurora-A .
|
-
- HY-76711
-
|
|
Opioid Receptor
|
Cancer
|
|
Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system .
|
-
- HY-N14847
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
1-Hydroxyauramycin B is an anthracycline antibiotic. 1-Hydroxyauramycin B has anti-Gram-positive bacteria and anti-tumor cell activity .
|
-
- HY-14807
-
|
CHR-2797
|
Aminopeptidase
|
Cancer
|
|
Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines .
|
-
- HY-156602A
-
|
OKI-179 hydrochloride
|
HDAC
|
Cancer
|
|
Bocodepsin hydrochloride (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin hydrochloride can be used for suppression on solid tumor and hematologic malignancies .
|
-
- HY-156675A
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Plecstatin-1 hydrochloride is an anticancer agent containing organoeuropium. Plecstatin-1 hydrochloride selectively targets plectin, a scaffolding protein and cellular connector, in tumor spheroids .
|
-
- HY-16111A
-
|
|
Farnesyl Transferase
Ras
|
Cancer
|
|
BMS-214662 hydrochloride is an inhibitor of farnesyltransferase (Farnesyl Transferase). BMS-214662 hydrochloride can effectively block the localization and function of Ras proteins on the cell membrane by inhibiting the prenylation modification of Ras proteins, thereby exerting anti-tumor activity. The IC50 value of BMS-214662 hydrochloride for H-Ras is 1.3 nM, and for K-Ras it is 8.4 nM. BMS-214662 hydrochloride can be used in the research of tumor diseases related to Ras .
|
-
- HY-107063
-
|
10-Undecen-1-yl-thiopseudourea iodide
|
Histamine Receptor
|
Cancer
|
|
AHR-1911 (10-Undecen-1-yl-Thiopseudourea Iodide;Isothiuronium) is a thiourea-based anti-inflammatory and anti-tumor agent that has an improving effect on burned skin. AHR-1911 produces histamine-like effects when injected intradermally and may reduce arterial pressure in anesthetized dogs. AHR-1911 inhibits tumor growth and reduces microsomal and C-polysome protein synthesis .
|
-
- HY-146819
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
|
-
- HY-16291A
-
|
LOR-253 hydrochloride; LT-253 hydrochloride
|
c-Myc
|
Inflammation/Immunology
|
|
APTO-253?(LOR-253) hydrochloride is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253?hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4?(KLF4)?tumor suppressor. APTO-253?hydrochloride exhibits antiarthritic activity .
|
-
- HY-50895S2
-
|
|
Isotope-Labeled Compounds
EGFR
Autophagy
|
Cancer
|
|
Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
|
-
- HY-16111
-
|
|
Farnesyl Transferase
Ras
|
Cancer
|
|
BMS-214662 is a farnesyl transferase inhibitor. BMS-214662 can effectively block the localization and function of Ras protein in the cell membrane by inhibiting the pro-group modification of Ras protein, thereby exerting anti-tumor activity. BMS-214662 has an IC50 value of 1.3 nM for H-Ras and 8.4 nM for K-Ras. BMS-214662 can be used to study Ras-related tumor diseases .
|
-
- HY-P10370
-
|
|
Bacterial
Apoptosis
|
Infection
Cancer
|
|
d-(KLAKLAK)2, as an antibacterial and anti-tumor polypeptide, is a representative of the antimicrobial peptide group, and also has good anticancer properties. d-(KLAKLAK)2 is able to kill bacteria by damaging their cell membranes, causing cell contents to leak out. d-(KLAKLAK)2 can also inhibit tumor cell proliferation by causing mitochondrial swelling and mitochondrial membrane destruction, triggering apoptosis (programmed cell death) .
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-
- HY-168035
-
|
|
Histone Methyltransferase
|
Cancer
|
|
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
|
-
- HY-101780A
-
|
EDO-S101 hydrochloride; NL-101 hydrochloride
|
HDAC
|
Cancer
|
|
Tinostamustine hydrochloride (EDO-S101 hydrochloride) is a compound with anti-multiple myeloma activity and the ability to promote CD38 expression. Tinostamustine hydrochloride enhances the sensitivity of tumor cells to the anti-CD38 monoclonal antibody daratumumab by increasing the acetylation level of histone H3. Tinostamustine hydrochloride can increase the expression of MICA and MICB, thereby activating NK cells. Tinostamustine hydrochloride can significantly delay tumor growth and improve the survival rate of mice .
|
-
- HY-149092
-
|
|
TAM Receptor
|
Cancer
|
|
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
|
-
- HY-13016
-
|
XL184; BMS-907351
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-P10869
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Inflammation/Immunology
Cancer
|
|
dCNP binds to NPR-B/C receptor, activates cGMP signaling pathway, and regulates vascular function. dCNP exhibits anti-hypoxia property through downregulation of hypoxia-related genes expressions like HIF1α and HIF2α. dCNP inhibits the induction of tumor stroma and exhibits anti-fibrosis activity. dCNP upregulates CTLs, NK cells, and conventional type 1 dendritic cells in tumors, and activates immune responses .
|
-
- HY-W014233
-
|
|
Endogenous Metabolite
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
L-Histidinol dihydrochloride is an orally active histidyl-tRNA synthetase inhibitor. L-Histidinol dihydrochloride interferes with the initiation stage of protein synthesis, thus affecting cell proliferation and metabolism. L-Histidinol dihydrochloride has the effect of modulating the sensitivity of tumor cells to chemotherapeutic agents. L-Histidinol dihydrochloride reduces the toxicity of certain chemotherapeutic agents to normal tissues and enhance the sensitivity of tumor cells to chemotherapeutic agents .
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-
- HY-152293
-
|
|
VEGFR
ERK
|
Cancer
|
|
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models . EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-159577
-
|
|
PI3K
mTOR
Akt
|
Cancer
|
|
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
|
-
- HY-153358
-
|
|
HDAC
|
Cancer
|
|
TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .
|
-
- HY-145925B
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor) .
|
-
- HY-N0370S
-
-
- HY-P1727A
-
|
|
YAP
|
Cancer
|
|
Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-N0344
-
-
- HY-155216
-
|
|
Pyruvate Kinase
|
Cancer
|
|
PKM2 activator 10 (Compd I) is a PKM2 activator with anti-tumor activity. PKM2 activator 10 can be utilized in cancer research .
|
-
- HY-148811
-
|
ICP-723
|
c-Met/HGFR
|
Cancer
|
|
Zurletrectinib is a potent tyrosine kinase inhibitor. Zurletrectinib serves as an antineoplastic agent. Zurletrectinib can used for research of preventing TRK-mediated related diseases, such as tumors .
|
-
- HY-153891
-
|
|
Drug Intermediate
|
Cancer
|
|
Deruxtecan 2-hydroxypropanamide is a highly stable Deruxtecan (HY-13631E) analog that specifically binds to receptors highly expressed in tumor cells .
|
-
- HY-14754
-
|
S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
|
Ras
Autophagy
|
Cancer
|
|
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
|
-
- HY-N4116
-
|
|
Fungal
|
Infection
Cancer
|
|
Xanthyletin is a coumarin isolated from Stauranthus perforatus, with anti-tumor and anti-bacterial activities. Xanthyletin also inhibits symbiotic fungus cultivated by leaf-cutting ants .
|
-
- HY-N7611
-
|
|
Others
|
Cancer
|
|
7-Prenyloxyaromadendrin is a flavonoid from Pterocaulon alopecuroides with antitumor activity. 7-Prenyloxyaromadendrin shows good antiproliferative activity in tumor cell lines .
|
-
- HY-W088413
-
|
|
Biochemical Assay Reagents
|
Others
|
|
DOTA-amideis a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. DOTA-amide can be used for conjugation of peptides and radionuclides.
|
-
- HY-112129
-
-
- HY-N4322
-
|
|
PKC
|
Inflammation/Immunology
Cancer
|
|
Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities .
|
-
- HY-16477A
-
|
ME2906 free acid; Mono-L-aspartyl chlorin e6 free acid; NPe6 free acid
|
Photosensitizer
|
Cancer
|
|
Talaporfin sodium, can be used in intraoperative photodynamic therapy (PDT) with a 664-nm semiconductor laser, was evaluated for efficacy and safety in treating primary malignant parenchymal brain tumors .
|
-
- HY-150256
-
|
|
YAP
|
Cancer
|
|
YTP-17 is an orally active YAP-TEAD protein-protein interaction inhibitor with an IC50 of 4 nM. YTP-17 shows anti-tumor efficacy .
|
-
- HY-119739
-
|
|
GCGR
|
Metabolic Disease
Cancer
|
|
Skyrin is an anthraquinone compound that can be isolated from almond fruit. Skyrin is a receptor-selective glucagon antagonist. Skyrin can inhibit the growth of tumor cells .
|
-
- HY-124084
-
-
- HY-W678394
-
|
|
Biochemical Assay Reagents
|
Others
|
|
DOTA-Thiolis a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. DOTA-Thiol can be used for conjugation of peptides and radionuclides.
|
-
- HY-13892
-
|
CHIR-258 dilactic acid; TKI258 dilactic acid
|
VEGFR
|
Cancer
|
|
Dovitinib (dilactic acid) is an orally active inhibitor of VEGF kinase. Dovitinib (dilactic acid) inhibits receptor tyrosine kinases (RTKs) involved in solid and hematologic cancers and tumor angiogenesis .
|
-
- HY-N4000
-
|
|
Others
|
Cancer
|
|
Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth . Digitonin is an natural detergent .
|
-
- HY-103088
-
|
E7046
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
|
Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. Palupiprant exhibits anti-tumor activities .
|
-
- HY-N14106
-
|
|
Bacterial
|
Infection
Cancer
|
|
Cinerubin R has anti-Gram-positive bacteria and inhibition of tumor cell activity, and its inhibition effect on multidrug resistant (MDR) cells is the same as that on protocells .
|
-
- HY-N14604
-
|
|
Fungal
|
Infection
|
|
Chandrananimycin B has anti-mucor activity, as well as anti-tumor cell activity such as CCL HT29, MFXF 529L, MACL McF-7 .
|
-
- HY-163129
-
|
|
Apoptosis
MMP
|
Cancer
|
|
BPU arrests cell cycle progression in the sub-G1 phase. BPU is an anticancer agent through inhibiting blood vessel formation in tumor tissues .
|
-
- HY-158067
-
-
- HY-144434
-
-
- HY-W782078
-
-
- HY-128599
-
|
|
PARP
|
Cancer
|
|
NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity .
|
-
- HY-125374A
-
|
XRP9881 dihydrate
|
Microtubule/Tubulin
|
Cancer
|
|
Larotaxel (dihydrate) (XRP9881 (dihydrate)), a new taxane compound prepared by partial synthesis from 10-deacetyl baccatin III, is active against tumors .
|
-
- HY-129307
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Gilvocarcin V is an antibiotic with antibacterial activity and can be isolated from Actinomycete. Gilvocarcin V also has anti-tumor activity and can be used in cancer research .
|
-
- HY-P99425
-
-
- HY-159668
-
|
|
ADC Linker
|
Cancer
|
DL002 is a ADC linker that can be used to synthesize antibody-drug conjugates containing BCL-2 family protein degraders, and it's used in tumor research .
|
-
- HY-160020
-
|
|
Androgen Receptor
|
Cancer
|
|
ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .
|
-
- HY-N0706
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Gracillin is a steroidal saponin that can be extracted from the roots of the plant and has anti-tumor properties. Gracillin can induce cancer cell apoptosis and autophagy .
|
-
- HY-162156
-
|
|
Mps1
|
Cancer
|
|
TTK inhibitor 4 (compound 16) is a potent inhibitor of threonine tyrosine kinase (TTK), with the IC50 value of 0.016 μM, that has anti-tumor activity .
|
-
- HY-108520
-
|
|
RAR/RXR
Apoptosis
|
Cancer
|
|
HX630 is a potent retinoic acid X receptor (RXR) agonist, can induce apoptosis, has anti-tumor effect, and can be used in Cushing's disease research .
|
-
- HY-P991097
-
|
|
VEGFR
PD-1/PD-L1
|
Cancer
|
|
PM-8002 is a bispecific antibody that targets both PD-L1 and VEGF-A. PM-8002 can be used for the study of solid tumors .
|
-
- HY-W069604
-
-
- HY-P99057
-
|
CDX-1127
|
TNF Receptor
|
Cancer
|
|
Varlilumab (CDX-1127) is a first-in-class human IgG1 anti-CD27 monoclonal antibody. Varlilumab has an anti-tumor activity .
|
-
- HY-124939
-
|
|
MMP
|
Cancer
|
|
ND-322 hydrochloride is a potent and selective water-soluble gelatinase inhibitor. ND-322 hydrochloride reduces melanoma tumor growth and delays metastatic dissemination .
|
-
- HY-124617
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
AMXT1501 is a novel inhibitor of the polyamine transport system. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells .
|
-
- HY-W039116
-
-
- HY-N14605
-
|
|
Fungal
|
Infection
|
|
Chandrananimycin C has anti-mucor activity, as well as anti-tumor cell activity such as CCL HT29, MFXF 529L, MACL McF-7 .
|
-
- HY-12449
-
|
LY3039478
|
Notch
γ-secretase
|
Cancer
|
|
Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested .
|
-
- HY-N12335
-
|
|
Others
|
Others
|
|
Desacetylxanthanol (Compound 4) is a sesquiterpenoid derived from Xanthium strumarium. Desacetylxanthanol has anti-tumor necrosis factor-associated apoptosis-inducing ligand (TRAIL) activity .
|
-
- HY-16160
-
|
|
Autophagy
ICMT
|
Cancer
|
|
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research .
|
-
- HY-162863
-
|
|
Apoptosis
|
Cancer
|
ERK-MYD88 interaction inhibitor 1 is an ERK-MYD88 interaction inhibitor. ERK-MYD88 interaction inhibitor 1 can induce an HRI-mediated integrated stress response (ISR), leading to cancer cell-specific immunogenic cell apoptosis (apoptosis). ERK-MYD88 interaction inhibitor 1 can induce anti-tumor T cell responses in Lewis lung cancer mice, exhibiting anti-tumor activity .
|
-
- HY-10180A
-
|
|
Aurora Kinase
|
Cancer
|
|
MLN8054 sodium is an Aurora A inhibitor with radiosensitivity-enhancing activity. MLN8054 sodium can activate the DNA double-strand break reaction of prostate cancer cells in in vitro experiments. The application of MLN8054 sodium is closely related to accumulation in the G2/M phase of the cell cycle and polyploid formation. In vivo experiments show that MLN8054 sodium can significantly delay the growth of prostate cancer tumors and promote tumor cell apoptosis when used in combination with radiotherapy .
|
-
- HY-10251
-
|
AC480
|
EGFR
|
Cancer
|
|
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
- HY-173125
-
![Spiro[4.5]decane-7,9-dione](http://file.medchemexpress.com/product_pic/hy-w102669.gif)
![Exatecan-amide-bicyclo[1.1.1]pentan-1-ol](http://file.medchemexpress.com/product_pic/hy-160597.gif)
