Search Result
Results for "
Mouse tumor model
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156633
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PC14586
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MDM-2/p53
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Cancer
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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 .
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- HY-125850
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- HY-159641
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BAY-3605349
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Molecular Glues
Keap1-Nrf2
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Metabolic Disease
Inflammation/Immunology
Cancer
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VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors .
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- HY-P990148
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VEGFR
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Cancer
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Anti-Mouse VEGF-A Antibody (2G11-2A05) is a rat-derived IgG2a κ type antibody inhibitor, tragrting to mouse VEGF-A with high affinity. Anti-Mouse VEGF-A Antibody (2G11-2A05) shows good anti-tumor effect in gastric cancer xenograft models .
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- HY-P990117
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Integrin
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Cardiovascular Disease
Cancer
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Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
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- HY-15323
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P505-15 Hydrochloride
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Syk
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
Src
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Cancer
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PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models .
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- HY-152293
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VEGFR
ERK
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Cancer
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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.
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- HY-161952
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JAB-3312
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SHP2
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Cancer
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Sitneprotafib (JAB-3312) is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. Sitneprotafib has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
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- HY-124628
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Fatty Acid Synthase (FASN)
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Cancer
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IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
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- HY-P99943
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KN-046
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PD-1/PD-L1
CTLA-4
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Cancer
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Erfonrilimab (KN-046) is a monoclonal antibody targeting PD-L1/CTLA-4. Erfonrilimab blocks the PD-L1 and CTLA-4 pathways, thereby regulating T cell function. Erfonrilimab enhances the secretion of IL-2 in superantigen-stimulated peripheral blood mononuclear cells. Erfonrilimab inhibits tumor growth in xenograft and double gene knock-in mouse models. Erfonrilimab can be used in research related to a variety of advanced solid tumors, including non-small cell lung cancer and nasopharyngeal carcinoma.
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- HY-P1727
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Super-TDU
Maximum Cited Publications
6 Publications Verification
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YAP
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Cancer
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Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model .
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- HY-N7526
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DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone
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Apoptosis
Autophagy
PI3K
Akt
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Neurological Disease
Inflammation/Immunology
Cancer
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Naphthazarin (DHNQ) is a microtubule depolymerizing agent. Naphthazarin can improve motor function and reduce neuroinflammation in mouse models of Parkinson's disease. Naphthazarin can induce tumor cell apoptosis, autophagy, and cell cycle arrest. Naphthazarin can also induce erythrocyte apoptosis. Naphthazarin can be used in the research of tumors and neurodegenerative diseases .
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- HY-160215
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TGF-β Receptor
p38 MAPK
TGF-beta/Smad
Interleukin Related
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Cancer
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GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
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- HY-178836
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Drug-Linker Conjugates for ADC
Ras
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Cancer
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Z56-L23 is a conjugate of RAS-targeting ADC cytotoxic payload-linker with anti-tumor activity. Z56-L23 can be conjugated with HER3 antibody, EGFR antibody or EGFRxHER3 bispecific antibody to form intact antibody-drug conjugates (ADCs). ADC molecules related to Z56-L23 effectively inhibit the proliferation of tumor cells and also significantly suppress tumor growth in xenograft mouse models. Z56-L23 can be used in the research of pancreatic cancer .
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- HY-156111
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PROTACs
Androgen Receptor
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Cancer
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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 .
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- HY-136447
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ASP4132
1 Publications Verification
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AMPK
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Cancer
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ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
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- HY-P990789
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CTLA-4
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Others
Inflammation/Immunology
Cancer
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Anti-Mouse CTLA-4 Antibody (9H10) is a kind of syrian hamster IgG antibody inhibitor, targeting to CTLA-4. Anti-Mouse CTLA-4 Antibody (9H10) binds mouse CTLA-4 and blocks the interaction between CTLA-4 and its ligand. Anti-Mouse CTLA-4 Antibody (9H10) shows potent anti-tumor effect in various tumor models, such as breast and colon cancer .
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- HY-153364
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PPAR
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Cancer
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FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models .
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- HY-153521
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BCL6
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Cancer
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CCT374705 is an orally active BCL6 inhibitor (IC50 = 4.8 nM) with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
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- HY-P990107
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TGF-β Receptor
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Cancer
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Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
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- HY-12182A
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Prostaglandin Receptor
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Cancer
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ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
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- HY-P991481
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CCR
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Inflammation/Immunology
Cancer
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S-531011 is a human IgG1 monoclonal antibody (mAb) targeting CCR8. S-531011 reduces tumor-infiltrating CCR8+ Tregs and has anti-tumor activity in CT26.WT and EMT6 tumor-bearing mouse tumor models. S-531011 can be used in the study of cancer immunity. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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- HY-139852
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Phosphatase
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Cancer
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PLAP-IN-1 is a selective PLAP inhibitor with an IC50 of 0.032 μM. PLAP-IN-1 acts as a tumor-targeting agent; its fluorescein-conjugated derivative specifically binds to PLAP-positive tumor cells in vitro and targets cervical cancer in mouse xenograft models. PLAP-IN-1 can be used in the research of cervical cancer and ovarian cancer .
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- HY-172930
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Molecular Glues
IKZF Family
Potassium Channel
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Inflammation/Immunology
Cancer
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PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
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- HY-D2062
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Fluorescent Dye
Integrin
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Cancer
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ATTO 740 NHS ester is a near-infrared fluorescent dye and a multimodal fluorescence/photoacoustic contrast agent with excellent near-infrared emission properties and extremely high photostability. The photoacoustic signal of ATTO 740 NHS ester shows no significant decrease after continuous irradiation with a 750 nm laser for 30 min, making it suitable for in vivo fluorescence imaging and photoacoustic contrast imaging. When conjugated with the cystine knot peptide R01, ATTO 740 NHS ester enables precise detection of integrin αvβ6-positive cells and tumors in nude mouse xenograft models .
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- HY-169779
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p62
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Cancer
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PTX80 is an antagonist of p62 with an IC50 value of 31.18 nM. PTX80 reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model .
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- HY-163081
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PARP
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Cancer
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PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
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- HY-157029S
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Ras
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Cancer
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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 .
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- HY-145331A
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Arginase
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Cancer
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ARG1-IN-1 (Compound 3) hydrochloride is an orally active arginase inhibitor with an IC50 value of 29 nM. ARG1-IN-1 hydrochloride can inhibit serum arginase activity and increase arginine levels in mouse tumor models. ARG1-IN-1 hydrochloride is applicable for tumor research .
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- HY-176508
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Casein Kinase
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Cancer
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KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models .
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- HY-P990257
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c-Fms
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Cancer
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Anti-Mouse CSF1 Antibody (5A1) is a rat-derived anti-mouse CSF1 IgG1 κ type antibody inhibitor. Anti-Mouse CSF1 Antibody (5A1) can inhibit cells proliferation and macrophage-induced invasion. Anti-Mouse CSF1 Antibody (5A1) shows potent anti-tumor effect in various tumor models, such as neuroblastoma .
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- HY-15782
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Aminoacyl-tRNA Synthetase
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Cancer
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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 .
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- HY-157031S
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Ras
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Cancer
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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 .
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- HY-149464
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Ras
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Cancer
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ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model .
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- HY-15324
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P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
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Syk
Src
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
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Cancer
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PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models . .
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- HY-153482
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Small Interfering RNA (siRNA)
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Cancer
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ATU027 is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
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- HY-12182
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Prostaglandin Receptor
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Cancer
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ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
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- HY-111209
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S14161
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PI3K
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Cancer
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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 .
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- HY-126379
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Apoptosis
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Cancer
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CDDO-2P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-2P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model .
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- HY-145331
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Arginase
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Cancer
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ARG1-IN-1 (Compound 3) is an orally active arginase inhibitor with an IC50 value of 29 nM. ARG1-IN-1 can inhibit serum arginase activity and increase arginine levels in mouse tumor models. ARG1-IN-1 is applicable for tumor research .
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- HY-153482A
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Small Interfering RNA (siRNA)
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Cancer
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ATU027 sodium is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 sodium has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
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- HY-177796
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Apoptosis
CDK
Caspase
PARP
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Cancer
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TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a KD of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC50 = 6.53 μM) and HCCLM3 cells (IC50 = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research .
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- HY-177483
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Oxaliplatin-artesunate
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Ferroptosis
Mitochondrial Metabolism
Glutathione Peroxidase
Transferrin Receptor
MMP
Dihydroorotate Dehydrogenase
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Cancer
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OART (Oxaliplatin-artesunate) is a ferroptosis inducer. OART significantly inhibits tumor cell proliferation. OART induces cytoplasmic and mitochondrial LPO to promote tumor ferroptosis, via destroying glutathione-mediated ferroptosis defense system and enhancing iron-dependent Fenton reaction. OART enhances tumor immunogenicity, transforming tumor environment from immunosuppressive to immunosensitive. OART has strong tumor regression in tumor-bearing mouse models. OART can be used for cancer immunotherapy research .
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- HY-P991307
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LILRB
Transmembrane Glycoprotein
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Cancer
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BND-35 is a human monoclonal antibody (mAb) targeting LILRB4/ILT3/CD85k. BND-35 blocks the interaction of ILT3 with APOE and fibronectin, enhances the pro-inflammatory activity of various myeloid cells, and reverses ILT3-mediated immunosuppression of T cells by various suppressive myeloid cells. BND-35 has anti-tumor activity in the hILT3 transgenic mouse tumor model .
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- HY-175857
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HDAC
Apoptosis
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Cancer
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HDAC-IN-92 is a pan-HDAC inhibitor with an IC50 of 12.58 µM in A2780 cells. HDAC-IN-92 demonstrates broad-spectrum, notable cytotoxic activity against a range of human cancer cell lines, including ovarian, liver, and breast carcinomas. HDAC-IN-92 causes apoptosis and demonstrates a notable decrease in tumor cell colony formation. HDAC-IN-92 inhibits the formation of blood vessels in the chick chorioallantoic membrane (CAM). HDAC-IN-92 exhibits anti-tumor effect in a 4T1 tumor-bearing mouse model. HDAC-IN-92 can be used for research targeting solid tumor .
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- HY-176740
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PROTACs
Bcl-2 Family
p38 MAPK
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Apoptosis
ERK
JNK
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Cancer
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PROTAC Bcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 has strong anti-tumor activity against HepG2 cells and HUVEC cells. PROTAC Bcl-xL degrader-4 induces cells apoptosis by decreasing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly inhibits tumor growth in xenograft tumor mouse models . Pink: MAPK ligand (HY-176741); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W017440)
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- HY-106603
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Diarylsulfonylurea; LY186641
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Calcium Channel
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Cancer
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Sulofenur (LY186641) is an orally active anti-tumor agent. Sulofenur induces gene expression through calcium ion-dependent pathways and some protein kinase-independent pathways, and its effect is particularly enhanced in H-ras mutant cells. Sulofenur exhibits significant activity in mouse solid tumor models and human tumor xenograft models .
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- HY-P1728
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YAP
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Cancer
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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 .
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- HY-P1728A
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YAP
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Cancer
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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 .
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- HY-135217
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Apoptosis
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Cancer
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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 .
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- HY-175727
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DGK
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Cancer
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DGKα-IN-9 is a diacylglycerol kinase alpha (DGKα) inhibitor. DGKα-IN-9 demonstrates a tumor growth inhibition in MC38 or or CT26 mouse tumor model. DGKα-IN-9 can be used for the study of cancer .
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- HY-174424
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PD-1/PD-L1
Apoptosis
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Cancer
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NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer .
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- HY-155681
-
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PD-1/PD-L1
Monoamine Oxidase
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Cancer
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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%) .
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- HY-111145
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Androgen Receptor
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Cancer
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RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
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- HY-100443
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PX-102
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FXR
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Cancer
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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 .
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- HY-160215A
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TGF-β Receptor
p38 MAPK
TGF-beta/Smad
Interleukin Related
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Cancer
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GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
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- HY-148839
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c-Myc
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Cancer
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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 .
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- HY-P990259
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Transmembrane Glycoprotein
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Inflammation/Immunology
Cancer
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Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
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- HY-19459A
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- HY-13646C
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HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride
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P-glycoprotein
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Cancer
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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 .
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- HY-P1727A
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YAP
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Cancer
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Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model .
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- HY-139716
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NF-κB
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Inflammation/Immunology
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IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.
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- HY-147784
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Btk
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Cancer
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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 .
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- HY-155146
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Necroptosis
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Cancer
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Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
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- HY-163192
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ROR
Apoptosis
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Cancer
|
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W6134 is highly potent and selective RORγ covalent inhibitor with an IC50 of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC) .
|
-
- HY-168147
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp-1-IN-24 (compund 7) is an ENPP1 inhibitor that, in combination with anti-PD-1 antibodies, achieves 77.7% tumor growth inhibition and improves survival in mouse models .
|
-
- HY-W854934
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
IKP-104 is a microtubule/tubulin inhibitor (IC50 = 1.31 μM). IKP-104 arrests cells in mitosis and the M phase by inhibiting microtubule polymerization and inducing cytoskeletal microtubule depolymerization. IKP-104 inhibits the growth of mouse and human tumor cell lines. IKP-104 exhibits anti-tumor effects in mouse ascites tumors and lung cancer models. IKP-104 is useful in the research of cancers such as leukemia, lung cancer and melanoma .
|
-
- 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-162892
-
|
|
Epigenetic Reader Domain
|
Cancer
|
BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model .
|
-
- HY-170436
-
|
|
Photosensitizer
Apoptosis
|
Cancer
|
|
NFh-NMe-2 is a photosensitizer, that interacts with nitroreductase, generates singlet oxygen in tumor cells, exhibits cytotoxicity in cancer cells, and induces apoptosis. NFh-NMe-2 exhibits antitumor efficacy in mouse models .
|
-
- HY-157847
-
|
|
STAT
|
Cancer
|
|
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 .
|
-
- HY-161736
-
|
|
CDK
|
Cancer
|
|
ARN25499 (compound 15) is a CDC42 inhibitor. ARN25499 can be used in cancer-related research .
|
-
- HY-172937
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 13 (compound MR3) is potent ERα degrader with an IC50 of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model .
|
-
- HY-169918
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-34 (compound A8) is a phenyl urea SHP2 inhibitor with anti-cancer activity. SHP2-IN-34 significantly suppresses tumor growth in CT26 mouse model .
|
-
- HY-163076
-
|
|
Apoptosis
|
Others
|
|
Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
|
-
- HY-13762
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-19606
-
|
Antibiotic MI 43-37F11
|
Interleukin Related
NO Synthase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cytogenin (Antibiotic MI 43-37F11) is an orally active antineoplastic antibiotic. Cytogenin regulates the inflammatory cytokine, reduces the levels of iNOS, NO and IL-6 in mouse macrophages, and exhibits antidiabetic efficacy in mice. Cytogenin inhibits growth of Ehrlich ascites tumor in mouse model .
|
-
- HY-165603
-
|
|
Liposome
VEGFR
FGFR
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Si5-N14 is a key component of siloxane-incorporated lipid nanoparticles (SiLNP), possessing pro-vascular repair and anti-tumor activities. In the transgenic GFP mouse model, Si5-N14 can mediate CRISPR-Cas9 editing. In the Lewis lung carcinoma (LLC) tumor-bearing mouse model, Si5-N14 can knock out the expression of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) to exert an anti-tumor effect. In a mouse model of lung injury induced by viral infection, the delivery of Fibroblast Growth Factor-2 (FGF-2) mRNA via Si5-N14 can promote vascular repair, increase blood oxygen levels, and improve lung function. Si5-N14 shows promise for research in the fields of oncology, pneumonia, and cardiovascular diseases .
|
-
- HY-106431
-
|
Olpadronate; OLP
|
Farnesyl Transferase
|
Metabolic Disease
Cancer
|
|
Olpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid also prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis .
|
-
- HY-162239
-
|
|
Drug Intermediate
|
Cancer
|
|
Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
|
-
- HY-172453
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
XW-032 is an apo-IDO1 inhibitor, with an IC50 of 21 nM. XW-032 (TGI = 63%) exhibits potent in vivo anti-tumor efficacy in the CT26 syngeneic mouse model and is expected to be applied in the research of the field of cancer .
|
-
- HY-125850R
-
|
|
Drug Metabolite
Reference Standards
HIV
Interleukin Related
|
Infection
Inflammation/Immunology
Cancer
|
|
Berberrubine (chloride) (Standard) is the analytical standard of Berberrubine (chloride). This product is intended for research and analytical applications. Berberrubine chloride is an orally active metabolite of berberine. Berberrubine chloride alleviates mucosal lesions and inflammation in mouse colitis models. Berberrubine chloride has anti-inflammatory, anti-tumor, and antiviral activities .
|
-
- HY-135217R
-
|
|
Apoptosis
Reference Standards
|
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-P991464
-
|
|
TNF Receptor
|
Cancer
|
|
IBI37G5 is a human monoclonal antibody (mAb) targeting TNFRSF18/GITR/CD357. IBI37G5 has anti-tumor activity in MC38 and B16F10 mouse tumor models. IBI37G5 can be used in the study of cancer immunity .
|
-
- HY-182467
-
|
|
Molecular Glues
IKZF Family
E1/E2/E3 Enzyme
|
Cancer
|
|
BMS-986482 is a CELMoD, CRBN-mediated, selective IKZF1-4 Molecular Glue degrader. The activity of BMS-986482 is driven by a non-traditional CELMoD core that selectively degrades the IKZF protein family. BMS-986482 inhibits tumor growth in preclinical mouse models. BMS-986482 can be used for the research of advanced solid tumors .
.
|
-
- HY-178271
-
|
|
Drug Intermediate
|
Cancer
|
|
P-SCN-Bn-NOTA is a metal chelator and molecular imaging probe precursor that allows radiolabeling with Ga-68. P-SCN-Bn-NOTA can be conjugated to CD70-specific molecules B3, B6, ABDB3 and ABDB6 to form NOTA-labeled derivatives. P-SCN-Bn-NOTA is applicable for preclinical PET/CT imaging of CD70-expressing tumors in NCG mouse PDX models. P-SCN-Bn-NOTA can be used in studies related to CD70-positive tumors .
|
-
- HY-P992352
-
|
|
|
|
|
ES005 is an anti-tumor compound and LAG3 inhibitor. ES005 blocks the interactions of LAG3 with MHC-II, LSECtin and FGL1, thereby effectively reversing the LAG3-mediated inhibition of T cell activation and NFAT reporter gene expression. ES005 exhibits significant tumor growth inhibitory effects in syngeneic mouse breast tumor models using humanized LAG3 knock-in mice. ES005 can be used for breast tumor-related research .
|
-
- HY-182238
-
|
|
MAP4K
Interleukin Related
|
Cancer
|
|
HPK1-IN-69 is an orally active HPK1 inhibitor with an IC50 of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors .
|
-
- HY-P992388
-
|
|
LILRB
|
Cancer
|
|
IO-108 is a humanized IgG4 monoclonal antibody and a competitive inhibitor of LILRB2, with a KD value of 1.97 nM. IO-108 competitively blocks the binding of LILRB2 to its ligands including HLA-G, MHC-I, ANGPTL2 and SEMA4A, reprograms tumor-associated myeloid cells, drives the conversion of suppressive myeloid cells into a pro-inflammatory phenotype, and restores the cytotoxic activity of T cells and NK cells. IO-108 inhibits tumor growth in LILRB2 transgenic mouse models. IO-108 can be used for the research of solid tumors .
|
-
- HY-182043
-
|
|
c-Kit
PDGFR
|
Cancer
|
|
BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KIT V654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KIT V654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors .
|
-
- HY-186151
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53 null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer .
|
-
- HY-W719784
-
|
|
Others
|
Cancer
|
|
Dimethynur is an anti-tumor agent. Dimethynur exerts anti-tumor effects in solid sarcoma mouse models. Dimethynur can be used in cancer research .
|
-
- HY-P991966
-
|
|
EGFR
|
Cancer
|
|
Anti-Human/Mouse EGFR Antibody (7A7) ia an anti-mouse EGFR monoclonal antibody proposed to be the mouse equivalent of cetuximab. Anti-Human/Mouse EGFR Antibody (7A7) fails to induce tumor regression in the HPV38 tumor model where EGFR is not expressed in mice. Anti-Human/Mouse EGFR Antibody (7A7) can be used in EGFR-expressing HPV38 tumor-related studies .
|
-
- HY-105361
-
|
BL 6782
|
Drug Derivative
|
Cancer
|
|
BMY 25282 (BL 6782) is a mitomycin C (MMC) analog. BMY 25282 catalyzes oxygen activation in hepatocytes. BMY 25282 overcomes MMC tolerance in colon cancer cells and mouse models of colon cancer. BMY 25282 inhibits tumor growth in mouse models of leukemia and melanoma. BMY 25282 can be used in research on cancers such as leukemia, melanoma, and colon cancer .
|
-
- HY-183774
-
|
|
TAM Receptor
|
Cancer
|
|
NTQ2494 is a potent and orallty active AXL kinase inhibitor with an IC50 of 4.89 nM. NTQ2494 inhibits AXL kinase catalytic activity. NTQ2494 suppresses tumor growth in mouse xenograft models. NTQ2494 can be used for the research of advanced hematological malignancies, solid tumors .
|
-
- 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-13762A
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene hydrochloride is an antihistamine agent and a chemical sensitizer. Tesmilifene hydrochloride targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene hydrochloride overcomes multidrug resistance .
|
-
- HY-P11624
-
|
|
Apoptosis
|
Cancer
|
|
PP-60 is an apoptosis inducer. PP-60 inhibits the proliferation of cancer cells and induces cancer cell apoptosis. PP-60 exerts anti-tumor effects in nude mouse liver tumor models. PP-60 is applicable to research related to cancers such as liver cancer, lung cancer, and prostate cancer .
|
-
- HY-183186
-
|
|
METTL3
Cytochrome P450
|
Cancer
|
|
EP102 is an orally active, selective inhibitor of the METTL3/METTL14 complex with an IC50 of 2 nM. EP102 reduces intracellular N6-methyladenosine levels, inhibits cancer cell proliferation, and thereby suppresses tumor growth in mouse models. EP102 is applicable for the research of acute myeloid leukemia, ovarian solid tumors and advanced solid tumors .
|
-
- HY-19211
-
|
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
KW-2170 hydrochloride is an alkylating agent and topoisomerase II inhibitor. KW-2170 hydrochloride stabilizes the topoisomerase II-DNA complex, causing DNA double-strand breaks, thereby preventing DNA replication and transcription, and ultimately leading to the death of tumor cells. KW-2170 hydrochloride exhibits potent and broad-spectrum anti-tumor activity in various mouse and human tumor models. KW-2170 hydrochloride can be used in the research of solid tumors .
|
-
- HY-150233
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models) .
|
-
- HY-172970
-
|
|
CDK
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
HQY1428 is an orally active CDK12 inhibitor. HQY1428 inhibits DNA replication, causes G2/M arrest in SKOV3 cells, induces DNA double-strand breaks and apoptosis. HQY1428 has anti-tumor activity in the SKOV3 xenograft mouse model. HQY1428 combined with the HER2 inhibitor Lapatinib (HY-50898) in the NCI-N87 xenograft mouse model produces a synergistic therapeutic effect .
|
-
- HY-16634
-
|
|
MDM-2/p53
|
Cancer
|
|
MI-888 (TFA) is an orally active MDM2-p53 interaction inhibitor with a Ki of 0.44 nM. MI-888 (TFA) can achieve rapid, complete, and sustained tumor regression in a xenograft mouse model of cancer .
|
-
- HY-W016794
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
NSC3852 exhibits anti-proliferative activity against cancer cell MCF-7. NSC3852 promotes the ROS generation, DNA damage, and apoptosis in MCF-7. NSC3852 exhibits anti-tumor against leukemia in mouse model
|
-
- HY-160843
-
|
|
Apoptosis
|
Cancer
|
|
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 .
|
-
- 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-176404
-
|
|
HSP
|
Cancer
|
|
DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC50: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model .
|
-
- HY-113701
-
|
|
Androgen Receptor
|
Cancer
|
|
CH5137291 is an orally active pure antagonist of the androgen receptor (AR), without generating agonist metabolites. CCH5137291 directly blocks the transfer of AR from the cytoplasm to the nucleus. H5137291 can completely inhibit tumor growth in cells and mouse models of castration-resistant prostate cancer models. CH5137291 can be used for the study of castration-resistant prostate cancer (CRPC) .
|
-
- HY-155109
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-114 is a potent stimulator of interferon genes (STING) agonist. Antitumor agent-114 activates immunity and reduces tumor volume in a mouse model of breast cancer. Antitumor agent-114 can be used for immunity and cancer diseases research .
|
-
- HY-156881
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
Apoptosis
|
Cancer
|
|
PARG-IN-4 (Formula (A)) is an orally available PARG inhibitor (EC50=1.9 nM) with cell membrane permeability. PARG-IN-4 can effectively inhibit tumor growth in mouse models. PARG-IN-4 can be used in cancer research .
|
-
- HY-124875
-
|
HIF inhibitor 64B
|
HIF/HIF Prolyl-Hydroxylase
|
Neurological Disease
|
|
Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model .
|
-
- HY-P992043
-
|
ANK-101
|
Interleukin Related
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Tolododekin alfa (ANK-101) is a drug conjugate that anchors and combines IL-12 with Aluminum Hydroxide (HY-B1521). Tolododekin alfa promotes the recruitment of effector CD8 + T cells to tumor sites, enhances the production of γ-interferon, upregulates the expression of PD-L1, and induces sustained pro-inflammatory gene expression in mouse tumor models. Tolododekin alfa can be used for research related to advanced solid tumors .
|
-
- 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-136927
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-Y1356
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
2,4-Dimethoxybenzaldehyde is a tumor initiator with genotoxic property. 2,4-Dimethoxybenzaldehyde can induce benign papilloma development and converse to squamous cell carcinoma in the skin of susceptible mouse models. 2,4-Dimethoxybenzaldehyde can be used for skin cancer research .
|
-
- 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-17658
-
|
|
Apoptosis
|
Cancer
|
|
Apiol analog-1 (Compound 2b) is an analog of Apiol (HY-135217). 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-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-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-117366
-
|
|
PKC
|
Cancer
|
|
PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
|
-
- HY-182082
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
XYD270 is an orally active BRD9 PROTAC degrader. XYD270 inhibits the proliferation of cancer cells. XYD270 suppresses tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia .
|
-
- HY-149035
-
|
|
Others
|
Cancer
|
|
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
|
-
- HY-156681A
-
|
(S)-STX-478; (S)-STX-478-101; (S)-LY4064809
|
PI3K
|
Cancer
|
|
(S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .
|
-
- HY-179712
-
|
|
TrxR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
As-CA11 is a Thioredoxin reductase (TrxR) inhibitor with an IC50 of 18.7 nM. As-CA11 can induce cancer cells apoptosis and ROS production. As-CA11 can reduce the level of reduced Trx and increase the level of oxidized Trx. As-CA11 demonstrates anti-tumor activity in the 4T1 tumor-bearing mouse model .
|
-
- 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-N15497
-
|
|
Reactive Oxygen Species (ROS)
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Terpestacin is found in Phoma exigua var. heteromorpha. Terpestacin binds to UQCRB to inhibit the production of mitochondrial ROS and HIF-1α. Terpestacin inhibits tumor angiogenesis in the FM3A breast cancer cell xenograft mouse model. Terpestacin has antitumor activity and phytotoxicity .
|
-
- HY-160021
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma .
|
-
- HY-111170
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
STA-9584 is a potent vascular disrupting agent (VDA) that targets tubulin. STA-9584 exhibits potent antitumor activity in mouse xenograft model by selectively targeting microvasculature at both the center and periphery of tumors. STA-9584 can be used for research in prostate and breast cancer .
|
-
- HY-P991960
-
|
|
CTLA-4
Interleukin Related
|
Cancer
|
|
JS007 is a humanized IgG1 monoclonal antibody and also a CTLA-4 binder, with a Kd of 0.21 nM for CTLA-4. JS007 blocks the interaction between CTLA-4 and B7-1. JS007 activates T cells, promotes increased IL-2 secretion, and inhibits tumor growth in CTLA-4 knock-in mouse syngeneic tumor models. JS007 is applicable to research related to cancer and advanced solid tumors.
|
-
- HY-149539
-
|
|
FLT3
RET
|
Cancer
|
|
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
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-
- HY-P991660
-
|
|
c-Met/HGFR
|
Cancer
|
|
ARGX-111 is an anti-MET antibody. ARGX-111 blocks HGF-dependent and -independent signaling, downregulating MET expression on the tumor cell surface. ARGX-111 depletes MET-expressing circulating tumor cells through enhanced antibody-dependent cell-mediated cytotoxicity (ADCC), thereby inhibiting tumor metastasis. ARGX-111 depletes circulating tumor cells and inhibits bone and lung metastasis in an orthotopic mouse model of metastatic breast cancer. ARGX-111 is promising for research in breast cancer and other cancers .
|
-
- HY-16916
-
NS1643
1 Publications Verification
|
Potassium Channel
Autophagy
|
Cancer
|
|
NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K + channels with an EC50 of 10.5 μM. NS1643 inhibits the growth of breast cancer tumors in TNBC mouse models. NS1643 inhibits cell migration and invasion of breast cancer cells .
|
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
- HY-170850
-
|
|
Kinesin
|
Cancer
|
|
MKLP2-IN-1 (compound 12a) is an inhibitor of MKLP2 with good oral bioavailability. MKLP2-IN-1 inhibits the microtubule-stimulated ATPase activity of recombinant MKLP2 in vitro and suppresses tumor growth in a mouse Calu-6 lung cancer model .
|
-
- HY-P990116
-
|
|
Osteopontin
|
Inflammation/Immunology
|
|
Anti-Mouse osteopontin/SPP1 Antibody (103D6) is a mouse-derived anti-mouse osteopontin/SPP1 IgG2c κ type antibody inhibitor. Anti-Mouse osteopontin/SPP1 Antibody (103D6) increases cytotoxic T lymphocyte lytic activity and suppresses colon tumor growth. Anti-Mouse osteopontin/SPP1 Antibody (103D6) ameliorates liver injury in common bile duct ligation (CBDL)-induced primary sclerosing cholangitis mice models .
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-
- 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-W110138
-
|
|
DNA/RNA Synthesis
Cytochrome P450
ROCK
|
Cancer
|
|
Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
|
-
- HY-169310
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
|
-
- HY-149666
-
|
|
DGK
|
Cancer
|
|
BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.09 (DGKα) and 0.006 μM (DGKζ) .
|
-
- 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-149667
-
|
|
DGK
|
Cancer
|
|
BMS-332 is a dual DGKα/ζ lipid kinase inhibitor, with IC50s of 5 and 1 nM against DGKα and DGKζ, respectively. BMS-332 enhances the antigen-specific T cell response. BMS-332 reduces the viral load in the liver and spleen when combined with anti-PD-1 in chronic infection models. BMS-332 can be used for the study of T cell immune checkpoint strategy .
|
-
- HY-123334
-
|
|
Porcupine
Wnt
|
Cancer
|
|
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 .
|
-
- HY-117520
-
|
|
Proteasome
|
Cancer
|
|
FV-162 is a potent, orally active and irreversible proteasome inhibitor. FV-162 exhibits cytotoxic to human myeloma cell lines and primary myeloma cells. FV-162 inhibits tumor growth in a myeloma xenograft mouse model. FV-162 can be used for myeloma research .
|
-
- HY-170453
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
|
-
- HY-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-180850
-
|
|
PROTACs
Estrogen Receptor/ERR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer .
|
-
- 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-P991958
-
|
|
CTLA-4
|
Cancer
|
|
GIGA-564 is a fully human anti-CTLA4 IgG1 monoclonal antibody with a Kd of 9.8 nM. GIGA-564 binds to a unique epitope of CTLA-4, mediates FcR-dependent signaling pathways, depletes CTLA-4-highly-expressing regulatory T cells within tumors, and inhibits the proliferation of peripheral regulatory T cells. GIGA-564 exhibits anti-tumor activity in mouse models. GIGA-564 can be used for tumor research .
|
-
- HY-176758
-
|
|
Glutathione Peroxidase
|
Cancer
|
|
GPX4-IN-17 (Compound 9i) is an inhibitor of GPX4 with potent cytotoxicity (IC50 = 0.3 nM). GPX4-IN-17 shows strong binding affinity against GPX4 (KD = 20.4 nM). GPX4-IN-17 inhibits tumor growth in the xenograft tumor mouse model without detectable cytotoxicity. GPX4-IN-17 can enhance cancer chemotherapy and overcome tumor resistance. GPX4-IN-17 can be studied in antitumor reseach .
|
-
- HY-155523
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-P991057
-
|
|
CD47
|
Cancer
|
|
STI-6643 is a fully human IgG4 antibody that targets CD47. STI-6643 blocks CD47-SIRPα interaction, and enables macrophage-mediated phagocytosis of tumor cells. STI-6643 shows anti-tumor activity in mouse lymphoma xenograft models. STI-6643 can be used for the research of Burkitt's lymphoma, solid tumors, relapsed or refractory tumors, and lymphoma. The isotype control for STI-6643 can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
|
-
- HY-13762S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cancer
|
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-162001
-
|
|
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-106431R
-
|
Olpadronate (Standard); OLP (Standard)
|
Reference Standards
Others
|
Metabolic Disease
Cancer
|
|
Olpadronic acid (Standard) is the analytical standard of Olpadronic acid. This product is intended for research and analytical applications. Olpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid also prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis .
|
-
- HY-P991639
-
|
|
Apoptosis
|
Cancer
|
|
BIW-8962 is a humanized anti-ganglioside GM2 antibody. BIW-8962 exhibits ADCC/CDC activity against multiple myeloma cells. BIW-8962 demonstrates potent anti-tumor activity in mouse xenograft models. BIW-8962 is indicated for research in myeloma and other cancers .
|
-
- HY-N0421
-
|
Cinobufagine
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- 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-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-174830
-
|
|
PD-1/PD-L1
|
Cancer
|
|
GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with Kd values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy .
|
-
- HY-182506
-
|
BM 12.531
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
Azimexon (BM 12.531) is an orally active immunomodulator with radioprotective and antitumor activities. Azimexon prolongs survival in multiple mouse models, enhances immunity and hematopoiesis, and alleviates radiation injury and tumor metastasis. Azimexon causes reversible hemolytic anemia in rats and dogs, and exerts therapeutic activity against adjuvant-induced arthritis in rats. Azimexon can be used for the research of lung carcinoma, leukemia, multiple myeloma, lung tumor, arthritis, breast cancer and AIDS‑related complex .
|
-
- HY-P99948
-
|
AMG-596
|
EGFR
CD3
|
Neurological Disease
Cancer
|
|
Etevritamab (AMG-596) is a bispecific T-cell engager that targets EGFRvIII and CD3. Etevritamab simultaneously binds CD3 on T cells and EGFRvIII on glioblastoma multiforme cells, thereby forming a bridge structure. Etevritamab triggers T-cell activation, proliferation, secretion of cytotoxic substances, and tumor cell lysis. Etevritamab extends overall survival and induces tumor regression in mouse models of glioblastoma multiforme. Etevritamab can be used for research related to glioblastoma .
|
-
- 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-129510
-
|
|
EGFR
Mitosis
|
Cancer
|
|
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
|
-
- HY-111251
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
4SC-207 is a potent, orally active microtubule inhibitor. 4SC-207 inhibits microtubule growth to inhibit tumor cell proliferation in vitro and in vivo, and promotes a mitotic delay/arrest, followed by apoptosis or aberrant divisions. 4SC-207 inhibits tumor growth in taxane resistant xenograft mouse models. 4SC-207 can be used for cancer research, such as colon adenocarcinoma and other malignancies .
|
-
- HY-P991646
-
|
heMab
|
Transmembrane Glycoprotein
|
Cancer
|
|
ING-1 (heMab) is a high-affinity humanized monoclonal antibody against epithelial cell adhesion molecule (Ep-CAM). ING-1 is a transmembrane glycoprotein mediating Ca 2+. ING-1 binds to Ep-CAM on tumor cells and exhibits potent in vitro activity, targeting and inhibiting tumor growth and metastasis in mouse cancer models. ING-1 is useful in the research of breast, colorectal, and lung cancers, among other cancers .
|
-
- HY-159771
-
|
|
FAP
|
Cancer
|
|
FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.
|
-
- 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-163760
-
|
|
HuR
MMP
|
Cancer
|
|
ZM-32 is an inhibitor for human antigen R (HuR), that downregulates the expression of VEGF-A and MMP9, and thus inhibits breast cancer tumor angiogenesis. ZM-32 exhibits broad-spectrum anti-proliferative effects in a variety of cancer cell lines, and exhibits antitumor efficacy against MDA-MB-231 in mouse models .
|
-
- HY-12797
-
|
|
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
GF 15 is an inhibitor of centrosomal clustering during cell mitosis, with an EC50 value of 900 nM for inducing multipolar spindles. GF 15 is a derivative of griseofulvin that inhibits tubulin polymerization at concentrations above 25 μM. GF 15 inhibits tumor growth and significantly prolongs survival in mouse xenograft models of human colon cancer and multiple myeloma .
|
-
- HY-139418
-
|
|
FXR
|
Cancer
|
|
PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models .
|
-
- HY-19938
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
MTL-005 is a boron-containing radiosensitizer used in Boron Neutron Capture Therapy (BNCT). MTL-005 enriches the boron-10 isotope in tumor tissues, causing nuclear fission under thermal neutron irradiation, releasing high linear energy transfer (LET) α particles and lithium ions, which selectively destroy tumor cells while minimizing damage to surrounding normal tissues. MTL-005 significantly controlls the tumor progression in the SCCVII squamous cell carcinoma mouse model and prolonged the survival of the mice. MTL-005 can be used to study solid tumors such as head and neck cancer.
|
-
- HY-145729
-
|
AZD9150
|
STAT
Apoptosis
|
Cancer
|
|
Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
|
-
- HY-145729A
-
|
AZD9150 sodium
|
STAT
Apoptosis
|
Cancer
|
|
Danvatirsen sodium (AZD9150 sodium) is an antisense oligonucleotide targeting STAT3. Danvatirsen sodium reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen sodium inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen sodium inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen sodium achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen sodium can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
|
-
- HY-P992338
-
|
|
Mesothelin
Constitutive Androstane Receptor
|
Inflammation/Immunology
Cancer
|
|
CT-1119 is an autologous human anti-Mesothelin chimeric antigen receptor macrophage (CAR-M). CT-1119 mediates CAR-dependent, antigen-dependent functional activities. CT-1119 acts as a phagocytosis inducer, tumor cell killer, pro-inflammatory cytokine inducer, and M1 macrophage polarizer. CT-1119 exhibits stronger resistance to M2 repolarization and reduces tumor burden in a mouse lung cancer xenograft model. CT-1119 can be used for the research of mesothelin-expressing solid tumors .
|
-
- HY-P10947
-
|
|
Epigenetic Reader Domain
YAP
|
Cancer
|
|
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
|
-
- HY-182468
-
|
|
Histone Acetyltransferase
Estrogen Receptor/ERR
CDK
|
Cancer
|
|
OP-3136 is a selective KAT6 inhibitor. OP-3136 reduces the proliferative capacity of cancer cells and inhibits cell growth in ER + breast cancer cell models with overexpressed KAT6. When combined with ER antagonists/degraders or CDK4/6 inhibitors, OP-3136 exhibits synergistic anti-tumor activity in mouse xenograft models. OP-3136 can be used in studies related to HR +/HER2 - breast cancer .
|
-
- HY-P990004
-
|
|
Tim3
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse TIM-3 Antibody (B8.2C12) is an anti-mouse TIM-3 IgG1 monoclonal antibody. Anti-Mouse TIM-3 Antibody (B8.2C12) can block the binding of Tim-3 with Phosphatidylserine (PtdSer) and CEACAM1 without interfering with the binding to Galectin-9. Anti-Mouse TIM-3 Antibody (B8.2C12) can inhibit tumor growth and activate tumor infiltrating CD8 + T cells. Anti-Mouse TIM-3 Antibody (B8.2C12) can be used for studying cancer such as breast cancer and colon cancer and constructing experimental autoimmune encephalomyelitis (EAE) models .
|
-
- 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-176798
-
|
|
Lactate Dehydrogenase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model .
|
-
- HY-169347
-
|
LC-05-004
|
Molecular Glues
Casein Kinase
|
Cancer
|
|
dCK1α-2 is an orally active CK1α molecular glue degrader that targets p53 pathway-related targets. dCK1α-2 exhibits anti-tumor efficacy in mouse models and can increase the expression of p53-related genes. .
|
-
- HY-121490
-
|
|
Apoptosis
|
Cancer
|
|
IMM-02 is a DID-DAD binding inhibitor with activity promoting actin assembly and microtubule stabilization. IMM-02 is able to trigger serum response factor-mediated gene expression and lead to cell cycle arrest and apoptosis. IMM-02 has shown the ability to slow tumor growth in a mouse colon cancer xenograft model .
|
-
- HY-16726R
-
|
CG100649 (Standard)
|
Reference Standards
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-182915
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-26 is an orally active FGFR inhibitor. FGFR-IN-26 inhibits FGFR2 wild-type and clinically relevant resistance mutations. FGFR-IN-26 inhibits tumor growth in FGFR2-amplified xenograft mouse models. FGFR-IN-26 can be used for the research of cancer, suah as gastric carcinoma .
|
-
- HY-182922
-
|
|
PROTACs
STAT
|
Cancer
|
|
SD-965 is a selective STAT3 PROTAC degrader with a DC50 of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma .
|
-
- HY-170936
-
|
|
FAK
Hippo (MST)
YAP
|
Cancer
|
|
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
|
-
- HY-154313
-
|
Clospirazine
|
Ras
|
Cancer
|
|
Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
|
-
- HY-106963
-
|
LGD1550
|
RAR/RXR
|
Cancer
|
|
ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
|
-
- HY-P991233
-
|
|
EGFR
|
Cancer
|
|
BAT1006 is a monoclonal antibody targeting HER2 extracellular domain II with enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) for the study of HER2-positive locally advanced/metastatic solid tumors. BAT1006 has an approximately 5-fold enhanced ADCC effect compared to pertuzumab (HY-P9912) and exhibits potent anti-tumor activity in the HER2-positive Calu-3 xenograft mouse model .
|
-
- HY-147696
-
|
|
HSP
AMPK
Reactive Oxygen Species (ROS)
|
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-180989
-
|
|
PROTACs
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PROTAC PLK1 Degrader-2 (Compound NC1) is a PLK1 PROTAC degrader with an Kd of 6.06 μM. PROTAC PLK1 Degrader-2 significantly inhibits the proliferation of HeLa cells, induces cell cycle arrest and apoptosis. PROTAC PLK1 Degrader-2 exhibits significant anti-tumor activity in a HeLa cell xenograft tumor mouse model. PROTAC PLK1 Degrader-2 can be used for the study of cervical cancer.
|
-
- HY-175802
-
|
HYBI-084
|
WDR5
Potassium Channel
|
Inflammation/Immunology
Cancer
|
|
HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 + cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM .
|
-
- HY-161954
-
|
|
HDAC
|
Cancer
|
|
HDAC8-IN-12 (compound 5k) is a non-hydroxamic acid, selective inhibitor of HDAC8 (IC50: 0.12 nM) and a potent inhibitor of breast cancer. HDAC8-IN-12 triggers anti-tumor immunity by activating T cells, increasing the proportion of M1 macrophages and decreasing the proportion of M2 macrophages. HDAC8-IN-12 (50 mg/kg) exerts tumor suppressive effects in an orthotopic mouse model of breast cancer .
|
-
- HY-179380
-
|
|
Phosphatase
IFNAR
JAK
STAT
|
Cancer
|
|
PTPN2-IN-2 is a potent and orally active PTPN2 inhibitor (IC50 = 7.05 nM) that enhances the IFN-γ signaling pathway. PTPN2-IN-2 inhibits PTP1B with an IC50 of 9.88 nM. PTPN2-IN-2 inhibits tumor growth, promotes the activation and infiltration of tumor immune cells in a B16-OVA mouse model. PTPN2-IN-2 can be used for the research of melanoma .
|
-
- HY-178954
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1-IN-32 (Compound 45) is a potent and orally effective IDO1 inhibitor with an IC50 of 10 pM. IDO1-IN-32 exhibits significant anti-proliferative activity against Hela cells. IDO1-IN-32 can significantly inhibit tumor growth in CT26 and LCC transplanted mouse models by activating anti-tumor immunity. IDO1-IN-32 can be used for research on colon cancer and breast cancer .
|
-
- HY-119357
-
|
|
Microtubule/Tubulin
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
|
TN-16 is a Microtubule polymerization inhibitor. TN-16 induces G2/M cell cycle arrest, metaphase mitotic arrest and Apoptotic cell death in cells, and blocks late Autophagic flux by inhibiting autophagosome-lysosome fusion. TN-16 suppresses tumor growth in syngeneic mouse breast cancer models. TN-16 can be used in research related to neuroblastoma, cervical cancer, breast cancer and other tumors .
|
-
- 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-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-168012
-
|
|
Ras
Phosphatase
|
Cancer
|
|
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
|
-
- HY-165503
-
|
|
Wnt
β-catenin
|
Cancer
|
|
AZ1366 is an orally active tankyrase inhibitor. AZ1366 stabilizes Axin2, reduces NuMA levels, disrupts the interaction between tankyrase and NuMA, induces G2/M phase arrest, inhibits the Wnt pathway, and downregulates the expression of β-catenin-dependent genes. AZ1366 inhibits tumor growth in colorectal cancer xenograft models. AZ1366 synergistically inhibits the proliferation of non-small cell lung cancer cells, improves tumor control and significantly prolongs survival in orthotopic non-small cell lung cancer mouse models. AZ1366 is applicable to research related to colorectal cancer and non-small cell lung cancer .
|
-
- HY-175260
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ (IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer .
|
-
- HY-135953
-
|
|
Apoptosis
|
Cancer
|
|
CDDO-3P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-3P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model . CDDO-3P-Im is a orally active necroptosis inhibitor that can be used for the research of ischemia/reperfusion (I/R) .
|
-
- HY-168934
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR137 is a WRN degrader, with an IC50 of 8 nM. KWR137 exhibits good anti-proliferative activity against MSI-H cells, with a GI50 of 509 nM in SW48 cells and a GI50 of 824 μM in HCT116 cells. It also demonstrates anti-tumor growth effects in xenograft mouse models. KWR137 can be used for cancer research .
|
-
- HY-160061
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model .
|
-
- HY-183804
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-16 is an orally active ERα PROTAC degrader with a DC50 of 1.4 nM and an IC50 of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research .
|
-
- HY-111193
-
|
3-Chloroprocainamide
|
NF-κB
Apoptosis
|
Cancer
|
|
Declopramide (3-Chloroprocainamide) is an orally active antitumor agent, which inhibits proliferation of cancer cells HL60 and K562, and inhibits tumor growth of human brain astrocytoma (T24) in mouse model. Declopramide induces apoptosis, inhibits NF-κB through inhibition of IκBα degradation. Declopramide serves also as chemosensitizer in research .
|
-
- HY-155740
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC50=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability .
|
-
- HY-P991328
-
|
|
Notch
|
Cancer
|
|
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
|
-
- HY-183866
-
|
Maleimide-KGDEVD-doxorubicin
|
HSP
IFNAR
|
Cancer
|
|
MPD-1 (Maleimide-KGDEVD-doxorubicin) is a peptide drug conjugate (PDC). MPD-1 enhances CD8 + T cell tumor infiltration, and activates antigen-presenting cells. MPD-1 enables dual-trigger payload release, amplifies cytotoxicity via in situ feedback, and selectively delivers payload to tumor microenvironments via enhanced albumin metabolism and macropinocytosis. MPD-1 exhibits antitumor efficacy in mouse colorectal cancer models. MPD-1 can be used for the research of colorectal cancer .
|
-
- HY-155848
-
|
|
Phosphatase
|
Cancer
|
|
LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.
|
-
- HY-P992441
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
PHST001 is a humanized anti-CD24 antibody. PHST001 binds cell-surface CD24, blocks CD24-Siglec10 interaction, and engages Fc receptors to promote macrophage-mediated tumor cell phagocytosis. PHST001 inhibits growth of breast cancer and ovarian cancer, and reduces metastatic lesions in mouse xenograft models. PHST001 can be used for the research of triple negative breast cancer, HER2+ breast cancer, metastatic tumors, and ovarian cancer .
|
-
- HY-123045
-
|
|
CDK
|
Cancer
|
|
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
|
-
- HY-180430
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-208, a Bufalin (HY-N0877) analogue, is a potent and orally active antitumor agent. Antitumor agent-208 exhibits antiproliferative activity against tumor cell line (IC50 =0.30-1.09 nM). Antitumor agent-208 inhibits tumor growth in a MV-4-11 xenograft mouse model. Antitumor agent-208 can be used for cancer research, such as acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC) .
|
-
- HY-148807C
-
|
QC8222 sodium; TACH 101 sodium
|
Apoptosis
Histone Demethylase
|
Cancer
|
|
Zavondemstat (QC8222; TACH 101) sodium is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat sodium induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat sodium suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat sodium can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
|
-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-160740
-
|
|
Others
|
Cancer
|
|
Antitumor agent-148 (Example 1) is an anti-cancer agent. Antitumor agent-148 effectively inhibits the growth, migration and invasion of cancer cells. Antitumor agent-148 significantly inhibits the lymphatic metastasis of breast cancer cells in mouse models. Antitumor agent-148 can be used for the study of malignant tumors such as breast cancer, lung cancer and gastric cancer .
|
-
- HY-182269
-
|
|
Cathepsin
Apoptosis
PARP
Caspase
|
Cancer
|
|
Cathepsin-IN-5 is a cathepsin inhibitor with IC50 values of 6.2 μM and 81 nM for cathepsin L and cathepsin S. Cathepsin-IN-5 inhibits cancer cells proliferation, induces apoptosis, reduces growth of hepatocellular tumors in mouse models, and modulates expression of genes linked to cell death, cell proliferation, and cellular processes. Cathepsin-IN-5 can be used for the research of hepatocellular carcinoma .
|
-
- HY-172454
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-36 (Compound B8) is an allosteric inhibitor of SHP2, with an IC50 value of 9.0 nM. In addition, its IC50 for p-ERK is 40 nM. SHP2-IN-36 also exhibited significant antitumor activity in the KYSE520 xenograft mouse model. SHP2-IN-36 can be used for research in the field of anti-tumor .
|
-
- HY-163673
-
|
|
Glucocorticoid Receptor
Drug-Linker Conjugates for ADC
|
Inflammation/Immunology
|
|
Glucocorticoid receptor modulator 4 (Compound DL5) is a conjugate of a linker and a glucocorticoid receptor modulator. Glucocorticoid receptor modulator 4 exhibits GRE Reporter activity in mTNF expressing K562 cell with an EC50 of 40 μM. Glucocorticoid receptor modulator 4 binds with an anti-tumor necrosis factor (TNF) antibody, and exhibits anti-inflammtory activity against arthritis in mouse models .
|
-
- HY-148918
-
|
|
β-catenin
Wnt
Bcl-2 Family
|
Inflammation/Immunology
Cancer
|
E722-2648 is an inhibitor targeting the BCL9 and β-catenin complex with antitumor activity. E722-2648 blocks complex formation by disrupting the interaction between the two proteins, thereby inhibiting β-catenin-mediated transcriptional activity and downregulating the expression of WNT target genes. E722-2648 effectively inhibits tumor growth in colon cancer xenograft models and colorectal cancer mouse models. E722-2648 can be used for the research of colon cancer and colorectal cancer .
|
-
- HY-121365
-
|
|
Bacterial
|
Infection
|
|
Forphenicinol is an immunomodulator and a derivative of the bacterial metabolite forphenicine. It increases the phagocytosis of yeast by peritoneal macrophages isolated from thioglycolate-stimulated mice. Forphenicinol (100 μg/animal) prevents cyclophosphamide-induced suppression of delayed-type hypersensitivity (DTH), as well as enhances DTH in response to the hapten oxazolone or sheep red blood cells in mice. It enhances the bactericidal activity of macrophages against P. aeruginosa in mice when administered at a dose of 0.5 mg/kg.2 Forphenicinol (15.6-1,000 μg/animal) increases survival in a mouse model of P. aeruginosa infection. It also inhibits tumor growth in S180 sarcoma and IMC carcinoma mouse xenograft models when administered at doses ranging from 0.05 to 5 mg/kg per day.
|
-
- HY-116504
-
|
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
|
-
- HY-16232
-
|
D 19575; Glucosylifosfamide mustard
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma .
|
-
- HY-151462
-
RP-6685
3 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
|
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 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-12440
-
|
|
IAP
Apoptosis
|
Cancer
|
|
HM90822 is an orally active IAP antagonist. HM90822 induces ubiquitination and proteasome-dependent degradation of XIAP, cIAP1 and cIAP2 in sensitive pancreatic cancer cells. HM90822 induces Apoptotic cell death. HM90822 inhibits tumor growth in Panc-1 pancreatic cancer xenograft and orthotopic mouse models. HM90822 can be used for the research of pancreatic cancer .
|
-
- HY-107811A
-
|
|
Autophagy
α-synuclein
Apoptosis
Monoamine Oxidase
Mitosis
|
Neurological Disease
Cancer
|
|
Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol hydrochloride can induce cell mitosis, Autophagy and Apoptosis. Harmol hydrochloride promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol hydrochloride has anti-tumor, anti-depressant and anti-aging activities. Harmol hydrochloride improves motor impairment in a mouse Parkinson's disease model .
|
-
- HY-N0421R
-
|
Cinobufagine (Standard)
|
Reference Standards
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- HY-155971
-
|
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cell activation (VISTA). VISTA-IN-2 induces VISTA degradation in cells through an autophagic mechanism. VISTA-IN-2 rescues VISTA-mediated immunosuppression, and enhances antitumor activity of immune cells. VISTA-IN-2 also activates the antitumor immunity and inhibits tumor growth in a CT26 mouse model .
|
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-183103
-
|
|
Bcr-Abl
Src
Btk
|
Cancer
|
|
PDD-87 is an orally active, blood-brain barrier permeable kinase inhibitor, with IC50 values ranging from 0.07 nM to 0.72 nM against ABL, SRC family, BTK kinases and their key mutants. PDD-87 induces antiproliferative effects in leukemia and lymphoma cells, and inhibits tumor growth in mouse xenograft models. PDD-87 can be used for the research of leukemia and lymphoma .
|
-
- HY-107811
-
Harmol
1 Publications Verification
|
Autophagy
α-synuclein
Apoptosis
Monoamine Oxidase
Mitosis
|
Neurological Disease
Cancer
|
|
Harmol is an orally active β-carboline alkaloid. Harmol is a TFEB activator and monoamine oxidase inhibitor. Harmol can induce cell mitosis, Autophagy and Apoptosis. Harmol promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol has anti-tumor, anti-depressant and anti-aging activities. Harmol improves motor impairment in a mouse Parkinson's disease model .
|
-
- HY-P991663
-
|
|
Tie
|
Cancer
|
|
AMG-780 is a fully human IgG2 antibody that targets angiopoietin 1 (Ang1) (IC50 = 4.5 nM) and angiopoietin 2 (Ang2) (IC50 = 0.06 nM). AMG-780 inhibits tumor growth in the Colo205 xenograft mouse model by inhibiting both Ang1 and Ang2. AMG-780 is indicated for the research of cancers such as colon cancer .
|
-
- HY-165245
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
|
-
- HY-W747797
-
|
|
Isotope-Labeled Compounds
Apoptosis
|
Cancer
|
|
Cinobufagine-d3 is the deuterium labeled Cinobufagin (HY-N0421). Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-P991336
-
|
INBRX-106; ES-102
|
Orexin Receptor (OX Receptor)
|
Inflammation/Immunology
Cancer
|
|
Ordastobart (INBRX-106; ES-102) is a hexavalent OX40 agonist antibody. Ordastobart enhances OX40 receptor clustering, signaling, and downstream activation, thereby increasing the proliferation and activation of CD4 + and CD8 + T cells in vitro and in vivo. Ordastobart exhibits anti-tumor effects and improves survival in mouse models of cancer. Ordastobart is indicated for research in cancers such as fibrosarcoma and colorectal cancer .
|
-
- HY-P11050A
-
|
|
Apoptosis
|
Cancer
|
|
SP94 is a peptide ligand with high specificity for hepatocellular carcinoma cells. SP94 selectively binds to multiple hepatocellular carcinoma cell lines in vitro. SP94 inhibits tumor growth in a mouse model of hepatocellular carcinoma by promoting apoptosis and reducing angiogenesis. SP94 can be used as a specific probe for hepatocellular carcinoma imaging. SP94 is useful for hepatocellular carcinoma research .
|
-
- HY-148807
-
|
QC8222 free base; TACH 101 free base
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Zavondemstat (QC8222 free base; TACH 101 free base) is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
|
-
- HY-152830
-
|
Q702
|
c-Fms
TAM Receptor
MHC
|
Cancer
|
|
Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
|
-
- 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) .
|
-
- HY-180912
-
|
|
CDK
Apoptosis
|
Cancer
|
|
HS-36 is a highly selective and orally active dual inhibitor of CDK4 and CDK9 with IC50 values of 18.9 and 4.2 nM respectively. HS-36 exhibits nanomolar-level potent activity against various cancer cells, inducing G0/G1 phase arrest and promoting cell apoptosis. HS-36 efficiently inhibits tumor growth in a mouse model of MV-4-11 tumors. HS-36 can be used for the study of acute myeloid leukemia .
|
-
- HY-P991372
-
|
RN927C antibody
|
TROP2
|
Cancer
|
|
Anti-TROP2 Antibody (RN927C antibody) is a human monoclonal antibody targeting Trop-2. Anti-TROP2 Antibody exerts in vitro inhibitory effects on a variety of tumor cell lines. Anti-TROP2 Antibody exhibits anti-tumor activity in mouse pancreatic PDX, ovarian PDX, lung PDX and triple-negative breast cancer (TNB) PDX models. Anti-TROP2 Antibody can be used for research on pancreatic cancer, ovarian cancer, lung cancer and triple-negative breast cancer .
|
-
- HY-P10761
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-164429
-
|
|
Integrin
Elastase
|
Cancer
|
|
VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
|
-
- HY-P991310
-
|
LT3015; LT-3000
|
LPL Receptor
|
Neurological Disease
Cancer
|
|
Lpathomab (LT3015; LT-3000) is a human IgG1 monoclonal antibody (mAb) targeting LPA. Lpathomab reduces the release of IL-8 and IL-6 cytokines in SKOV3 cells and blocks LPA-triggered tumor cell migration. Lpathomab reduces neovascularization in Matrigel plug and CNV models. Lpathomab inhibits brain injury in the CCI mouse model. Lpathomab can be used in the study of brain injury, ovarian cancer, diabetic neuropathy, and spinal cord injury. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-148918A
-
|
|
β-catenin
Wnt
Bcl-2 Family
|
Cancer
|
E722-2648 TFA is an inhibitor targeting the BCL9 and β-catenin complex with antitumor activity. E722-2648 TFA blocks complex formation by disrupting the interaction between the two proteins, thereby inhibiting β-catenin-mediated transcriptional activity and downregulating the expression of WNT target genes. E722-2648 TFA effectively inhibits tumor growth in colon cancer xenograft models and colorectal cancer mouse models. E722-2648 TFA can be used for the research of colon cancer and colorectal cancer .
|
-
- HY-108894
-
|
|
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Ferumoxytol is an FDA-approved ultrasmall superparamagnetic iron oxide preparation and iron replacement agent that exerts selective activity against leukemia cells with low ferroportin expression. Ferumoxytol increases intracellular iron levels, induces reactive oxygen species (ROS) production via the Fenton reaction, and triggers oxidative stress and cell death. Ferumoxytol reduces disease burden in mouse models and patient-derived leukemia models. As an MRI contrast agent, Ferumoxytol enables imaging of vascular lesions, tumors and lymph nodes. Ferumoxytol can be used in research related to acute myeloid leukemia and blast-phase chronic myeloid leukemia .
|
-
- HY-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-186013
-
|
|
Apoptosis
|
Cancer
|
|
CML-07-119 is a selective inhibitor of GGPP synthase (GGPPS) with an IC50 of ~27 nM. CML-07-119 induces apoptosis and exhibits anticancer activity against acute myeloid leukemia (AML) cells, including those harbouring TP53 mutations. CML-07-119 inhibits tumor growth in an AML mouse xenograft model. CML-07-119 can be used for AML research .
|
-
- HY-181054
-
|
|
Bcl-2 Family
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Mcl-1-IN-21 is a selective Mcl-1 protein inhibitor. Mcl-1-IN-21 can induce apoptosis, elevate intracellular ROS, reduce mitochondrial membrane potential, exert cytotoxicity against human cervical cancer cells, and inhibit tumor growth in a human cervical cancer xenograft mouse model. Mcl-1-IN-21 can be used for the research of cervical cancer .
|
-
- HY-173189
-
|
2′,5′-ApApA; 2′,5′-trioligoadenylate; 5'-O-Triphosphoryladenylyl-(2'→5')-adenylyl-(2'→5')-adenosine
|
DNA/RNA Synthesis
RSV
|
Infection
Cancer
|
|
2-5A is a RNase L activator, signal mediator and innate immune second messenger. 2-5A induces the expression of interferons and interferon-stimulated genes in recipient cells in a RNase L-dependent manner. 2-5A inhibits tumor growth in mouse models via paracrine RNase L activation derived from cancer cells. 2-5A can be used in studies related to viral infection and cancer .
|
-
- HY-13440
-
AMG 511
5 Publications Verification
|
PI3K
|
Cancer
|
|
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
|
-
- HY-169937
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
|
-
- HY-175870
-
|
|
Ras
|
Cancer
|
|
Eras-4001 (Compound 14-1) is a pan-KRAS inhibitor. Eras-4001 has potent antitumor activities and significantly inhibits the proliferation of wild-type and mutant (such as KRAS G12D, KRAS G12V and KRAS G12C) cancer cells. Eras-4001 effectively inhibits tumor growth in GP2D and Panc0403 xenograft mouse models .
|
-
- HY-175652
-
|
|
PROTACs
Adenosine Receptor
|
Cancer
|
|
AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .
|
-
- HY-110077
-
API-1
1 Publications Verification
|
Akt
Apoptosis
Caspase
PARP
|
Cancer
|
|
API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC50 = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model .
|
-
- HY-121081
-
|
|
CDK
|
Cancer
|
|
BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-958 shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-958 exhibits good metabolic stability. BAY-958 effectively inhibits tumor growth in mouse xenograft models without significant toxicity .
|
-
- HY-155532
-
|
|
Apoptosis
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-146462
-
|
|
Apoptosis
ROS Kinase
|
Cancer
|
|
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
|
-
- HY-131328
-
|
LOXO-305
|
Btk
|
Cancer
|
|
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
|
-
- HY-182084
-
|
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
|
Cancer
|
|
BRD9 ligand-12 is a BRD9 ligand. BRD9 ligand-12 can be used as a ligand for target protein for PROTAC to develop and design degradative agents for PROTAC BRD9, such as XYD270 (HY-182082). XYD270 inhibits tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia .
|
-
- HY-180557
-
|
|
Folate Receptor (FR)
|
Cancer
|
|
4A-BFA-11 is a folate-targeted PEG-MMAE conjugate that exhibits specific binding affinity for the folate receptor α (FR-α) (KD = 106.7 nM). 4A-BFA-11 achieves tumor enrichment by combining PEG-mediated long circulation (EPR effect) and folate receptor targeting. 4A-BFA-11 undergoes enzymatic cleavage at the tumor site to release the active payload, enabling precise action. 4A-BFA-11 sefficiently carries, targets, and controls the release of MMAE in tumor tissues in a HeLa mouse model. 4A-BFA-11 can be used for cervical cancer, ovarian cancer, and lung cancer research .
|
-
- HY-152830A
-
|
Q702 TFA
|
c-Fms
TAM Receptor
MHC
|
Cancer
|
|
Adrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
|
-
- HY-148807A
-
|
QC8222; TACH 101
|
Apoptosis
Histone Demethylase
|
Cancer
|
|
Zavondemstat (QC8222; TACH 101) L-lysine is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat L-lysine induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat L-lysine suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat L-lysine can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
|
-
- HY-182239
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PDL1 degrader-3 (comppund e24) is a PD-L1 degrader. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer .
|
-
- HY-149913
-
|
|
Orphan Nuclear Receptor
|
Cancer
|
|
NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model .
|
-
- HY-129510R
-
|
|
EGFR
Mitosis
Reference Standards
|
Cancer
|
|
4-Methyl erlotinib (Standard) is the analytical standard of 4-Methyl erlotinib. This product is intended for research and analytical applications. 4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
|
-
- HY-118722
-
|
|
DNA/RNA Synthesis
Cytochrome P450
|
Cancer
|
|
RB-90740 is a type of biological reducing agent. RB-90740 is activated through metabolic reduction and generates cytotoxic products, thereby selectively killing tumor cells (usually in a hypoxic environment). RB-90740 has selective toxicity towards hypoxic cells, which is mainly achieved by causing DNA strand breaks and activating reducing enzymes (such as Cytochrome P450). RB-90740 does not initially exhibit cytotoxicity similar to its in vitro properties in hypoxic cells in mouse models. RB-90740 can be used to study the tumor physiological environment
|
-
- HY-183364
-
-
- HY-183328
-
|
|
MNK
Bcl-2 Family
|
Cancer
|
|
MNK1/2-IN-11 is a potent, selective and orally active MNK1/2 inhibitor with MNK1 IC50 of 1.2 nM, MNK2 IC50 of 1.3 nM. MNK1/2-IN-11 reduces eukaryotic translation initiation factor 4E phosphorylation, decreases Mcl-1 and Cyclin D1 expression. MNK1/2-IN-11 inhibits tumor growth in mouse CT26 colorectal tumor models. MNK1/2-IN-11 can be used for the research of colorectal cancer .
|
-
- HY-177345
-
|
|
Sigma Receptor
Apoptosis
Caspase
|
Cancer
|
|
SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer .
|
-
- HY-162133
-
|
|
STING
Apoptosis
IKK
IFNAR
NF-κB
|
Cancer
|
MSA-2-Pt, platinum salt-modified MSA-2 (HY-136927), is a STING agonist. MSA-2-Pt inducing cell
death by platinum and activating the STING pathway by MSA-2. MSA-2-Pt direct activates STING pathway, induces phosphorylation of TBK1, IRF3, and NF-κB p65. MSA-2-Pt enhances tumor infiltration of CD4 + and CD8 + T cells, and induces tumor cell death and apoptosis in mouse colon carcinoma and melanoma models .
|
-
- HY-163527
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
|
-
- HY-155993
-
|
|
PARP
|
Cancer
|
|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
|
-
- HY-121081A
-
|
BAY-958 hydrochloride
|
CDK
|
Cancer
|
|
BAY-1112054 (BAY-958) hydrochloride is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-1112054 hydrochloride shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-1112054 hydrochloride exhibits good metabolic stability. BAY-1112054 hydrochloride effectively inhibits tumor growth in mouse xenograft models without significant toxicity .
|
-
- HY-153503
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
|
Cancer
|
|
ALK-IN-24 is an orally active ALK inhibitor with an IC50 value of 1.7 nM. ALK-IN-24 also inhibits insulin receptor kinase with an IC50 value of 6 nM. ALK-IN-24 suppresses the proliferation of lung adenocarcinoma cells. ALK-IN-24 inhibits ALK-driven tumor growth in xenograft mouse models. ALK-IN-24 can be used in research related to non-small cell lung cancer .
|
-
- HY-P991353
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models .
|
-
- 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-122849
-
|
|
c-Kit
|
Cancer
|
|
CHMFL-KIT-031 is a highly selective KIT V559D inhibitor, with an IC50 of 28 nM. CHMFL-KIT-031 potently affects KIT V559D mutant’s phosphorylation at Y703/719/823 sites. CHMFL-KIT-031 inhibits the tumor growth in BaF3-TEL-KIT-V559D cell inoculated mouse model .
|
-
- HY-145239
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 + T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .
|
-
- HY-P991366
-
|
AL008
|
CD47
|
Cancer
|
|
IBI-397 is a human monoclonal antibody (mAb) targeting SIRPα/CD172a . IBI-397 promotes human monocyte-derived dendritic cell-mediated T cell proliferation and increases the expression of CD86 and HLA-DR. IBI-397 has antitumor activity in the mouse MDA-MB-231 tumor model. IBI-397 can be used in Myeloma research .
|
-
- HY-180897
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
RSK4-IN-2 (compound 16o) is a potent, orally active RSK4 inhibitor with an IC50 of 17 nM. RSK4-IN-2 suppresses esophageal squamous cell carcinoma (ESCC) cell growth and invasion, by inhibiting phosphorylation of RSK4 downstream targets. RSK4-IN-2 inhibits tumor growth and metastasis in ESCC mouse models. RSK4-IN-2 can be used for ESCC research .
|
-
- HY-147008
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC) .
|
-
- 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-143286
-
|
|
PROTACs
FLT3
|
Cancer
|
|
PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .
|
-
- HY-133151
-
|
|
CXCR
|
Cancer
|
|
CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma .
|
-
- HY-177021
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models .
|
-
- HY-177914
-
|
|
MEK
|
Cancer
|
|
MEK-IN-7 (compound WX086) is potent, orally active and selective MEK inhibitor (MEK1 IC50 = 29.62 nM). MEK-IN-7 inhibits HT29 and A375 cell proliferation with IC50s of 0.62 and 0.40 nM. MEK-IN-7 inhibits tumor growth in a HL-29 xenograft mouse model. MEK-IN-7 can be used for melanoma and colon cancer research .
|
-
- HY-179391
-
|
|
Telomerase
Apoptosis
|
Cancer
|
|
Telomerase-IN-9 is a potent and selective telomerase inhibitor. Telomerase-IN-9 significantly reduces telomerase activity by binding to hTERT, leading to decreased telomerase function. Telomerase-IN-9 induces apoptosis and inhibits colony formation. Telomerase-IN-9 reduces tumor burden, restores antioxidantbalance, and preserves lung architecture in a Benzo[a]pyrene (HY-107377)-induced lung cancer mouse model. Telomerase-IN-9 can be used for the research of lung cancer .
|
-
- HY-15186
-
|
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-175988
-
|
|
DNA Methyltransferase
HDAC
|
Cancer
|
|
DNMT/HDAC-IN-2 (Compound Y7) is a DNMT and HDAC inhibitor with IC50 values for DNMT1, HDAC1, and HDAC6 of 365, 0.2, and 8.91 nM respectively. DNMT/HDAC-IN-2 inhibits the proliferation of breast cancer cells. DNMT/HDAC-IN-2 significantly reduces tumor growth in xenografts and transgenic breast cancer mouse models. DNMT/HDAC-IN-2 can be used for the study of breast cancer .
|
-
- HY-161629
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
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-
- HY-18676B
-
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OSU-T315 analog
|
Integrin
Autophagy
Apoptosis
Caspase
PDHK
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Cancer
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|
ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models .
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-
- HY-173433
-
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Epigenetic Reader Domain
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Cancer
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|
JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .
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- HY-101447
-
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EPH 116
|
Src
Apoptosis
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Cancer
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|
SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
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- HY-157317
-
|
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Apoptosis
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Cancer
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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 .
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- HY-15186C
-
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GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
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-
- HY-169120
-
|
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Telomerase
|
Cancer
|
|
FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
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-
- HY-172874
-
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Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
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|
TDO-IN-2 (Compound 5c) is an orally active TDO inhibitor (IC50: 1.25 μM). TDO-IN-2 has antitumor activity in the Hepa1-6 hepatocellular carcinoma allograft mouse model. TDO-IN-2 has synergistic effects with the PD-1/PD-L1 inhibitor BMS-202 (HY-19745) and can be used to study tumor immune tolerance .
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- HY-139061
-
|
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LPL Receptor
ROCK
|
Cancer
|
|
Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
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-
- HY-176957
-
|
|
Wee1
|
Cancer
|
|
PKMYT1-IN-11 (Example 1) is a PKMYT1 inhibitor with an IC50 of 4.49 nM. PKMYT1-IN-11 inhibits the proliferation of HCC1569 cells. When combined with Gemcitabine (HY-17026), PKMYT1-IN-11 shows a significant anti-tumor effect in the OVCAR3 xenograft mouse model. PKMYT1-IN-11 can be used for the study of various cancers such as breast cancer and ovarian cancer .
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-
- HY-168300
-
|
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Reactive Oxygen Species (ROS)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
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-
- HY-P992032
-
|
BAY-943 antibody
|
Interleukin Related
|
Cancer
|
|
TPP-9476 is an anti-human IL3RA (CD123) monoclonal antibody with human IL3RA Kd of 11 nM and cynomolgus monkey IL3RA Kd of 16 nM. TPP-9476 binds specifically to human and cynomolgus monkey IL3RA, undergoes target-dependent internalization into lysosomes of IL3RA-positive cells.TPP-9476 exerts antiproliferative effects in IL3RA-expressing acute myeloid leukemia and classical Hodgkin lymphoma cells, reduces tumor burden, improves survival, and induces complete tumor remission in relevant xenograft mouse models .
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-
- HY-P10744
-
|
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Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-119264
-
|
|
Molecular Glues
Ras
Apoptosis
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PRLX-93936 is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 inhibits HIF-1 under hypoxic conditions (IC50 = 0.09 μM in cell-based reporter gene assay). PRLX-93936 suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 is applicable to research related to pancreatic cancer and multiple myeloma .
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-
- HY-119264A
-
|
|
Molecular Glues
Apoptosis
Ras
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PRLX-93936 dihydrochloride is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 dihydrochloride binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 dihydrochloride induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 dihydrochloride inhibits HIF-1 under hypoxic conditions (IC50 = 0.09 μM in cell-based reporter gene assay). PRLX-93936 dihydrochloride suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 dihydrochloride is applicable to research related to pancreatic cancer and multiple myeloma .
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-
- HY-147081
-
AS 1411
2 Publications Verification
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 .
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-
- HY-177332
-
|
|
TAM Receptor
SARS-CoV
Akt
|
Infection
Cancer
|
|
SLC-391 is an orally active AXL kinase inhibitor with an IC50 of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer .
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-
- HY-178716
-
|
|
Phosphatase
IFNAR
STAT
JAK
|
Cancer
|
|
PTPN2/1-IN-4 (Compound WS35) is an orally active, dual-functional inhibitor of PTPN1 and PTPN2 with IC50s of 12.8 and 5.8 nM for PTPN1 and PTPN2, respectively. PTPN2/1-IN-4 modulates the IFNγ-JAK-STAT signaling pathway and significantly augments CD8+ T-cell tumor infiltration. PTPN2/1-IN-4 has potent anticancer activity, robustly inhibiting tumor growth both as a monotherapy and in combination with an anti-PD-1 antibody in B16-OVA syngeneic mouse models .
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-
- HY-100543
-
-
- HY-P992406
-
|
|
MMP
IFNAR
|
Cancer
|
|
MEDI-3622 is a human monoclonal antibody against ADAM17. MEDI-3622 blocks the ADAM17-mediated shedding of CD16A and CD62L on NK cells, and binds with high specificity to a surface loop unique to the metalloprotease catalytic domain of ADAM17. MEDI-3622 enhances IFNγ production by NK cells when they bind to antibody-coated tumor cells. MEDI-3622 can be used in the research of ovarian cancer, Burkitt lymphoma, head and neck cancer, and colorectal cancer .
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-
- HY-103043
-
|
|
Others
|
Cancer
|
|
Pz 285 is an anti-cancer agent. Pz 285 shows significant inhibitory effect on the viability of MDA-MB-231 breast cancer cells, with an IC50 of 15.0 μM. Pz 285 exhibits remarkable antitumor effects in the mouse tumor xenograft model constructed with highly lung-metastatic MDA-MB-231 LM24 Her2+ breast cancer cells. Pz 285 can be used for the study of breast cancer, especially metastatic breast cancer .
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-
- HY-149433
-
|
|
PROTACs
Androgen Receptor
Apoptosis
|
Cancer
|
|
BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .
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-
- HY-181020
-
|
|
Phosphodiesterase (PDE)
p38 MAPK
Akt
mTOR
ERK
|
Cancer
|
|
Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma .
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- HY-16232R
-
|
D 19575 (Standard); Glucosylifosfamide mustard (Standard)
|
Reference Standards
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
Glufosfamide (Standard) is the analytical standard of Glufosfamide. This product is intended for research and analytical applications. Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma .
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-
- HY-181484
-
|
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STING
IKK
IFNAR
Interleukin Related
CXCR
|
Cancer
|
|
STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer .
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- HY-181541
-
|
|
HDAC
Apoptosis
Wnt
β-catenin
MDM-2/p53
c-Myc
|
Cancer
|
|
HIT211504993 is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.070 μM. HIT211504993 suppresses cancer cell proliferation, cause G1 phase cell cycle arrest and induces apoptosis. HIT211504993 inhibits Myc-driven tumorigenesis via nucleocytoplasmic acetylation, p53 modulation, and Wnt/β-catenin signaling modulation. HIT211504993 inhibits tumor growth in a colon cancer xenograft mouse model. HIT211504993 can be used for the research of colon cancer .
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-
- 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 .
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-
- HY-160962
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
SM1044 is a dihydroartemisinin (DHA) dimer. SM1044 activates caspase, induces apooptosis in RL95-2 and KLE cells. SM1044 inhibits proliferations of cancer cells RL95-2, KLE, HEC-50, HEC-1-A, HEC-1-B, AN3CA, with IC50 < 3.6 μM . SM1044 inhbits tumor growth in RL95-2 xenograft mouse model .
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- HY-P992021
-
|
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Transmembrane Glycoprotein
|
Cancer
|
|
WM-A1-3389 is an anti-human IGSF1monoclonal antibody and tumor growth inhibitor. WM-A1-3389 specifically binds to the C-terminus of IGSF1, increases secretion of Granzyme B, IFN−γ, and TNF−α, and inhibits growth of colon cancer or biliary tract cancer in xenogeneic or allogeneic mouse implantation models. WM-A1-3389 can be used for the research of colon cancer, biliary tract cancer, and head and neck cancer .
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-
- HY-155195
-
|
|
FLT3
|
Cancer
|
|
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .
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-
- HY-143286A
-
|
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PROTACs
FLT3
|
Cancer
|
|
PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader，with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells，can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia .
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-
- HY-161630
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
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-
- HY-182059
-
|
|
Glutathione S-transferase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GSTP1-IN-1 is a selective GSTP1 inhibitor with an IC50 of 0.79 μM and a Kd of 0.63 μM. GSTP1-IN-1 inhibits the proliferation of gastric cancer cells, induces ROS production and depletes glutathione. GSTP1-IN-1 achieves systemic exposure and is well tolerated in xenograft mouse models, while inhibiting tumor growth. GSTP1-IN-1 can be used in gastric cancer-related research .
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-
- HY-175318S
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-161520
-
|
|
Glucocorticoid Receptor
NF-κB
|
Inflammation/Immunology
|
|
Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model .
|
-
- HY-161631
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
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-
- HY-149677
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
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-
- HY-P992439
-
|
|
CXCR
|
Cancer
|
|
PF-06747143 is recombinant anti-human antibody targeting CXCR4. PF-06747143 blocks CXCL12-induced calcium flux, F-actin polymerization, chemotaxis, cell migration, and leukemic cell bone marrow homing. PF-06747143 reduces tumor burden and improves survival in mouse models of hematologic malignancies. PF-06747143 can be used for the research of chronic lymphocytic leukemia, acute myeloid leukemia, and hematologic malignancies .
|
-
- HY-144777
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
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-
- HY-159739
-
|
|
Androgen Receptor
|
Cancer
|
|
M17-B15 is an androgen receptor dimerization inhibitor with an IC50 of 30 nM. M17-B15 effectively disrupts AR self-association, thereby suppressing AR signaling. M17-B15 exhibits extraordinary anti- prostate cancer (PCa) efficacy in vitro and in mouse xenograft tumor models.M17-B15 can be used for the study of prostate cancer .
|
-
- HY-10823
-
|
GW1843; 1843U89; OSI-7904
|
Thymidylate Synthase
DNA/RNA Synthesis
|
Cancer
|
|
OSI-7904L (GW1843; 1843U89; OSI-7904) is a thymidylate synthase (TS) inhibitor with a Ki of 90 pM. OSI-7904L blocks de novo synthesis of thymidine nucleotides, DNA synthesis and induces cell death. OSI-7904L inhibits the growth of human cells, induces tumor regression, and achieves durable antitumor effects in mouse xenograft models. OSI-7904L can be used in research related to colon adenocarcinoma .
|
-
- HY-181849
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma .
|
-
- HY-155780
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- HY-180880
-
|
|
Apoptosis
|
Cancer
|
|
TFAP2β modulator-1 (compound A6) is a potent TFAP2β modulator that promotes TFAP2β condensation by inducing conformational changes in the intrinsically disordered region. TFAP2β modulator-1 promotes TFAP2β condensation, induces apoptosis, and exhibits anti-tumor functions in esophageal squamous cell carcinoma (ESCC) cells, mouse models, and organoids. TFAP2β modulator-1 can be used for ESCC research .
|
-
- HY-129602
-
|
|
PROTACs
STAT
Apoptosis
|
Cancer
|
|
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 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-179578
-
|
|
Enolase
AMPK
Autophagy
Apoptosis
mTOR
Caspase
|
Metabolic Disease
Cancer
|
|
SU212 is a podophyllotoxin-derived ENO1 inhibitor and AMPK activator. SU212 can selectively induce oxidative phosphorylation, reduce glycolysis activity and glucose uptake in tumor cells, and directly bind to ENO1 without affecting these pathways in normal cells. SU212 induces apoptosis and promotes ENO1 degradation via proteasomal and autophagic pathways without inhibiting the catalytic activity. SU212 leads to mitotic arrest and apoptosis in TNBC (triple-negative breast cancer) cells by activating AMPK, demonstrating potent anti-tumor activity in vitro. SU212 inhibits tumor growth and metastasis in syngeneic, xenograft, and diabetic mouse models, exhibiting an excellent safety profile. SU212 can be used in research on t TNBC, diabetes, and fatty liver disease .
|
-
- 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-159838
-
|
EI‐1071
|
c-Fms
Amyloid-β
|
Neurological Disease
Cancer
|
|
Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer .
|
-
- HY-185098
-
|
|
PD-1/PD-L1
Transmembrane Glycoprotein
|
Cancer
|
|
PD1-PDL1-IN-4 (compound 19) is a potent and orally active PD1-PDL1 inhibitor that modulates TIGIT and PD-1 signalling pathways. PD1-PDL1-IN-4 can rescue CD8 + T cell and mouse splenocyte proliferation. PD1-PDL1-IN-4 inhibits tumor growth in a CT26 syngeneic colon adenocarcinoma mouse model. PD1-PDL1-IN-4 can be used for research on colon cancer .
|
-
- HY-170510
-
|
|
Galectin
|
Cancer
|
|
GB2095 is an orally active and selective galectin-3 inhibitor. GB2095 shows superior selectivity for both human (KD = 0.036 μM) and mouse galectin-3 (KD = 0.35 μM) over other galectins (such as h-Gal-1/4N/4C/8N/8C/9N/9C and m-galectin-1). GB2095 inhibits tumor growth in syngeneic mouse models of breast and melanoma cancers. GB2095 can be used for breast and melanoma cancer research .
|
-
- HY-183257
-
|
|
Autophagy
Beclin1
Reactive Oxygen Species (ROS)
p97
|
Cancer
|
|
ATI-1 is an autophagy initiation inhibitor. ATI-1 targets valosin-containing protein (VCP/p97, disrupts its interaction with UFL1, impairs UFMylation homeostasis associated with VCP, promotes polyubiquitination and degradation of Beclin1, and blocks the formation of early autophagosomes. ATI-1 induces synergistic death of autophagy-dependent malignant tumor cells under nutrient deprivation conditions, accompanied by decreased mitochondrial membrane potential, reduced ROS levels and lysosomal stress. ATI-1 exhibits anti-tumor efficacy in a pancreatic adenocarcinoma xenograft mouse model. ATI-1 can be used for the research of pancreatic adenocarcinoma and lung cancer .
|
-
- HY-181869
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia .
|
-
- HY-P992146
-
|
MYTX-011 Antibody; Q-397
|
ADC Antibody
c-Met/HGFR
|
Cancer
|
|
Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-182700
-
|
|
Complement System
VEGFR
|
Cancer
|
|
NRPa-308 is a potent and orally active Neuropilin-1 (NRP-1) antagonist with an IC50 of 42 μM for inhibiting VEGF-A165 binding to NRP-1. NRPa-308 blocks the specific interaction between VEGF-A165 and NRP-1. NRPa-308 effectively suppresses angiogenesis in vitro and in vivo and reduces the viability of a broad spectrum of human solid and haematological cancer cells. NRPa-308 inhibits tumor growth and prolongs median survival in a human breast cancer xenograft mouse model. NRPa-308 can be used for the research of multiple human malignancies including solid tumors and hematological cancers .
|
-
- HY-147081A
-
|
AGRO-100 sodium
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium 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 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-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-176149
-
|
|
CaMK
MMP
AMPK
Apoptosis
Autophagy
|
Cancer
|
|
Fluoxetine-Conjugated Platinum(IV) prodrug-1 (Compound 8) is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research .
|
-
- 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-107811R
-
|
|
Apoptosis
Monoamine Oxidase
Autophagy
α-synuclein
Mitosis
Reference Standards
|
Neurological Disease
Cancer
|
|
Harmol (Standard) is the analytical standard of Harmol (HY-107811). This product is intended for research and analytical applications. Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol can induce cell mitosis, Autophagy and Apoptosis. Harmol promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol has anti-tumor, anti-depressant and anti-aging activities. Harmol improves motor impairment in a mouse Parkinson's disease model .
|
-
- HY-148813
-
AK-2292
2 Publications Verification
|
PROTACs
STAT
|
Cancer
|
|
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 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-155781
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- 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-176457
-
|
|
Small Interfering RNA (siRNA)
MDM-2/p53
PROTACs
|
Cancer
|
|
ZS3-046 is a TAF1 PROTAC degrader. ZS3-046 promotes the ubiquitination and degradation of TAF1. ZS3-046 activates p53 and induces apoptosis in acute myeloid leukemia (AML) cells. ZS3-046 has antitumor activity in an AML tumor xenograft mouse model. (Target protein ligand (HY-176467); CRBN ligase (HY-41547); Linker (HY-176469); CRBN ligase + Linker (HY-176470)) .
|
-
- HY-183791A
-
-
- HY-175332
-
|
|
Apoptosis
Bcl-2 Family
Caspase
MDM-2/p53
|
Cancer
|
|
Apoptosis inducer 43 is an apoptosis inducer. Apoptosis inducer 43 can induce apoptosis, SubG0-G1 cell cycle arrest, secondary necrosis, and upregulate caspase-3, p53, and Bax/Bcl-2 expression in HCT116 cells. Apoptosis inducer 43 can inhibit tumor growth in a solid Ehrlich carcinoma (SEC) mouse model. Apoptosis inducer 43 can be used to study cancers such as colon cancer, leukemia, and non-small cell lung cancer .
|
-
- HY-P991664
-
|
|
Src
Akt
ERK
TAM Receptor
c-Met/HGFR
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers .
|
-
- HY-146755
-
|
|
Trk Receptor
|
Cancer
|
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
|
-
- HY-179321
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC4 Degrader-1 (compound SCT-1) is a potent and selective PROTAC HDAC4 degrader. PROTAC HDAC4 Degrader-1 reduces HDAC4 protein level, induces S phase cell cycle arrest, and inhibits cell colony formation, thereby inhibiting proliferation of the tumor cells. PROTAC HDAC4 Degrader-1 exhibits efficacy in a H460 mouse model. PROTAC HDAC4 Degrader-1 can be used for cancer research, such as lung cancer .
|
-
- HY-171030
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Pro-GA is a γ-glutamyl cyclotransferase (GGCT) inhibitor. Pro-GA inhibits the enzymatic activity of GGCT, disrupts glutathione homeostasis, induces the production of mitochondrial ROS, and upregulates the expression of p21, p27 and p16 in cells. Pro-GA inhibits the growth of cancer cells, induces cell cycle arrest and cellular senescence. Pro-GA exerts anti-tumor effects in breast cancer xenograft mouse models. Pro-GA can be used in research related to bladder cancer and breast cancer .
|
-
- HY-120031
-
|
|
STAT
PARP
Apoptosis
|
Cancer
|
|
NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer .
|
-
- HY-P1408
-
|
|
Integrin
VEGFR
|
Cancer
|
|
Obtustatin is a non-RGD disintegrin consisting of 41 residues. Obtustatin inhibits the adhesion of α1β1 integrin to type IV Collagen (HY-NP003), blocks α1β1 integrin signaling in endothelial cells, and suppresses FGF2-induced angiogenesis. Obtustatin inhibits tumor progression in mouse models and upregulates VEGF expression in sarcoma-bearing mice. Obtustatin can be used in research related to Lewis lung carcinoma and S-180 sarcoma .
|
-
- HY-179466
-
|
|
Microtubule/Tubulin
Apoptosis
Caspase
|
Cancer
|
|
BKT300 is a potent and selective protein regulator of cytokinesis 1 (PRC1) inhibitor. BKT300 inhibits PRC1 dephosphorylation at T481, disrupts actin and microtubule formation, induces G2/M cell cycle arrest, triggers mitotic catastrophe, and promotes apoptosis, thereby inhibiting proliferation and migration of acute myeloid leukemia (AML) cells while sparing normal cells. BKT300 inhibits tumor growth in mouse xenograft AML models. BKT300 can be used for the research of AML .
|
-
- HY-146461
-
|
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
|
-
- HY-179615
-
|
|
Apoptosis
Bcl-2 Family
Survivin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Entadamide A-CO-C12 is an Entadamide A (HY-N12125) derivative with potent anti-cancer activity, particularly against breast cancer cell lines. Entadamide A-CO-C12 promotes apoptosis, suppresses migratory ability, sphere formation, and stem-like cell populations. Entadamide A-CO-C12 inhibits tumor growth in a 4T1 mouse model. Entadamide A-CO-C12 can be used for the research of breast cancer .
|
-
- HY-181668
-
|
|
ULK
|
Cancer
|
|
ULK1-IN-4 (compound 12i) is a ULK1 inhibitor with an IC50 of 4.7 μM against human ULK1, and it exhibits selectivity for Aurora A/Aurora B kinases. ULK1-IN-4 forms a covalent bond with the thiol group of the Cys182 residue of ULK1, thereby inhibiting the kinase activity of ULK1. ULK1-IN-4 inhibits the growth of colorectal cancer cells and exerts tumor-suppressive activity in a mouse model of colorectal cancer .
|
-
- HY-180913
-
|
|
Connective Peptide
|
Cancer
|
|
FQI2-34 is an orally active TFCP2 (LSF) small molecule allosteric inhibitor. FQI2-34 directly binds to the LSF protein (Ki = 63 nM), inhibits the oligomerization of LSF, efficiently suppresses the transcriptional activity of LSF (IC₅₀ = 48 nM), and interferes with the SF-DNA interaction. FQI2-34 exhibits significant anti-proliferative activity against Huh7 cells and induces tumor regression in mouse models. FQI2-34 can be used for research on liver cancer .
|
-
- HY-162688
-
|
|
Telomerase
G-quadruplex
Apoptosis
Ferroptosis
|
Others
|
|
Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model .
|
-
- HY-P992487
-
|
|
Claudin
Fc Receptor (FcR)
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
ZL-1211 is an anti-CLDN18.2 monoclonal antibody. ZL-1211 exhibits enhanced binding affinity to CD16A. ZL-1211 induces ADCC-mediated cell lysis and triggers the production of IFNγ, TNFα and IL6. ZL-1211 promotes antibody-dependent cellular cytotoxicity. ZL-1211 exerts anti-tumor activity in a mouse xenograft model of gastric cancer. ZL-1211 can be used for the research of gastric cancer .
|
-
- HY-168589
-
|
|
Apoptosis
Cytochrome P450
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
|
-
- HY-182619
-
|
|
PPAR
|
Cancer
|
|
PPARα/δ antagonist-1 is an orally active, highly selective dual antagonist of PPARα/δ, with IC50 values of 0.113 μM and 0.025 μM against human PPARα and PPARδ, respectively. PPARα/δ antagonist-1 exhibits an excellent in vitro activity profile and preliminary efficacy in mouse tumor models. PPARα/δ antagonist-1 can be used in studies related to cancers (melanoma metastasis, ovarian cancer) .
|
-
- HY-178472
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker) .
|
-
- HY-119024
-
|
|
SHP1
STAT
|
Cancer
|
|
BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8 + T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields .
|
-
- HY-177338
-
|
|
STING
Cyclic GMP-AMP Synthase
IFNAR
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
STING agonist-45 is a selective STING agonist (EC50 = 0.28 μM). STING agonist-45 activates the innate immune response through the cGAS-STING pathway, upregulating key markers such as p-TBK1 and IRF3. STING agonist-45 exhibits robust STING activation in human peripheral blood mononuclear cells (PBMCs), inducing the production of type I interferons (such as IFN-β) and downstream cytokines (such as TNF-α and IL-6). STING agonist-45 enhances anti-tumor immunity, inhibits tumor growth, and increases CD8 + T cell infiltration in mouse models. STING agonist-45 is promising for the study of STING-related diseases .
|
-
- HY-181599
-
|
|
Mitochondrial Metabolism
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
Caspase
Bcl-2 Family
Atg8/LC3
|
Cancer
|
|
XAN-5 is a mitochondrial DNA G-quadruplex (mtG4) ligand with a Kd of 3.8 μM. XAN-5 selectively binds and stabilizes mtG4 structures, disrupting mitochondrial gene transcription and DNA replication. XAN-5 triggers mitochondrial dysfunction, ROS overproduction, G0 phase arrest and caspase-dependent apoptosis. XAN-5 inhibits autophagy and induces immunogenic cell death. XAN-5 inhibits tumor growth in a mouse liver cancer model while enhancing tumor-infiltrating CD4 + and CD8 + T cells. XAN-5 targets two cancer resistance mechanisms simultaneously. XAN-5 can be used for the research of liver cancer .
|
-
- HY-N2199
-
|
|
Apoptosis
Autophagy
PI3K
JNK
mTOR
p38 MAPK
CDK
MMP
TGF-beta/Smad
STAT
β-catenin
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
|
Inflammation/Immunology
Cancer
|
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
|
-
- HY-175455
-
|
|
PROTACs
Androgen Receptor
Akt
|
Cancer
|
|
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .
|
-
- HY-181663
-
|
|
PD-1/PD-L1
JAK
|
Cancer
|
|
PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3 +CD8 + and CD3 +CD4 + cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer .
|
-
- HY-100543R
-
|
ICI-118551 (Standard)
|
Adrenergic Receptor
Reference Standards
Apoptosis
Caspase
Bcl-2 Family
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Zenidolol (ICI-118551) (Standard) is the analytical standard of Zenidolol (HY-100543). This product is intended for research and analytical applications. Zenidolol is a selective β2-adrenergic receptor antagonist with Ki values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research.
|
-
- HY-15163
-
|
TG02; SB1317
|
JAK
CDK
FLT3
|
Cancer
|
|
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
|
-
- HY-139062
-
|
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
|
-
- HY-P991004
-
|
LB-101
|
CD47
PD-1/PD-L1
|
Cancer
|
|
Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
|
-
- HY-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
|
-
- HY-180805
-
|
|
Hexokinase
Mitophagy
Apoptosis
GLUT
|
Cancer
|
|
HK2-IN-3 (compound 12) is a potent hexokinase 2 (HK2) inhibitor with an IC50 of 56.4 nM. HK2-IN-3 reduces glucose uptake and downregulated GLUT1/GLUT4 in oral squamous cell carcinoma (OSCC). HK2-IN-3 induces mitophagy and apoptosis. HK2-IN-3 suppresses tumor growth and angiogenesis in OSCC xenograft mouse models. HK2-IN-3 can be used for OSCC research .
|
-
- HY-16468
-
|
MSI-1256; ENT-01 free acid
|
Bacterial
HBV
FAK
Dengue Virus
|
Infection
Neurological Disease
Cancer
|
|
Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson ,s disease mouse models .
|
-
- HY-179468
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-49 (compound B16) is a potent and selective STAT3 inhibitor. STAT3-IN-49 binds to the SH2 domain of STAT3, thereby suppressing its phosphorylation and nuclear translocation. STAT3-IN-49 inhibits triple-negative breast cancer (TNBC) cell migration, invasion, and colony formation. STAT3-IN-49 inhibits tumor growth in an MDA-MB-231 xenograft mouse model. STAT3-IN-49 can be used for TNBC research .
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-
- HY-172888
-
|
|
Endogenous Metabolite
Sialyltransferase
FAK
Integrin
|
Cancer
|
|
SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50 = 3.59 μM). SPP-037 inhibits integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 inhibits cancer cell proliferation, migration and exhibits antiangiogenic activity. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used for the research of triple-negative breast cancer .
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-
- HY-P991447
-
|
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VISTA
|
Cancer
|
|
Anti-VSIR/VISTA Antibody (SG7) is a human monoclonal antibody (mAb) targeting VISTA/B7-H5. Anti-VSIR/VISTA Antibody (SG7) inhibits VISTA function and prevents PSGL-1 and VSIG3 from binding to VISTA. Anti-VSIR/VISTA Antibody (SG7) has anti-tumor activity in the mouse B16F10 melanoma model. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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-
- HY-181816
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-60 is the counterpart of the small-molecule immuno-probe [ 18F] LG‑8, and the two together enable integrated immuno-diagnosis and therapy. PD-1/PD-L1-IN-60 exhibits potent anti-tumor activity in mouse models of melanoma and lung cancer with high PD‑L1 uptake. PD-1/PD-L1-IN-60 can be used for relevant research on melanoma and lung cancer .
|
-
- HY-175454
-
|
|
DNA/RNA Synthesis
PDGFR
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Cancer
|
|
YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibits tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research .
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-
- HY-176537
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) .
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- HY-70006A
-
|
TOK-001 hydrochloride; VN-124-1 hydrochloride
|
Molecular Glues
Androgen Receptor
MNK
Cytochrome P450
Apoptosis
|
Cancer
|
|
Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research [1][2].
|
-
- HY-P11253
-
|
|
VISTA
|
Inflammation/Immunology
|
|
DOTA-Bn-CA-170 is a molecular probe targeting the VISTA protein, with a Kd value of 0.124 nM. DOTA-Bn-CA-170 is formed by covalently linking the p-SCN-Bn-DOTA ligand with CA-170 (HY-101093). DOTA-Bn-CA-170 labeled with [ 68Ga]Ga successfully achieves specific and high-contrast PET imaging of VISTA expression in various tumor-bearing mouse models. DOTA-Bn-CA-170 can be used for the study of VISTA-targeted immunotherapy .
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-
- HY-162873
-
|
|
MEK
Raf
|
Cancer
|
|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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-
- HY-175820
-
|
|
VEGFR
ERK
Apoptosis
EGFR
|
Cancer
|
|
AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer .
|
-
- HY-P11756
-
|
|
ASCT
|
Cancer
|
|
P-LPK is a dodecapeptide that specifically targets SLC1A5, which is highly expressed on the membrane of colorectal cancer cells, with a Kd value of 1.19 μM. P-LPK has no intrinsic cell proliferation regulatory activity. Gallium-68-labeled P-LPK selectively accumulates at colorectal cancer tumor sites in xenograft mouse models. P-LPK can serve as a targeted carrier to deliver Camptothecin (HY-16560) to colorectal cancer cells, forming the conjugate P-LPK-CPT. P-LPK can be used in the research of colorectal cancer .
|
-
- HY-109061R
-
|
YH25448 (Standard); GNS-1480 (Standard)
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
Reference Standards
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
|
-
- HY-170855A
-
|
|
PROTACs
RET
|
Cancer
|
|
YW-N-7 (TFA) is a PROTAC that targets both the inhibition and degradation of RET kinase, with a DC50 of 88 nM. YW-N-7 (TFA) exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse tumor model and can be used in the area of cancer (Structure: red part represents the target protein ligand: HY-170856; blue part represents the E3 ligase ligand: HY-1708557; black part represents the linker; E3 ligase ligand + linker: HY-170858) .
|
-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
|
-
- HY-174979
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Dac590 is an orally active and selective obesity-associated protein (FTO) inhibitor with an IC50 of 6.06 nM. Dac590 shows highly selective over ALKBH5 and ALKBH3. Dac590 suppresses oncogenic FTO signaling, induces myeloid differentiation, G1-phase cell cycle arrest, and apoptosis in acute myeloid leukemia (AML) cells. Dac590 inhibits xenograft tumor growth and prolongs survival in acute myeloid leukemia mouse models with no observed toxicity. Dac590 can be used for the research of AML .
|
-
- HY-175714
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
STING agonist-46 is an orally active STING agonist. STING agonist-46 activates the STING signaling pathway, promoting phosphorylation of TBK1 and IRF3, and secretion of IFN-β and IP-10. STING agonist-46 directly binds to STING and increases its thermal stability. STING agonist-46 demonstrates potent anti-tumor efficacy in B16F10, CT26, and 4T1 mouse models. STING agonist-46 can be used for cancer immunotherapy studies .
|
-
- HY-109061BR
-
|
YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
|
Reference Standards
|
Cancer
|
|
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
|
-
- HY-179370
-
|
|
Apoptosis
Akt
|
Cancer
|
|
EEF1A2-IN-1 is a potent and covalen EEF1A2 inhibitor. EEF1A2-IN-1 exhibits selective antiproliferative activity against osteosarcoma (OS) cells. EEF1A2-IN-1 induces apoptosis by inhibiting EEF1A2 and downregulating the AKT signaling pathway. EEF1A2-IN-1 inhibits tumor growth in a xenograft mouse model. EEF1A2-IN-1 can be used for the research of OS .
|
-
- HY-142870
-
|
|
Pyruvate Carboxylase (PC)
Apoptosis
β-catenin
ERK
Wnt
|
Cancer
|
|
ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer .
|
-
- HY-179045
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
ERα degrader 14 (Compound B7) is a potent ERα degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer .
|
-
- HY-70006
-
|
TOK-001; VN-124-1
|
Molecular Glues
Androgen Receptor
MNK
Cytochrome P450
Apoptosis
|
Cancer
|
|
Galeterone (TOK-001) is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research [1][2].
|
-
- HY-175805
-
|
|
EGFR
HDAC
Apoptosis
|
Cancer
|
|
EGFR/HDAC-IN-2 (Compound 38) is dual-functional inhibitor of EGFR and HDAC3 with IC50s of 20.34 and 1.09 nM for CDK9 and HDAC3, respectively. EGFR/HDAC-IN-2 has superior anti-proliferative activity against cancer cells, inhibits cell migration and induces late-stage cell apoptosis. EGFR/HDAC-IN-2 significantly inhibits triple-negative breast cancer (TNBC) tumor growth in xenograft mouse models. EGFR/HDAC-IN-2 can be used for cancers like TNBC research .
|
-
- HY-153321
-
|
NX-5948; BTK-IN-24
|
PROTACs
Btk
|
Inflammation/Immunology
Cancer
|
|
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
|
-
- 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-P990858
-
|
|
CD47
|
Cancer
|
|
Anti-CD47 Antibody (B6.H12) is a kind of mouse IgG1 κ chimeric antibody, targeting to human CD47. Anti-CD47 Antibody (B6.H12) blocks CD47 interactions with SIRPα. Anti-CD47 Antibody (B6.H12) inhibits cell proliferation, cell migration and invasion. Anti-CD47 Antibody (B6.H12) increases macrophage phagocytosis. Anti-CD47 Antibody (B6.H12) shows potent anti-tumor effect in various tumor models, such as osteosarcoma .
|
-
- HY-P99916
-
|
AMG-427
|
FLT3
CD3
TNF Receptor
|
Inflammation/Immunology
Cancer
|
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
|
-
- HY-178989
-
|
|
Phosphoglycerate Kinase (PGK)
Cuproptosis
|
Cancer
|
|
PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma .
|
-
- HY-156096
-
|
|
HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
|
-
- HY-181877
-
|
|
HDAC
Adenosine Receptor
|
Cancer
|
IHCH-3185 is an orally active class I HDAC inhibitor (HDAC1 IC50 =102.9 nM) and A2AR antagonist (A2AR Ki =7.6 nM). IHCH-3185 reverses immune gene silencing by inducing histone acetylation and blocks the adenosine signaling pathway to relieve T-cell suppression. IHCH-3185 exhibits antiproliferative activity, induces cell cycle arrest, and significantly improves the tumor microenvironment. IHCH-3185 reduces the proportion of regulatory T cells, increases the CD8 +/Treg ratio, and upregulates the expression of key factors such as H2-K1, Cxcl9 and Cxcl10. IHCH-3185 shows significant antitumor potential in CT26 and MC38 mouse tumor models and is suitable for related cancer research .
|
-
- HY-P990953
-
|
Gen1047
|
CD3
|
Cancer
|
|
Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
|
-
- HY-175846
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
|
TQFL13 is derivative of Thymoquinone (TQ) (HY-D0803) with potent anti-breast cancer activity. TQFL13 exhibits higher cytotoxicity against breast cancer cells (BT549, MDA-MB-231, 4T1). TQFL13 increases apoptosis and blocks the cell cycle at S and G2/G1 phases in breast cancer cells. TQFL13 shows dose-dependent anti-tumor efficacy in mouse breast cancer allograft model. TQFL13 can be used for the study of breast cancer .
|
-
- HY-180200
-
|
|
Ras
ERK
|
Cancer
|
|
RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
|
-
- HY-178777
-
|
|
PROTACs
BCL6
|
Cancer
|
|
BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker) .
|
-
- HY-P992082
-
|
|
VEGFR
|
Cancer
|
|
Anti-Human/Rat VEGF Antibody (A.4.6.1) is an antibody targeting human and rat vascular endothelial growth factor (VEGF) that potently inhibits tumor growth in various animal models. Anti-Human/Rat VEGF Antibody (A.4.6.1) is the parent antibody of Bevacizumab (HY-P9906), and it exhibits high affinity and high selectivity for binding to human VEGF . The isotype control for Anti-Human/Rat VEGF Antibody (A.4.6.1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
- HY-W276819
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-9 (Compound M2) is an inhibitor for polo-like kinase 1 (PLK1), that inhibits PLK proteins modified with peptides 1010pT, cdc25c and PBIP, with IC50s of 1.6, 0.8 and 1.4 μM, respectively. PLK1-IN-9 inhibits proliferations of cancer cells HeLa, HL60, SNU387/499, HepG2, exhibits cytotoxicity and induces apoptosis. PLK1-IN-9 inhibits tumor growth in HepG2 xenograft mouse model .
|
-
- HY-182242
-
|
|
c-Myc
|
Cancer
|
|
AGB-374 is an orally active NDUFS7 inhibitor. AGB-374 destabilizes NDUFS7 protein and inhibits oxidative phosphorylation by targeting mitochondrial complex I. AGB-374 reduces MYC protein levels in colon cancer cells in vivo and delays tumor growth in syngeneic mouse models of colon cancer. AGB-374 synergistically enhances the cytotoxicity of copper chelators against cancer cells. AGB-374 cooperates with copper chelators to downregulate MYC and NDUFS7 protein levels in cancer cells. AGB-374 can be used for the research of colon cancer .
|
-
- HY-181669
-
|
|
Histone Acetyltransferase
c-Myc
|
Cancer
|
|
P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma .
|
-
- HY-175646
-
|
|
Acyltransferase
mTOR
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
|
AGPAT4-IN-1 (Compound CL26) is a covalent AGPAT4 inhibitor with an IC50 of 795 nM. AGPAT4-IN-1 covalently binds to AGPAT4 at Cys 228 and significantly inhibits acyltransferase activity, LPA-to-PA conversion and downstream mTOR/S6K pathways. AGPAT4-IN-1 sensitizes hepatocellular carcinoma (HCC) tumors to Sorafenib (HY-10201) and significantly induces apoptosis with a synergistic response. AGPAT4-IN-1 has antitumor activity and reduces tumorigenicity and stemness in HCC xenograft mouse models .
|
-
- HY-182016
-
|
|
PROTACs
ATM/ATR
Checkpoint Kinase (Chk)
Apoptosis
DNA/RNA Synthesis
Caspase
Bcl-2 Family
MDM-2/p53
|
Cancer
|
|
PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer .
|
-
- HY-129085
-
|
C5OH
|
Drug Derivative
Apoptosis
NF-κB
|
Cancer
|
|
5-Methyl cromolyn (C5OH) disodium, an analog of Cromolyn (HY-B1619), is a S100P inhibitor. 5-Methyl cromolyn disodium inhibits the binding of S100P to its receptor RAGE, NF-κB activity and cell proliferation, and promotes Gemcitabine (HY-17026)-induced apoptosis. 5-Methyl cromolyn disodium reduces tumor growth and metastasis, and prolongs survival in mouse models of syngeneic PDAC. 5-Methyl cromolyn disodium can be used for pancreatic cancer like pancreatic ductal adenocarcinoma (PDAC) research .
|
-
- HY-169478
-
|
|
Liposome
|
Cancer
|
|
Lipid N2-3L is an ionizable cationic lipid (pKa = 8.99) that can be used to generate supramolecular lipid nanoparticles (SMLNPs) for mRNA delivery. Lipid nanoparticles formed by encapsulating a luciferase reporter gene with Lipid N2-3L were detected to accumulate in the lymph nodes of mice, indicating that they can effectively enter the mouse immune system. Lipid nanoparticles formed by encapsulating ovalbumin mRNA and the TLR7/8 agonist Resiquimod (HY-13740) with Lipid N2-3L were able to reduce tumor volume and increase survival in the MC-38-OVA mouse colon cancer model. Lipid N2-3L can be used in the research of drug delivery for cancer-related therapies .
|
-
- HY-182759
-
|
|
DNA Alkylator/Crosslinker
Topoisomerase
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer .
|
-
- HY-112817
-
|
8-Oxo-Deoxyguanosine triphosphate
|
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
|
-
- HY-179049
-
|
|
EGFR
Microtubule/Tubulin
Akt
ERK
Autophagy
Atg8/LC3
p62
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
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EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer .
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- HY-153321A
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(R,R)-NX-5948; (R,R)-BTK-IN-24
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Drug Isomer
PROTACs
Btk
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Inflammation/Immunology
Cancer
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(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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- HY-120281
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MEK
PI3K
Akt
Apoptosis
Caspase
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Cancer
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ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
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- HY-181871
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Trk Receptor
Akt
ERK
Apoptosis
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Cancer
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DZX19 (Compound C02) is an orally active, selective TRK inhibitor with a TRKA IC50 value of 1.32 nM, a TRKB IC50 of 2.28 nM, and a TRKC IC50 of 4.05 nM. DZX19 inhibits the kinase activities of wild-type TRKA, TRKA mutants (G595R, F589L, G667C), wild-type TRKB, and wild-type TRKC, and suppresses the phosphorylation of TRKA as well as its downstream AKT and ERK signaling pathways. DZX19 induces apoptosis. DZX19 inhibits tumor growth in a colorectal cancer xenograft mouse model. DZX19 is applicable for the research of colorectal cancer .
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- HY-137936
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Antibiotic
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Infection
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Terrecyclic acid is a sesquiterpene originally isolated from A. terreus with antibiotic and anticancer activity. It is active against S. aureus, B. subtilis, and M. roseus (MICs=25, 50, and 25 μg/mL, respectively). Terrecyclic acid induces a heat shock response, increases levels of reactive oxygen species (ROS), and inhibits NF-κB activity and cell growth in 3T3-Y9-B12 cells.2 In vivo, terrecyclic acid (0.1, 1, and 10 mg/ml) reduces the number of ascitic fluid tumor cells in a mouse model of P388 murine leukemia.
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- HY-182288
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STAT
Apoptosis
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Cancer
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YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer .
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- HY-180885S
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Ras
ERK
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Cancer
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KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .
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- HY-176942
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ROS1-IN-3
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ROS Kinase
Trk Receptor
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Cancer
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YP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1 G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC) .
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- HY-161641
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
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- HY-183013
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PROTACs
PARP
Apoptosis
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Cancer
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PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer .
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- HY-181065
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Epigenetic Reader Domain
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Cancer
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LS-170 is a YEATS2 YEATS domain inhibitor with an IC50 of 0.14 μM. LS-170 displays selectivity for the YEATS2 YEATS domain over other YEATS domain family members and other epigenetic 'reader' and 'eraser' proteins. LS-170 reduces chromatin occupancy of the Ada-two-A-containing (ATAC) complex, decreases ATAC-dependent histone acetylation levels, and downregulates expression of ATAC-governed genes. LS-170 suppresses tumor growth in a lung cancer mouse model. LS-170 can be used for the research of non-small cell lung cancer .
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- HY-N4308
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Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone
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NF-κB
IKK
Bcl-2 Family
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Cancer
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Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma .
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- HY-183674
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|
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Molecular Glues
MEK
Raf
PERK
Ras
p38 MAPK
Apoptosis
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Cancer
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MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer .
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- HY-178451
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|
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Apoptosis
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Cancer
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NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research .
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- HY-179631
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|
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Apoptosis
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Cancer
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2DG-ODDA is a 2-deoxyglucose (2-DG) (HY-13966) derivative with potent antitumor activity. 2DG-ODDA induces apoptosis, and reduces ATP production. 2DG-ODDA is taken up through both fatty acid and glucose transporters and is cleaved by α-Mannosidase (HY-P2950), releases 2DG to inhibit N-glycosylation and disrupt cellular metabolism. 2DG-ODDA inhibits tumor growth in a 4T1 mouse model. 2DG-ODDA can be used for the research of triple-negative breast cancer (TNBC) .
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- HY-169830
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|
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Drug Derivative
Apoptosis
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Cancer
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2-(Cyclohexylmethyl)-plumbagin is a derivative of the naphthoquinone compound Plumbagin (HY-N1497). Under nutrient-deprived conditions, 2-(Cyclohexylmethyl)-plumbagin selectively exhibits cytotoxicity against PANC-1 human pancreatic cancer cells (PC50 = 0.11 µM) and reduces the phosphorylation of Akt and mTOR in PANC-1 cells. 2-(Cyclohexylmethyl)-plumbagin also induces apoptosis (Apoptosis) in PANC-1 cells at a concentration of 1 µM. Additionally, 2-(Cyclohexylmethyl)-plumbagin reduces tumor volume and weight in a xenograft MiaPaCa-2 pancreatic cancer mouse model .
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- HY-182644
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Toll-like Receptor (TLR)
NF-κB
TNF Receptor
Interleukin Related
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Cancer
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SMU-Z1 is a TLR1/2 heterodimer agonist with an EC50 of 4.88 nM. SMU-Z1 activates the NF-κB pathway, triggers pro-inflammatory cytokine production, and induces the generation of TNF-α, IL-1β, IL-6 and NO. SMU-Z1 promotes splenocyte proliferation and upregulates the expression of CD8 +T cells, NK cells and dendritic cells. SMU-Z1 exhibits significant anti-tumor effects in mouse leukemia models. SMU-Z1 can be used for leukemia-related research .
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- HY-148409
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Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
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Cancer
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MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
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- HY-164503
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NEP010
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EGFR
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Cancer
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Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFR wt, EGFR L858R/T790M, EGFR L858R and EGFR T790M, respectively .
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- HY-N0841
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Dihydrobrusatol; NSC310616
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Parasite
NF-κB
p38 MAPK
Phosphatase
Apoptosis
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Infection
Cancer
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Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
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- HY-P1181
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Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
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Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
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Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
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- HY-172200A
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PD-1/PD-L1
HDAC
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Inflammation/Immunology
Cancer
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PD-L1/HDAC6-IN-1 TFA is an orally active dual inhibitor of PD-L1 and HDAC6, with IC50 values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 TFA binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 TFA exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma .
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- HY-P10427
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|
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CXCR
Dengue Virus
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Neurological Disease
Inflammation/Immunology
Cancer
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DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
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- HY-172200
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PD-1/PD-L1
HDAC
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Inflammation/Immunology
Cancer
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PD-L1/HDAC6-IN-1 is an orally active dual inhibitor of PD-L1 and HDAC6, with IC50 values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma .
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- HY-178964
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PROTACs
RET
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Cancer
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PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .
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- HY-183771
-
|
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CDK
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Bcl-2 Family
Caspase
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Cancer
|
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CDK4/6-IN-28 is a potent, orally active, and selective CDK4/6 inhibitor IC50 values of 14.02 and 10.03 nM, respectively. CDK4/6-IN-28 inhibits breast cancer cell colony formation, migration, and proliferation. CDK4/6-IN-28 induces G1-phase cell cycle arrest and apoptosis in breast cancer cells. CDK4/6-IN-28 exhibits tumor inhibitory activity in breast cancer xenograft mouse models. CDK4/6-IN-28 can be used for the research of breast cancer .
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- HY-178941
-
|
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Dihydroorotate Dehydrogenase
Apoptosis
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
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DHODH-IN-32 (Compound A1) is a DHODH inhibitor. DHODH-IN-32 shows significant cytotoxicity against NCI-60 cell lines, especially being sensitive to breast cancer, prostate cancer and leukemia cell lines. DHODH-IN-32 can induce cell apoptosis by activating the Caspase pathway. DHODH-IN-32 causes G0/G1 phase cell cycle arrest and inhibits cellular metabolism by ROS. DHODH-IN-32 exhibits significant anti-tumor properties in mouse breast cancer models. DHODH-IN-32 can be used for the study of breast cancer .
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- HY-179505
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YAP
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Cancer
|
|
OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research .
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- HY-182019
-
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HDAC
SHMT
Apoptosis
Reactive Oxygen Species (ROS)
Ferroptosis
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Cancer
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HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia .
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-
- HY-160777A
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|
Galeterone 3β-imidazole dihydrochloride
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Molecular Glues
Androgen Receptor
MNK
Apoptosis
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Cancer
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VNPP433-3β (Galeterone 3β-imidazole) dihydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
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-
- HY-120825
-
|
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Apoptosis
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Keap1-Nrf2
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Cancer
|
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QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model .
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- HY-178367
-
|
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Phosphatase
Apoptosis
Caspase
PARP
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Cancer
|
|
PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research .
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- HY-178960
-
|
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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Tubulin-IN-59 (Compound 8g) is an orally active Tubulin inhibitor. Tubulin-IN-59 exhibits potent anti-proliferative activity against HCT116 colorectal cancer, HeLa cervical cancer, and HepG2 liver cancer cell lines, with its IC₅₀ value ranging from 16 to 35 nM. Tubulin-IN-59 arrests HeLa cells in the G2/M phase and induces cell apoptosis. Tubulin-IN-59 demonstrates significant anti-tumor activity in the HT29 human colon cancer mouse xenograft model. Tubulin-IN-59 can be used for the study of colorectal cancer and cervical cancer .
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-
- HY-150613
-
|
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Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
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- HY-181260
-
|
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Histone Methyltransferase
Apoptosis
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Cancer
|
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PRMT5-MTA-IN-8 is an orally active PRMT5-MTA complex inhibitor (IC50 = 4.4 nM). PRMT5-MTA-IN-8 inhibits the intracellular production of symmetric dimethylarginine (SDMA) as well as the proliferation of MTAP-deficient cells. PRMT5-MTA-IN-8 exerts antitumor efficacy by inhibiting PRMT5, reducing SDMA levels and inducing tumor cell apoptosis in mouse models of triple-negative breast cancer. PRMT5-MTA-IN-8 can be used in research related to cancers such as triple-negative breast cancer .
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- HY-160777
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Galeterone 3β-imidazole
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Molecular Glues
Androgen Receptor
MNK
Apoptosis
|
Cancer
|
|
VNPP433-3β (Galeterone 3β-imidazole) is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β induces cell apoptosis. VNPP433-3β inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
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-
- 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.
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-
- HY-178391
-
|
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ROS Kinase
p38 MAPK
ERK
Apoptosis
|
Cancer
|
|
SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .
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- HY-181943
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|
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Acyltransferase
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Cancer
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|
SPT-IN-2 is an orally active serine palmitoyltransferase (SPT) inhibitor (with an IC50 of 0.71 nM against human SPT2). SPT-IN-2 inhibits ceramide synthesis, suppresses cancer cell growth, and exhibits in vivo anti-tumor activity, favorable metabolic stability and cell membrane permeability in xenograft mouse models. SPT-IN-2 blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide levels and the levels of 3-ketodihydrosphingosine (3-KDS), the immediate downstream product of SPT. SPT-IN-2 can be used in research related to lung adenocarcinoma, acute promyelocytic leukemia and breast cancer .
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- HY-181152
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|
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FGFR
|
Cancer
|
|
FGFR3-IN-11(compound B11) is a Fibroblast growth factor receptor 3 (FGFR3) inhibitor with a Ka value of 4.8 μM. FGFR3-IN-11 induces apoptosis, suppresses colony formation, and causes dose-dependent G0/G1 cell cycle arrest in cancer cells. FGFR3-IN-11 exerts anticancer activity against cancer cells with minimal toxicity toward normal hepatocytes and demonstrates tumor growth suppression in xenograft mouse models. FGFR3-IN-11 can be used for the research of hepatocellular carcinoma .
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-
- HY-182382
-
|
|
Apoptosis
MDM-2/p53
Caspase
|
Cancer
|
|
Anticancer agent 311 is an apoptosis inducer and p53 modulator. Anticancer agent 311 increases p53 levels, activates cleaved caspase-3, reduces p-Cdc25C levels, and disrupts p-p44/42 MAPK phosphorylation. Anticancer agent 311 induces G2/M phase arrest, inhibits cancer cell viability in a concentration- and time-dependent manner, and exhibits low toxicity to non-cancer cells. Anticancer agent 311 prevents tumor growth and angiogenesis in mouse xenograft models without detectable toxicity. Anticancer agent 311 can be used for the research of lung cancer .
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- HY-160777B
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Galeterone 3β-imidazole hydrochloride
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Molecular Glues
Androgen Receptor
MNK
Apoptosis
|
Cancer
|
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VNPP433-3β (Galeterone 3β-imidazole) hydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
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-
- HY-164411
-
|
|
c-Met/HGFR
|
Cancer
|
|
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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- HY-P10323
-
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Tumstatin (74-98), human
|
Integrin
FAK
mTOR
Apoptosis
|
Cancer
|
|
T7 Peptide is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma .
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-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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-
- HY-N18106
-
|
|
EBV
|
Cancer
|
|
Amygdalinic acid (Compound 3) is a glycoside. Amygdalinic acid can be isolated from Persicae Semen. Amygdalinic acid inhibits Epstein-Barr virus early antigen activation. Amygdalinic acid delays two-stage chemical carcinogenesis in mouse skin, reduces papilloma incidence .
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-
- HY-179382
-
|
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FLT3
Apoptosis
|
Cancer
|
|
HSB401 is an orally active FLT3 inhibitor (IC50: 28, 5, 72, 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, FLT3-ITD, respectively). HSB401 downregulates FLT3 signaling and induces cell cycle arrest and apoptosis. HSB401 spares c-KIT inhibition, thereby reducing the risk of myelosuppression. HSB401 significantly suppresses tumor growth in the MV4-11 xenograft mouse model. HSB401 can be used for the research of acute myeloid leukemia .
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-
- HY-P10323A
-
|
Tumstatin (74-98), human TFA
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Integrin
FAK
mTOR
Apoptosis
|
Cancer
|
|
T7 Peptide TFA is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide TFA inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide TFA induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide TFA is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma .
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-
- HY-144088
-
ZYF0033
2 Publications Verification
HPK1-IN-22
|
MAP4K
|
Inflammation/Immunology
Cancer
|
|
ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
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-
- HY-161785
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
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-
- HY-W142432
-
|
|
Biochemical Assay Reagents
β-catenin
Wnt
Arginase
TGF-beta/Smad
mTOR
Akt
ERK
Atg8/LC3
p62
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
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-
- HY-105369
-
|
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Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
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-
- HY-179430
-
|
|
Mps1
|
Cancer
|
|
TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer .
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-
- HY-172934
-
|
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Toll-like Receptor (TLR)
NO Synthase
PROTACs
|
Inflammation/Immunology
Cancer
|
|
FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8 + T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity. (Pink: target protein TLR7/8 agonist 1 ligand (HY-103698); black: linker (HY-172936); blue: FR-β ligand (HY-172935)) .
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-
- HY-180485
-
|
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PROTACs
Wee1
CDK
|
Cancer
|
|
PROTAC D16-M1P2 is an orally active PKMYT1 PROTAC degrader with a DC50 of 0.7 nM. PROTAC D16-M1P2 also inhibits the activity of PKMYT1 with an IC50 of 7.6 nM. PROTAC D16-M1P2 inhibits pCDK1 with an IC50 of 9 nM. PROTAC D16-M1P2 has demonstrated significant anti-tumor efficacy in mouse models and can be used for research on breast cancer .
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-
- HY-182743
-
|
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AMPK
MARK
YAP
|
Cancer
|
|
OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC50 values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer .
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- HY-13559A
-
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Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate
|
STAT
Apoptosis
Caspase
Interleukin Related
Autophagy
Reactive Oxygen Species (ROS)
Atg8/LC3
p62
JAK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
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- HY-13559
-
|
Azaspirane ; SKF 106615-12; SKF 106615A12
|
STAT
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
p62
Atg8/LC3
PARP
NF-κB
PERK
JAK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
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- HY-P1181A
-
|
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Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
|
|
Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
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- HY-175547
-
|
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PROTACs
MAP4K
ERK
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)) .
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- HY-181687
-
|
|
HSP
CDK
|
Cancer
|
|
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
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-
- HY-P10427A
-
|
|
CXCR
Dengue Virus
|
Infection
|
|
DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
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-
- HY-110102
-
|
Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615
|
JAK
STAT
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Caspase
Atg8/LC3
p62
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
|
-
- HY-W725179
-
|
|
EBV
|
Cancer
|
|
VK-2019 is an orally bioavailable selective inhibitor of EBNA1. By binding to the protein-DNA interface to interfere with the recruitment and anchoring of the viral DNA replication machinery, VK-2019 effectively blocks the replication and proliferation of EBV in latently infected cells. VK-2019 reduces the copy number and gene expression level of Epstein-Barr virus in tumor cells, decreases the number of EBER-positive cells, and exhibits significant antiviral, immunomodulatory and antiproliferative activities. VK-2019 successfully inhibits tumor growth in EBV-dependent xenograft models. VK-2019 has favorable systemic exposure and acceptable safety profiles, and is widely used in research on advanced nasopharyngeal carcinoma and various EBV-associated cancers .
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-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
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-
- HY-181906
-
|
|
PROTACs
Reactive Oxygen Species (ROS)
CDK
|
Cancer
|
|
ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC) .
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-
- HY-112817A
-
|
8-Oxo-Deoxyguanosine triphosphate trisodium
|
Apoptosis
|
Others
|
|
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP trisodium solution (100mM) acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP trisodium solution (100mM) causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP trisodium solution (100mM) in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP trisodium solution (100mM) is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
|
-
- HY-178343
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
|
-
- HY-179374
-
|
|
Aurora Kinase
HDAC
Apoptosis
|
Cancer
|
|
Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model .
|
-
- HY-185206
-
|
|
PROTACs
Itk
NF-κB
|
Cancer
|
|
BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma .
|
-
- HY-151411
-
|
|
RUNX
|
Cancer
|
|
RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model .
|
-
- HY-156566
-
|
|
PROTACs
Epigenetic Reader Domain
HSP
|
Cancer
|
|
PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .
|
-
- HY-B1341
-
|
Enidrel; SC-4642; NSC 15432
|
Endogenous Metabolite
Progesterone Receptor
|
Cancer
|
|
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
|
-
- HY-168715
-
|
|
SHP2
Apoptosis
MAPKAPK2 (MK2)
|
Cancer
|
|
SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
|
-
- HY-183329
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-92, an analog of KX-01 (HY-10340), is a potent orally active tubulin polymerization inhibitor that binds tubulin with a Ka of 1.29 μM. Tubulin polymerization-IN-92 simultaneously occupies the colchicine site in β-tubulin and a cavity in α-tubulin. Tubulin polymerization-IN-92 exerts antiproliferative activity, induces G2/M cell cycle arrest and apoptosis in cancer cells. Tubulin polymerization-IN-92 inhibits tumor growth in mouse xenograft models. Tubulin polymerization-IN-92 can be used for the research of colon cancer, cervical cancer, and Paclitaxel (HY-B0015)-resistant ovarian cancer .
|
-
- HY-157228
-
|
|
PROTACs
Ras
|
Cancer
|
|
ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
|
-
- HY-180281
-
|
|
Zinc Finger Protein
Apoptosis
PI3K
Akt
|
Cancer
|
|
PLAGL2-IN-1 is a inhibitor of pleiomorphic adenoma-like protein 2 (PLAGL2) with a Kd of 2.23 µM. PLAGL2-IN-1 suppresses PLAGL2 transcriptional activity, induces G0/G1 cell cycle arrest, and apoptosis, thereby inhibiting hepatocellular carcinoma (HCC) cell proliferation. PLAGL2-IN-1 disrupts extracellular matrix organization and suppresses the PI3K-AKT pathway by reducing AKT phosphorylation. PLAGL2-IN-1 inhibits tumor growth in an HCCLM3 xenograft mouse model. PLAGL2-IN-1 can be used for the research of HCC .
|
-
- HY-180277
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC50 of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 (DC50 > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML) .
|
-
- 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 .
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-
- HY-181842
-
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PARP
ERK
Apoptosis
|
Cancer
|
|
PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer .
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-
- HY-180117
-
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MMP
STAT
Apoptosis
|
Cancer
|
|
MMP-2/9-IN-2 (Compound 6k) is a MMP-2 and MMP-9 inhibitor, with IC50 values of 29.27 and 24.87 μM respectively. MMP-2/9-IN-2 exhibits good selective toxicity against multiple human hepatoma cell lines. MMP-2/9-IN-2 induces cell cycle arrest and apoptosis, significantly inhibits cell migration and invasion. MMP-2/9-IN-2 inhibits the phosphorylation of the STAT3 signaling pathway. MMP-2/9-IN-2 shows strong anti-tumor activity in a nude mouse xenograft model of HepG2 liver cancer cells .
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-
- HY-N13009
-
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Raf
HIF/HIF Prolyl-Hydroxylase
ERK
MEK
Reactive Oxygen Species (ROS)
Apoptosis
Caspase
|
Cancer
|
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MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in
EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer .
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- HY-158726
-
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Fluorescent Dye
Apoptosis
|
Cancer
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Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model .
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-
- HY-170968
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EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
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- HY-178819
-
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Integrin
Drug Intermediate
|
Cancer
|
|
NM-001 is a theranostic prodrug that targets ανβ3 integrin. NM-001 consists of cRGD and GFLG peptides, a DCM fluorophore and Chlorambucil (HY-13593). NM-001 internalizes into lysosomes of tumor cells via the cRGD peptide, and generates NM-002 (HY-178820) and Chlorambucil through intracellular cleavage at the GFLG peptide by overexpressed Cathepsin B (CTSB). NM-001 exhibits green fluorescence under physiological conditions, and converts to NIR fluorescence by CTSB activation. NM-001 has significant antitumor activity with low toxicity in HeLa cell xenografts mouse models. NM-001 can be used for real-time drug release monitoring research .
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- HY-156296
-
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CDK
Apoptosis
|
Cancer
|
|
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .
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-
- HY-173147
-
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CDK
|
Cancer
|
|
CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer .
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-
- HY-159912
-
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YAP
|
Cancer
|
|
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
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-
- HY-N0538
-
|
Xylite
|
Environmental Pollutants
Endogenous Metabolite
Bacterial
Autophagy
Atg7
Atg8/LC3
|
Metabolic Disease
Cancer
|
|
Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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-
- HY-P992005
-
|
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Transmembrane Glycoprotein
|
Cancer
|
|
DS-1055a is an anti-human GARP antibody. DS-1055a effectively depletes GARP-positive regulatory T cells in the tumor microenvironment, and activates effector T cells. DS-1055a exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .
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-
- HY-13032B
-
|
GSK 525762C; I-BET 762 besylate
|
Epigenetic Reader Domain
ERK
|
Cancer
|
|
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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-
- HY-P992056
-
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Autophagy
|
Cancer
|
|
Anti-Human/Mouse LY6E Antibody (9B12) is a high-affinity, multi-target antibody that binds specifically to LY6E. Anti-Human/Mouse LY6E Antibody (9B12) binds specifically to cell-surface LY6E and enters lysosomes via lipid raft-dependent endocytosis, thereby effectively inhibiting the growth of various LY6E-expressing solid tumors (such as breast cancer and lung cancer) in both in vitro and in vivo models. Anti-Human/Mouse LY6E Antibody (9B12) exerts a dual mechanism of action: on one hand, it blocks the interaction between PILRα and CD8α, specifically reduces the survival rate of peripheral CD8 + T cells and induces their activation, breaking the state of cellular quiescence; on the other hand, it recognizes and immunoprecipitates IDE under both non-denaturing and denaturing conditions, which is applicable to studies on the subcellular localization and protein interactions of IDE. The regulatory effect of Anti-Human/Mouse LY6E Antibody (9B12) on CD8 + T cells strictly depends on the presence of PILRα, and it does not affect CD4 + T cells or T cell development in the thymus, exhibiting high specificity .
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- HY-181797
-
|
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Amyloid-β
CD47
|
Cancer
|
|
CL121 is a Glutaminyl Cyclase inhibitor with an IC50 of 0.07 μM against human sQC and an IC50 of 0.54 μM against human gQC. CL121 reduces the level of pyroglutamate (pE)-modified CD47 on the surface of cancer cells. CL121 exhibits anti-tumor activity against triple-negative breast cancer .
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-
- HY-116940
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Sm4
1 Publications Verification
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Oct3/4
Notch
STAT
|
Cancer
|
|
Sm4 is a selective and orally active SOX18 inhibitor. Sm4 inhibits SOX18-DNA binding (IC50 = 97.5 μM); Sm4 disrupts the SOX18-RBPJ protein-protein interaction (IC50 = 42.3 μM). Sm4 blocks SOX18 DNA binding, disrupts multiple SOX18 protein-protein interactions with RBPJ, DDX1, DDX17, ILF3, SOX7 and STAT1, modulates SOX18 chromatin binding dynamics. Sm4 exerts anti‑angiogenic and anti‑lymphangiogenic effects, reduces tumor vascular density, triggers vascular defects in zebrafish, prolongs survival in mouse metastatic cancer models. Sm4 can be used for the research of breast cancer .
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-
- HY-170935
-
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SRPK
PARP
Caspase
Apoptosis
Autophagy
|
Cancer
|
|
SRSF1-IN-1 is a SRSF1 inhibitor. SRSF1-IN-1 inhibits SRSF1 expression, thereby modulating the splicing of Bcl-x pre-mRNA. SRSF1-IN-1 inhibits the proliferation of various cancer cells. SRSF1-IN-1 induces apoptosis in gastric cancer cells, reduces Bcl-xl expression, and upregulates cleaved PARP and caspase 3. SRSF1-IN-1 induces autophagy and promotes cell death. SRSF1-IN-1 exhibits anti-tumor activity in a mouse gastric cancer xenograft model. SRSF1-IN-1 can be used for the research of various cancers including liver cancer, gastric cancer, breast cancer, colon cancer, glioma, and melanoma .
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-
- HY-168954
-
|
|
c-Fms
Apoptosis
Akt
ERK
STAT
|
Inflammation/Immunology
Cancer
|
|
CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22% .
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-
- HY-183784
-
|
|
P2X Receptor
FAK
MMP
|
Cancer
|
|
P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research .
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-
- HY-P992209
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Anti-CD318/CDCP1 Antibody (25A11) is an anti-CDCP1 antibody. Anti-CD318/CDCP1 Antibody (25A11) drives the internalization of antibody-CDCP1 complexes, inhibits cancer cell migration and invasion, and blocks downstream migration/invasion signaling pathways. When conjugated with saponin, Anti-CD318/CDCP1 Antibody (25A11) mediates the killing of prostate cancer cells. When conjugated with saponin, this antibody acts as an immunotoxin to inhibit the growth and metastasis of primary prostate tumors in mouse xenograft models. Anti-CD318/CDCP1 Antibody (25A11) is applicable to prostate cancer-related research .
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-
- HY-W142432S
-
|
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Isotope-Labeled Compounds
Biochemical Assay Reagents
β-catenin
Wnt
Arginase
TGF-beta/Smad
mTOR
Akt
ERK
Atg8/LC3
p62
Autophagy
|
Metabolic Disease
|
|
Perfluoroundecanoic acid- 13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
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-
- HY-172878
-
|
|
Small Interfering RNA (siRNA)
HDAC
Apoptosis
|
Cancer
|
|
HDAC/PSMD14-IN-1 (Compound 8B) is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research .
|
-
- HY-176134
-
|
|
PROTACs
Ras
|
Cancer
|
|
RP03707 is a PROTAC degrader of KRAS G12D. RP03707 forms a ternary complex with KRAS G12D and the CRBN E3 ligase, promoting the ubiquitination and proteasomal degradation of KRAS G12D. RP03707 inhibits the growth of KRAS G12D-positive tumor cells .
|
-
- HY-162275
-
|
|
Histone Demethylase
Histone Methyltransferase
STAT
|
Cancer
|
|
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
|
-
- HY-181924
-
|
|
MAP4K
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
HPK1-IN-68 (Compound 39) is a HPK1 inhibitor with an IC50 of 2.8 nM. HPK1-IN-68 blocks HPK1 signaling, inhibits HPK1-mediated phosphorylation of SLP76, and promotes the production of the IL-2 cytokine. HPK1-IN-68 antagonizes the immunosuppressive effect mediated by PGE2. HPK1-IN-68 enhances the infiltration of CD3 +/CD8 + T cells into tumor tissues. HPK1-IN-68 exerts T cell-dependent antitumor efficacy in a mouse colon cancer model. HPK1-IN-68 exhibits significant synergistic antitumor effects when used in combination with anti-PD-1. HPK1-IN-68 is applicable to research related to colon cancer .
|
-
- HY-182083
-
|
|
PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer .
|
-
- HY-W768347
-
|
Xylite-13C5
|
Isotope-Labeled Compounds
Bacterial
Autophagy
Endogenous Metabolite
Atg8/LC3
Atg7
|
Cancer
|
|
Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
|
-
- HY-10201
-
Sorafenib
Maximum Cited Publications
283 Publications Verification
Bay 43-9006
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
STAT
Akt
MMP
Cadherin
p38 MAPK
ERK
MEK
PI3K
PARP
Bcl-2 Family
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
|
-
- HY-183246
-
|
|
PAK
Cdc42-binding kinase
|
Cancer
|
|
Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr 423/Thr 402/Thr 436 and Ser 141/Ser 144/Ser 154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer .
|
-
- HY-183607
-
|
|
STING
PD-1/PD-L1
IFNAR
Interleukin Related
CXCR
|
Cancer
|
|
SMU-3k is a STING activator and PD-L1 inhibitor, with a PD-L1 IC50 of 106 nM, a KD of 386 nM for human PD-L1, and a KD of 352 nM for murine PD-L1. SMU-3k activates the STING pathway, induces phosphorylation of TBK1 and IRF3, and promotes the expression of IFN-β, IL-6 and CXCL10. SMU-3k blocks the PD-1/PD-L1 interaction, reduces PD-L1 levels and induces PD-L1 internalization. Through dual immunomodulation, SMU-3k exerts synergistic tumor growth inhibitory effects in a mouse colon cancer model. SMU-3k can be used for the research of colon cancer .
|
-
- HY-174984
-
|
|
p97
Caspase
p62
|
Cancer
|
|
VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma .
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-
- HY-159922
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
|
-
- HY-10201A
-
|
Bay 43-9006 tosylate
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
STAT
Akt
MMP
Cadherin
p38 MAPK
ERK
MEK
PI3K
PARP
Bcl-2 Family
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
|
-
- HY-182356
-
|
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
|
MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .
|
-
- HY-185565
-
|
|
PD-1/PD-L1
CXCR
|
Cancer
|
|
PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma .
|
-
- HY-174086
-
|
|
Glutathione Peroxidase
Ferroptosis
ROS Kinase
PROTACs
|
Cancer
|
|
PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC50: 5.32 nM). PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC50 values are 0.09, 2.97, and 7.58 μM, respectively). PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193); blue: E3 ligase ligand (HY-1035960); black: linker (HY-W013907); E3 ligase ligand + linker (HY-174087)) .
|
-
- HY-163985
-
|
|
PROTACs
FGFR
Apoptosis
|
Cancer
|
|
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
|
-
- HY-154974
-
|
|
Liposome
|
Cancer
|
|
LNP Lipid-8 (11-A-M) is an ionizable single-tail multi-head lipid that can be used as a lipid nanoparticle (LNP) to deliver siRNA to T cells without targeting ligands. LNP Lipid-8 is more selective for T cells than other cell types such as hepatocytes. LNP Lipid-8 selectively delivers siRNA/sgRNA to T cells (especially CD8+ T cells) through endogenous lipid transport pathways, and can enter cells and release RNA through endocytosis to achieve gene silencing. LNP Lipid-8 loaded with GFP siRNA (siGFP) significantly led to GFP gene silencing in mouse models. LNP Lipid-8 showed good efficacy and safety in both cells and animals, without obvious liver targeting and toxicity. LNP Lipid-8 can be used for RNA delivery research in the fields of tumor immunotherapy and T cell-mediated autoimmune diseases .
|
-
- HY-168894
-
|
|
Ferroptosis
JAK
STAT
p38 MAPK
AMPK
GSK-3
Apoptosis
HSP
TNF Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
CT-1 is a secreted protein belonging to the IL-6 cytokine family. Overexpression of CT-1 enhances cell proliferation, migration and angiogenesis via the ADMA/DDAH pathway. CT-1 inhibits the growth of triple-negative breast cancer cells by simultaneously inducing Ferroptosis in N2-type tumor-associated neutrophils and cancer cells. CT-1 activates the Jak/STAT-3, p42/p44 MAPK and AMPK pathways, and inhibits GSK-3β activity through phosphorylation to induce cardiomyocyte hypertrophy. CT-1 enhances the viability of cardiomyocytes and neurons, reduces cell Apoptosis, induces the expression of heat shock proteins (HSP) and BNP, and inhibits TNF levels. CT-1 exerts anti-tumor activity in mouse models of triple-negative breast cancer. CT-1 improves cognitive impairment in mice. CT-1 is applicable to the research of ischemic heart disease, triple-negative breast cancer, myocardial hypertrophy, Parkinson's disease, hypertensive heart disease, myocardial infarction, acute Chagas cardiomyopathy, high-fat diet-induced cognitive impairment and diabetes-related cognitive impairment .
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-
- HY-182360
-
|
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PERK
Eukaryotic Initiation Factor (eIF)
Bcl-2 Family
Apoptosis
Reactive Oxygen Species (ROS)
STING
DNA/RNA Synthesis
PD-1/PD-L1
|
Cancer
|
|
Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer .
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-
- HY-155887
-
|
DSPE-PEG-NH2, MW 3400 ammonium
|
Liposome
|
Cancer
|
|
DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
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-
- HY-175236
-
|
|
PD-1/PD-L1
Apoptosis
ERK
JNK
Cadherin
p38 MAPK
GSK-3
IFNAR
Caspase
Bcl-2 Family
|
Cancer
|
|
SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research .
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-
- HY-178032
-
|
|
PARP
Apoptosis
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
STING
|
Cancer
|
|
PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy .
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-
- HY-179623
-
|
|
PI3K
mTOR
Akt
CDK
Cadherin
|
Cancer
|
|
PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer .
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-
- HY-136765
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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-
- HY-175369
-
|
|
PI3K
Akt
PD-1/PD-L1
Interleukin Related
CD3
|
Inflammation/Immunology
Cancer
|
|
PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers .
|
-
- HY-179617
-
|
|
E1/E2/E3 Enzyme
Interleukin Related
|
Cancer
|
|
Cbl-b-IN-30 is an orally active Casitas B-lineage lymphoma-b (CBLB) inhibitor. Cbl-b-IN-30 specifically binds to CBLB and inhibits its E3 ubiquitin ligase activity with an IC50 of 9.1 nM. Cbl-b-IN-30 can promote IL-2 secretion (EC50 = 187.5 nM) and enhance T cell activation. Cbl-b-IN-30 exerts antitumor activity and can induce immune memory. Cbl-b-IN-30 can be used for the research of colon cancer .
|
-
- HY-130133
-
|
|
PI3K
mTOR
Akt
Apoptosis
Paraptosis
p38 MAPK
Mitochondrial Metabolism
P-glycoprotein
CDK
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research .
|
-
- HY-141439
-
|
|
Keap1-Nrf2
Quinone Reductase
Glutathione S-transferase
Apoptosis
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a Dm value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis .
|
-
- HY-N2445
-
|
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
Cancer
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
- HY-N0171A
-
|
β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
|
Bacterial
Apoptosis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
PARP
MMP
Bcl-2 Family
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
NF-κB
mTOR
Lactate Dehydrogenase
CDK
Glutathione Peroxidase
SOD
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
- HY-N0171R
-
|
β-Sitosterol (Standard); 22,23-Dihydrostigmasterol (Standard))
|
Reference Standards
Apoptosis
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (Standard) is the analytical standard of Beta-Sitosterol. This product is intended for research and analytical applications. Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
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-
- HY-N0171
-
|
|
Apoptosis
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
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-
- HY-181986
-
|
|
Lipase
Apoptosis
|
Cancer
|
|
ERX-208 is an anticancer agent that induces endoplasmic reticulum stress by targeting lysosomal acid lipase A (LIPA), ultimately leading to cancer cell apoptosis. ERX-208 can be used in ovarian cancer research .
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-
| Cat. No. |
Product Name |
Type |
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- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Fluorescent Dye
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
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-
- HY-D2062
-
|
|
Fluorescent Dye
|
|
ATTO 740 NHS ester is a near-infrared fluorescent dye and a multimodal fluorescence/photoacoustic contrast agent with excellent near-infrared emission properties and extremely high photostability. The photoacoustic signal of ATTO 740 NHS ester shows no significant decrease after continuous irradiation with a 750 nm laser for 30 min, making it suitable for in vivo fluorescence imaging and photoacoustic contrast imaging. When conjugated with the cystine knot peptide R01, ATTO 740 NHS ester enables precise detection of integrin αvβ6-positive cells and tumors in nude mouse xenograft models .
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-
- HY-158726
-
|
|
Fluorescent Dye
|
|
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model .
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| Cat. No. |
Product Name |
Type |
-
- HY-155887
-
|
DSPE-PEG-NH2, MW 3400 ammonium
|
Biochemical Assay Reagents
|
|
DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10761
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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-
- HY-P1408
-
|
|
Integrin
VEGFR
|
Cancer
|
|
Obtustatin is a non-RGD disintegrin consisting of 41 residues. Obtustatin inhibits the adhesion of α1β1 integrin to type IV Collagen (HY-NP003), blocks α1β1 integrin signaling in endothelial cells, and suppresses FGF2-induced angiogenesis. Obtustatin inhibits tumor progression in mouse models and upregulates VEGF expression in sarcoma-bearing mice. Obtustatin can be used in research related to Lewis lung carcinoma and S-180 sarcoma .
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-
- HY-P1727
-
Super-TDU
Maximum Cited Publications
6 Publications Verification
|
YAP
|
Cancer
|
|
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model .
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-
- HY-P1181A
-
|
|
Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
|
|
Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
|
-
- HY-P1181
-
|
|
Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
|
|
Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
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-
- 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-P10427
-
|
|
CXCR
Dengue Virus
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
|
-
- HY-P10323
-
|
Tumstatin (74-98), human
|
Integrin
FAK
mTOR
Apoptosis
|
Cancer
|
|
T7 Peptide is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma .
|
-
- HY-P10323A
-
|
Tumstatin (74-98), human TFA
|
Integrin
FAK
mTOR
Apoptosis
|
Cancer
|
|
T7 Peptide TFA is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide TFA inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide TFA induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide TFA is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma .
|
-
- HY-P11050A
-
|
|
Apoptosis
|
Cancer
|
|
SP94 is a peptide ligand with high specificity for hepatocellular carcinoma cells. SP94 selectively binds to multiple hepatocellular carcinoma cell lines in vitro. SP94 inhibits tumor growth in a mouse model of hepatocellular carcinoma by promoting apoptosis and reducing angiogenesis. SP94 can be used as a specific probe for hepatocellular carcinoma imaging. SP94 is useful for hepatocellular carcinoma research .
|
-
- HY-P10427A
-
|
|
CXCR
Dengue Virus
|
Infection
|
|
DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
|
-
- HY-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
|
-
- 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-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-159771
-
|
|
FAP
|
Cancer
|
|
FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.
|
-
- HY-P10947
-
|
|
Epigenetic Reader Domain
YAP
|
Cancer
|
|
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
|
-
- 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-P11253
-
|
|
VISTA
|
Inflammation/Immunology
|
|
DOTA-Bn-CA-170 is a molecular probe targeting the VISTA protein, with a Kd value of 0.124 nM. DOTA-Bn-CA-170 is formed by covalently linking the p-SCN-Bn-DOTA ligand with CA-170 (HY-101093). DOTA-Bn-CA-170 labeled with [ 68Ga]Ga successfully achieves specific and high-contrast PET imaging of VISTA expression in various tumor-bearing mouse models. DOTA-Bn-CA-170 can be used for the study of VISTA-targeted immunotherapy .
|
-
- 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-P10744
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-P11624
-
|
|
Apoptosis
|
Cancer
|
|
PP-60 is an apoptosis inducer. PP-60 inhibits the proliferation of cancer cells and induces cancer cell apoptosis. PP-60 exerts anti-tumor effects in nude mouse liver tumor models. PP-60 is applicable to research related to cancers such as liver cancer, lung cancer, and prostate cancer .
|
-
- HY-180989
-
|
|
PROTACs
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PROTAC PLK1 Degrader-2 (Compound NC1) is a PLK1 PROTAC degrader with an Kd of 6.06 μM. PROTAC PLK1 Degrader-2 significantly inhibits the proliferation of HeLa cells, induces cell cycle arrest and apoptosis. PROTAC PLK1 Degrader-2 exhibits significant anti-tumor activity in a HeLa cell xenograft tumor mouse model. PROTAC PLK1 Degrader-2 can be used for the study of cervical cancer.
|
-
- HY-P11658
-
|
Peptoid 1
|
Peptides
|
Cancer
|
|
Anticancer peptoid 1 (Peptoid 1) is a peptoid with antitumor activity. Anticancer peptoid 1 exerts cytotoxicity primarily via plasma membrane damage. Anticancer peptoid 1 exerts cytotoxicity against a broad range of cancer cell lines, including those with multidrug resistance. Anticancer peptoid 1 inhibits tumor growth in a human breast cancer xenotransplantation mouse model without noticeable acute adverse effects. Anticancer peptoid 1 can be used for the research of cancer, such as breast cancer, and prostate cancer .
|
-
- HY-P11756
-
|
|
ASCT
|
Cancer
|
|
P-LPK is a dodecapeptide that specifically targets SLC1A5, which is highly expressed on the membrane of colorectal cancer cells, with a Kd value of 1.19 μM. P-LPK has no intrinsic cell proliferation regulatory activity. Gallium-68-labeled P-LPK selectively accumulates at colorectal cancer tumor sites in xenograft mouse models. P-LPK can serve as a targeted carrier to deliver Camptothecin (HY-16560) to colorectal cancer cells, forming the conjugate P-LPK-CPT. P-LPK can be used in the research of colorectal cancer .
|
-
- HY-K6008
-
1 Publications Verification
|
|
MCE Basement Membrane Matrix HC (High Concentration) is primarily composed of natural basement membrane matrix extracted from mouse tumors, with higher content of various cytokines than the standard type.This product is mainly used for angiogenesis experiments, construction of animal models and 3D tumor models.
|
-
- HY-K6005
-
1 Publications Verification
|
|
MCE Basement Membrane Matrix HC (High Concentration, Phenol Red) is primarily composed of natural basement membrane matrix extracted from mouse tumors, with higher content of various cytokines than the standard type.This product is mainly used for angiogenesis experiments, construction of animal models and 3D tumor models.
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
(5)
-
- HY-P990148
-
|
|
VEGFR
|
Cancer
|
|
Anti-Mouse VEGF-A Antibody (2G11-2A05) is a rat-derived IgG2a κ type antibody inhibitor, tragrting to mouse VEGF-A with high affinity. Anti-Mouse VEGF-A Antibody (2G11-2A05) shows good anti-tumor effect in gastric cancer xenograft models .
|
-
(5)
-
- HY-P990117
-
|
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
|
-
(5)
-
- HY-P990116
-
|
|
Osteopontin
|
Inflammation/Immunology
|
|
Anti-Mouse osteopontin/SPP1 Antibody (103D6) is a mouse-derived anti-mouse osteopontin/SPP1 IgG2c κ type antibody inhibitor. Anti-Mouse osteopontin/SPP1 Antibody (103D6) increases cytotoxic T lymphocyte lytic activity and suppresses colon tumor growth. Anti-Mouse osteopontin/SPP1 Antibody (103D6) ameliorates liver injury in common bile duct ligation (CBDL)-induced primary sclerosing cholangitis mice models .
|
-
(5)
-
- HY-P99948
-
|
AMG-596
|
EGFR
CD3
|
Neurological Disease
Cancer
|
|
Etevritamab (AMG-596) is a bispecific T-cell engager that targets EGFRvIII and CD3. Etevritamab simultaneously binds CD3 on T cells and EGFRvIII on glioblastoma multiforme cells, thereby forming a bridge structure. Etevritamab triggers T-cell activation, proliferation, secretion of cytotoxic substances, and tumor cell lysis. Etevritamab extends overall survival and induces tumor regression in mouse models of glioblastoma multiforme. Etevritamab can be used for research related to glioblastoma .
|
-
(5)
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
(5)
-
- HY-P99943
-
|
KN-046
|
PD-1/PD-L1
CTLA-4
|
Cancer
|
|
Erfonrilimab (KN-046) is a monoclonal antibody targeting PD-L1/CTLA-4. Erfonrilimab blocks the PD-L1 and CTLA-4 pathways, thereby regulating T cell function. Erfonrilimab enhances the secretion of IL-2 in superantigen-stimulated peripheral blood mononuclear cells. Erfonrilimab inhibits tumor growth in xenograft and double gene knock-in mouse models. Erfonrilimab can be used in research related to a variety of advanced solid tumors, including non-small cell lung cancer and nasopharyngeal carcinoma.
|
-
(5)
-
- 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 .
|
-
(5)
-
- HY-P991372
-
|
RN927C antibody
|
TROP2
|
Cancer
|
|
Anti-TROP2 Antibody (RN927C antibody) is a human monoclonal antibody targeting Trop-2. Anti-TROP2 Antibody exerts in vitro inhibitory effects on a variety of tumor cell lines. Anti-TROP2 Antibody exhibits anti-tumor activity in mouse pancreatic PDX, ovarian PDX, lung PDX and triple-negative breast cancer (TNB) PDX models. Anti-TROP2 Antibody can be used for research on pancreatic cancer, ovarian cancer, lung cancer and triple-negative breast cancer .
|
-
(5)
-
- HY-P990858
-
|
|
CD47
|
Cancer
|
|
Anti-CD47 Antibody (B6.H12) is a kind of mouse IgG1 κ chimeric antibody, targeting to human CD47. Anti-CD47 Antibody (B6.H12) blocks CD47 interactions with SIRPα. Anti-CD47 Antibody (B6.H12) inhibits cell proliferation, cell migration and invasion. Anti-CD47 Antibody (B6.H12) increases macrophage phagocytosis. Anti-CD47 Antibody (B6.H12) shows potent anti-tumor effect in various tumor models, such as osteosarcoma .
|
-
(5)
-
- HY-P990789
-
|
|
CTLA-4
|
Others
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CTLA-4 Antibody (9H10) is a kind of syrian hamster IgG antibody inhibitor, targeting to CTLA-4. Anti-Mouse CTLA-4 Antibody (9H10) binds mouse CTLA-4 and blocks the interaction between CTLA-4 and its ligand. Anti-Mouse CTLA-4 Antibody (9H10) shows potent anti-tumor effect in various tumor models, such as breast and colon cancer .
|
-
(5)
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
(5)
-
- HY-P991336
-
|
INBRX-106; ES-102
|
Orexin Receptor (OX Receptor)
|
Inflammation/Immunology
Cancer
|
|
Ordastobart (INBRX-106; ES-102) is a hexavalent OX40 agonist antibody. Ordastobart enhances OX40 receptor clustering, signaling, and downstream activation, thereby increasing the proliferation and activation of CD4 + and CD8 + T cells in vitro and in vivo. Ordastobart exhibits anti-tumor effects and improves survival in mouse models of cancer. Ordastobart is indicated for research in cancers such as fibrosarcoma and colorectal cancer .
|
-
(5)
-
- HY-P99916
-
|
AMG-427
|
FLT3
CD3
TNF Receptor
|
Inflammation/Immunology
Cancer
|
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
|
-
(5)
-
- HY-P990107
-
|
|
TGF-β Receptor
|
Cancer
|
|
Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
|
-
(5)
-
- HY-P991481
-
|
|
CCR
|
Inflammation/Immunology
Cancer
|
|
S-531011 is a human IgG1 monoclonal antibody (mAb) targeting CCR8. S-531011 reduces tumor-infiltrating CCR8+ Tregs and has anti-tumor activity in CT26.WT and EMT6 tumor-bearing mouse tumor models. S-531011 can be used in the study of cancer immunity. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P990004
-
|
|
Tim3
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse TIM-3 Antibody (B8.2C12) is an anti-mouse TIM-3 IgG1 monoclonal antibody. Anti-Mouse TIM-3 Antibody (B8.2C12) can block the binding of Tim-3 with Phosphatidylserine (PtdSer) and CEACAM1 without interfering with the binding to Galectin-9. Anti-Mouse TIM-3 Antibody (B8.2C12) can inhibit tumor growth and activate tumor infiltrating CD8 + T cells. Anti-Mouse TIM-3 Antibody (B8.2C12) can be used for studying cancer such as breast cancer and colon cancer and constructing experimental autoimmune encephalomyelitis (EAE) models .
|
-
(5)
-
- HY-P990953
-
|
Gen1047
|
CD3
|
Cancer
|
|
Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
|
-
(5)
-
- HY-P990257
-
|
|
c-Fms
|
Cancer
|
|
Anti-Mouse CSF1 Antibody (5A1) is a rat-derived anti-mouse CSF1 IgG1 κ type antibody inhibitor. Anti-Mouse CSF1 Antibody (5A1) can inhibit cells proliferation and macrophage-induced invasion. Anti-Mouse CSF1 Antibody (5A1) shows potent anti-tumor effect in various tumor models, such as neuroblastoma .
|
-
(5)
-
- HY-P991230
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
MK-4830 is a fully humanized monoclonal antibody of the immunoglobulin G4 subclass that specifically binds to ILT4 and blocks its interaction with HLA-G and other ligands. MK-4830 inhibits tumor growth in humanized mouse cancer models .
|
-
(5)
-
- HY-P991057
-
|
|
CD47
|
Cancer
|
|
STI-6643 is a fully human IgG4 antibody that targets CD47. STI-6643 blocks CD47-SIRPα interaction, and enables macrophage-mediated phagocytosis of tumor cells. STI-6643 shows anti-tumor activity in mouse lymphoma xenograft models. STI-6643 can be used for the research of Burkitt's lymphoma, solid tumors, relapsed or refractory tumors, and lymphoma. The isotype control for STI-6643 can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
|
-
(5)
-
- HY-P991646
-
|
heMab
|
Transmembrane Glycoprotein
|
Cancer
|
|
ING-1 (heMab) is a high-affinity humanized monoclonal antibody against epithelial cell adhesion molecule (Ep-CAM). ING-1 is a transmembrane glycoprotein mediating Ca 2+. ING-1 binds to Ep-CAM on tumor cells and exhibits potent in vitro activity, targeting and inhibiting tumor growth and metastasis in mouse cancer models. ING-1 is useful in the research of breast, colorectal, and lung cancers, among other cancers .
|
-
(5)
-
- HY-P991664
-
|
|
Src
Akt
ERK
TAM Receptor
c-Met/HGFR
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers .
|
-
(5)
-
- HY-P991660
-
|
|
c-Met/HGFR
|
Cancer
|
|
ARGX-111 is an anti-MET antibody. ARGX-111 blocks HGF-dependent and -independent signaling, downregulating MET expression on the tumor cell surface. ARGX-111 depletes MET-expressing circulating tumor cells through enhanced antibody-dependent cell-mediated cytotoxicity (ADCC), thereby inhibiting tumor metastasis. ARGX-111 depletes circulating tumor cells and inhibits bone and lung metastasis in an orthotopic mouse model of metastatic breast cancer. ARGX-111 is promising for research in breast cancer and other cancers .
|
-
(5)
-
- HY-P991447
-
|
|
VISTA
|
Cancer
|
|
Anti-VSIR/VISTA Antibody (SG7) is a human monoclonal antibody (mAb) targeting VISTA/B7-H5. Anti-VSIR/VISTA Antibody (SG7) inhibits VISTA function and prevents PSGL-1 and VSIG3 from binding to VISTA. Anti-VSIR/VISTA Antibody (SG7) has anti-tumor activity in the mouse B16F10 melanoma model. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P991307
-
|
|
LILRB
Transmembrane Glycoprotein
|
Cancer
|
|
BND-35 is a human monoclonal antibody (mAb) targeting LILRB4/ILT3/CD85k. BND-35 blocks the interaction of ILT3 with APOE and fibronectin, enhances the pro-inflammatory activity of various myeloid cells, and reverses ILT3-mediated immunosuppression of T cells by various suppressive myeloid cells. BND-35 has anti-tumor activity in the hILT3 transgenic mouse tumor model .
|
-
(5)
-
- HY-P990259
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
(5)
-
- HY-P991663
-
|
|
Tie
|
Cancer
|
|
AMG-780 is a fully human IgG2 antibody that targets angiopoietin 1 (Ang1) (IC50 = 4.5 nM) and angiopoietin 2 (Ang2) (IC50 = 0.06 nM). AMG-780 inhibits tumor growth in the Colo205 xenograft mouse model by inhibiting both Ang1 and Ang2. AMG-780 is indicated for the research of cancers such as colon cancer .
|
-
(5)
-
- HY-P991004
-
|
LB-101
|
CD47
PD-1/PD-L1
|
Cancer
|
|
Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
|
-
(5)
-
- HY-P991464
-
|
|
TNF Receptor
|
Cancer
|
|
IBI37G5 is a human monoclonal antibody (mAb) targeting TNFRSF18/GITR/CD357. IBI37G5 has anti-tumor activity in MC38 and B16F10 mouse tumor models. IBI37G5 can be used in the study of cancer immunity .
|
-
(5)
-
- HY-P991639
-
|
|
Apoptosis
|
Cancer
|
|
BIW-8962 is a humanized anti-ganglioside GM2 antibody. BIW-8962 exhibits ADCC/CDC activity against multiple myeloma cells. BIW-8962 demonstrates potent anti-tumor activity in mouse xenograft models. BIW-8962 is indicated for research in myeloma and other cancers .
|
-
(5)
-
- HY-P991233
-
|
|
EGFR
|
Cancer
|
|
BAT1006 is a monoclonal antibody targeting HER2 extracellular domain II with enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) for the study of HER2-positive locally advanced/metastatic solid tumors. BAT1006 has an approximately 5-fold enhanced ADCC effect compared to pertuzumab (HY-P9912) and exhibits potent anti-tumor activity in the HER2-positive Calu-3 xenograft mouse model .
|
-
(5)
-
- HY-P991328
-
|
|
Notch
|
Cancer
|
|
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
|
-
(5)
-
- HY-P991310
-
|
LT3015; LT-3000
|
LPL Receptor
|
Neurological Disease
Cancer
|
|
Lpathomab (LT3015; LT-3000) is a human IgG1 monoclonal antibody (mAb) targeting LPA. Lpathomab reduces the release of IL-8 and IL-6 cytokines in SKOV3 cells and blocks LPA-triggered tumor cell migration. Lpathomab reduces neovascularization in Matrigel plug and CNV models. Lpathomab inhibits brain injury in the CCI mouse model. Lpathomab can be used in the study of brain injury, ovarian cancer, diabetic neuropathy, and spinal cord injury. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P991353
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models .
|
-
(5)
-
- HY-P991366
-
|
AL008
|
CD47
|
Cancer
|
|
IBI-397 is a human monoclonal antibody (mAb) targeting SIRPα/CD172a . IBI-397 promotes human monocyte-derived dendritic cell-mediated T cell proliferation and increases the expression of CD86 and HLA-DR. IBI-397 has antitumor activity in the mouse MDA-MB-231 tumor model. IBI-397 can be used in Myeloma research .
|
-
(5)
-
- HY-P992352
-
|
|
|
|
|
ES005 is an anti-tumor compound and LAG3 inhibitor. ES005 blocks the interactions of LAG3 with MHC-II, LSECtin and FGL1, thereby effectively reversing the LAG3-mediated inhibition of T cell activation and NFAT reporter gene expression. ES005 exhibits significant tumor growth inhibitory effects in syngeneic mouse breast tumor models using humanized LAG3 knock-in mice. ES005 can be used for breast tumor-related research .
|
-
(5)
-
- HY-P992388
-
|
|
LILRB
|
Cancer
|
|
IO-108 is a humanized IgG4 monoclonal antibody and a competitive inhibitor of LILRB2, with a KD value of 1.97 nM. IO-108 competitively blocks the binding of LILRB2 to its ligands including HLA-G, MHC-I, ANGPTL2 and SEMA4A, reprograms tumor-associated myeloid cells, drives the conversion of suppressive myeloid cells into a pro-inflammatory phenotype, and restores the cytotoxic activity of T cells and NK cells. IO-108 inhibits tumor growth in LILRB2 transgenic mouse models. IO-108 can be used for the research of solid tumors .
|
-
(5)
-
- HY-P991966
-
|
|
EGFR
|
Cancer
|
|
Anti-Human/Mouse EGFR Antibody (7A7) ia an anti-mouse EGFR monoclonal antibody proposed to be the mouse equivalent of cetuximab. Anti-Human/Mouse EGFR Antibody (7A7) fails to induce tumor regression in the HPV38 tumor model where EGFR is not expressed in mice. Anti-Human/Mouse EGFR Antibody (7A7) can be used in EGFR-expressing HPV38 tumor-related studies .
|
-
(5)
-
- HY-P992043
-
|
ANK-101
|
Interleukin Related
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Tolododekin alfa (ANK-101) is a drug conjugate that anchors and combines IL-12 with Aluminum Hydroxide (HY-B1521). Tolododekin alfa promotes the recruitment of effector CD8 + T cells to tumor sites, enhances the production of γ-interferon, upregulates the expression of PD-L1, and induces sustained pro-inflammatory gene expression in mouse tumor models. Tolododekin alfa can be used for research related to advanced solid tumors .
|
-
(5)
-
- HY-P991960
-
|
|
CTLA-4
Interleukin Related
|
Cancer
|
|
JS007 is a humanized IgG1 monoclonal antibody and also a CTLA-4 binder, with a Kd of 0.21 nM for CTLA-4. JS007 blocks the interaction between CTLA-4 and B7-1. JS007 activates T cells, promotes increased IL-2 secretion, and inhibits tumor growth in CTLA-4 knock-in mouse syngeneic tumor models. JS007 is applicable to research related to cancer and advanced solid tumors.
|
-
(5)
-
- HY-P991958
-
|
|
CTLA-4
|
Cancer
|
|
GIGA-564 is a fully human anti-CTLA4 IgG1 monoclonal antibody with a Kd of 9.8 nM. GIGA-564 binds to a unique epitope of CTLA-4, mediates FcR-dependent signaling pathways, depletes CTLA-4-highly-expressing regulatory T cells within tumors, and inhibits the proliferation of peripheral regulatory T cells. GIGA-564 exhibits anti-tumor activity in mouse models. GIGA-564 can be used for tumor research .
|
-
(5)
-
- HY-P992338
-
|
|
Mesothelin
Constitutive Androstane Receptor
|
Inflammation/Immunology
Cancer
|
|
CT-1119 is an autologous human anti-Mesothelin chimeric antigen receptor macrophage (CAR-M). CT-1119 mediates CAR-dependent, antigen-dependent functional activities. CT-1119 acts as a phagocytosis inducer, tumor cell killer, pro-inflammatory cytokine inducer, and M1 macrophage polarizer. CT-1119 exhibits stronger resistance to M2 repolarization and reduces tumor burden in a mouse lung cancer xenograft model. CT-1119 can be used for the research of mesothelin-expressing solid tumors .
|
-
(5)
-
- HY-P992441
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
PHST001 is a humanized anti-CD24 antibody. PHST001 binds cell-surface CD24, blocks CD24-Siglec10 interaction, and engages Fc receptors to promote macrophage-mediated tumor cell phagocytosis. PHST001 inhibits growth of breast cancer and ovarian cancer, and reduces metastatic lesions in mouse xenograft models. PHST001 can be used for the research of triple negative breast cancer, HER2+ breast cancer, metastatic tumors, and ovarian cancer .
|
-
(5)
-
- HY-P992032
-
|
BAY-943 antibody
|
Interleukin Related
|
Cancer
|
|
TPP-9476 is an anti-human IL3RA (CD123) monoclonal antibody with human IL3RA Kd of 11 nM and cynomolgus monkey IL3RA Kd of 16 nM. TPP-9476 binds specifically to human and cynomolgus monkey IL3RA, undergoes target-dependent internalization into lysosomes of IL3RA-positive cells.TPP-9476 exerts antiproliferative effects in IL3RA-expressing acute myeloid leukemia and classical Hodgkin lymphoma cells, reduces tumor burden, improves survival, and induces complete tumor remission in relevant xenograft mouse models .
|
-
(5)
-
- HY-P992406
-
|
|
MMP
IFNAR
|
Cancer
|
|
MEDI-3622 is a human monoclonal antibody against ADAM17. MEDI-3622 blocks the ADAM17-mediated shedding of CD16A and CD62L on NK cells, and binds with high specificity to a surface loop unique to the metalloprotease catalytic domain of ADAM17. MEDI-3622 enhances IFNγ production by NK cells when they bind to antibody-coated tumor cells. MEDI-3622 can be used in the research of ovarian cancer, Burkitt lymphoma, head and neck cancer, and colorectal cancer .
|
-
(5)
-
- HY-P992021
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
WM-A1-3389 is an anti-human IGSF1monoclonal antibody and tumor growth inhibitor. WM-A1-3389 specifically binds to the C-terminus of IGSF1, increases secretion of Granzyme B, IFN−γ, and TNF−α, and inhibits growth of colon cancer or biliary tract cancer in xenogeneic or allogeneic mouse implantation models. WM-A1-3389 can be used for the research of colon cancer, biliary tract cancer, and head and neck cancer .
|
-
(5)
-
- HY-P992439
-
|
|
CXCR
|
Cancer
|
|
PF-06747143 is recombinant anti-human antibody targeting CXCR4. PF-06747143 blocks CXCL12-induced calcium flux, F-actin polymerization, chemotaxis, cell migration, and leukemic cell bone marrow homing. PF-06747143 reduces tumor burden and improves survival in mouse models of hematologic malignancies. PF-06747143 can be used for the research of chronic lymphocytic leukemia, acute myeloid leukemia, and hematologic malignancies .
|
-
(5)
-
- HY-P992146
-
|
MYTX-011 Antibody; Q-397
|
ADC Antibody
c-Met/HGFR
|
Cancer
|
|
Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P992487
-
|
|
Claudin
Fc Receptor (FcR)
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
ZL-1211 is an anti-CLDN18.2 monoclonal antibody. ZL-1211 exhibits enhanced binding affinity to CD16A. ZL-1211 induces ADCC-mediated cell lysis and triggers the production of IFNγ, TNFα and IL6. ZL-1211 promotes antibody-dependent cellular cytotoxicity. ZL-1211 exerts anti-tumor activity in a mouse xenograft model of gastric cancer. ZL-1211 can be used for the research of gastric cancer .
|
-
(5)
- HY-P992082
-
|
|
VEGFR
|
Cancer
|
|
Anti-Human/Rat VEGF Antibody (A.4.6.1) is an antibody targeting human and rat vascular endothelial growth factor (VEGF) that potently inhibits tumor growth in various animal models. Anti-Human/Rat VEGF Antibody (A.4.6.1) is the parent antibody of Bevacizumab (HY-P9906), and it exhibits high affinity and high selectivity for binding to human VEGF . The isotype control for Anti-Human/Rat VEGF Antibody (A.4.6.1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
(5)
- HY-P992005
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
DS-1055a is an anti-human GARP antibody. DS-1055a effectively depletes GARP-positive regulatory T cells in the tumor microenvironment, and activates effector T cells. DS-1055a exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .
|
-
(5)
- HY-P992056
-
|
|
Autophagy
|
Cancer
|
|
Anti-Human/Mouse LY6E Antibody (9B12) is a high-affinity, multi-target antibody that binds specifically to LY6E. Anti-Human/Mouse LY6E Antibody (9B12) binds specifically to cell-surface LY6E and enters lysosomes via lipid raft-dependent endocytosis, thereby effectively inhibiting the growth of various LY6E-expressing solid tumors (such as breast cancer and lung cancer) in both in vitro and in vivo models. Anti-Human/Mouse LY6E Antibody (9B12) exerts a dual mechanism of action: on one hand, it blocks the interaction between PILRα and CD8α, specifically reduces the survival rate of peripheral CD8 + T cells and induces their activation, breaking the state of cellular quiescence; on the other hand, it recognizes and immunoprecipitates IDE under both non-denaturing and denaturing conditions, which is applicable to studies on the subcellular localization and protein interactions of IDE. The regulatory effect of Anti-Human/Mouse LY6E Antibody (9B12) on CD8 + T cells strictly depends on the presence of PILRα, and it does not affect CD4 + T cells or T cell development in the thymus, exhibiting high specificity .
|
-
(5)
- HY-P992209
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Anti-CD318/CDCP1 Antibody (25A11) is an anti-CDCP1 antibody. Anti-CD318/CDCP1 Antibody (25A11) drives the internalization of antibody-CDCP1 complexes, inhibits cancer cell migration and invasion, and blocks downstream migration/invasion signaling pathways. When conjugated with saponin, Anti-CD318/CDCP1 Antibody (25A11) mediates the killing of prostate cancer cells. When conjugated with saponin, this antibody acts as an immunotoxin to inhibit the growth and metastasis of primary prostate tumors in mouse xenograft models. Anti-CD318/CDCP1 Antibody (25A11) is applicable to prostate cancer-related research .
|
-
(5)
- HY-P992414
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
MS17-38 is a monoclonal antibody targeting PODXL-v2. MS17-38 binds to a specific conformational epitope of PODXL-v2 on gastric cancer cells, modulates target function, inhibits gastric cancer cell growth and migration, and blocks tumor growth and lung metastasis. MS17-38 can be used for the research of gastric cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0171A
-
|
β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
|
Cardiovascular Disease
Structural Classification
Classification of Application Fields
Leguminosae
Glycine max (L.) merr
Plants
Inflammation/Immunology
Disease Research Fields
Steroids
Source Classification
|
Bacterial
Apoptosis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
PARP
MMP
Bcl-2 Family
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
NF-κB
mTOR
Lactate Dehydrogenase
CDK
Glutathione Peroxidase
SOD
|
|
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
-
- HY-N0171
-
|
|
Cardiovascular Disease
other families
Classification of Application Fields
Leguminosae
Plants
Endogenous metabolite
Glycyrrhiza uralensis Fisch.
Inflammation/Immunology
Disease Research Fields
Steroids
Source Classification
|
Apoptosis
Endogenous Metabolite
|
|
Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
-
- HY-125850
-
-
-
- HY-N0421
-
-
-
- HY-16468
-
-
-
- HY-107811
-
-
-
- HY-N0538
-
-
-
- HY-N0841
-
-
-
- HY-N0171R
-
|
β-Sitosterol (Standard); 22,23-Dihydrostigmasterol (Standard))
|
Cardiovascular Disease
other families
Classification of Application Fields
Leguminosae
Plants
Endogenous metabolite
Glycyrrhiza uralensis Fisch.
Inflammation/Immunology
Disease Research Fields
Steroids
Source Classification
|
Reference Standards
Apoptosis
Endogenous Metabolite
|
|
Beta-Sitosterol (Standard) is the analytical standard of Beta-Sitosterol. This product is intended for research and analytical applications. Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
|
-
-
- HY-N7526
-
-
-
- HY-N2445
-
|
|
Structural Classification
Classification of Application Fields
Piperaceae
Plants
Chalcones
Flavonoids
other families
Phenols
Polyphenols
Piper methysticum G.Forst.
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
-
- HY-163001
-
|
|
Microorganisms
Source Classification
|
Autophagy
p62
Atg8/LC3
|
|
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-112817
-
|
8-Oxo-Deoxyguanosine triphosphate
|
Microorganisms
Source Classification
|
Apoptosis
|
|
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
|
-
-
- HY-N15497
-
-
-
- HY-B1341
-
|
Enidrel; SC-4642; NSC 15432
|
Structural Classification
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Endocrinology
Steroids
Source Classification
|
Endogenous Metabolite
Progesterone Receptor
|
|
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
|
-
-
- HY-N13009
-
|
|
Phenols
Polyphenols
Morus alba L.
Plants
Moraceae
Source Classification
|
Raf
HIF/HIF Prolyl-Hydroxylase
ERK
MEK
Reactive Oxygen Species (ROS)
Apoptosis
Caspase
|
|
MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in
EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer .
|
-
-
- HY-135217
-
-
-
- HY-N12044
-
-
-
- HY-N2199
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Phenols
Polyphenols
Selaginellaceae
Plants
Biflavones
Selaginella tamariscina (P. Beauv.) Spring
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Autophagy
PI3K
JNK
mTOR
p38 MAPK
CDK
MMP
TGF-beta/Smad
STAT
β-catenin
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
|
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
|
-
-
- HY-N4308
-
|
Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone
|
Flavonols
Structural Classification
Flavonoids
other families
Classification of Application Fields
Plants
Disease Research Fields
Source Classification
Cancer
|
NF-κB
IKK
Bcl-2 Family
|
|
Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma .
|
-
-
- HY-125850R
-
-
-
- HY-135217R
-
-
-
- HY-N0421R
-
|
Cinobufagine (Standard)
|
Structural Classification
Animals
Steroids
Source Classification
|
Reference Standards
Apoptosis
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
-
- HY-107811R
-
-
-
- HY-N18106
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-157029S
-
|
|
|
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-157031S
-
|
|
|
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-175318S
-
|
|
|
p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
|
-
-
- HY-13762S
-
|
|
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
-
- HY-W747797
-
|
|
|
Cinobufagine-d3 is the deuterium labeled Cinobufagin (HY-N0421). Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
-
- HY-W768347
-
|
|
|
Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
|
-
-
- HY-180885S
-
|
|
|
KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .
|
-
-
- HY-W142432S
-
|
|
|
Perfluoroundecanoic acid- 13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-129602
-
|
|
|
PROTAC Synthesis
|
|
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 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-148813
-
AK-2292
2 Publications Verification
|
|
PROTAC Synthesis
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AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 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-157029S
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Alkynes
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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 .
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Alkynes
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Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
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- HY-157031S
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Alkynes
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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 .
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- HY-129510
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Alkynes
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4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
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- HY-175421
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Alkynes
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ArMan is an aryl mannoside ligand that can be chemically functionalized onto the surface of virus-like particles (VLPs) through click chemistry. VLPs can be used to target DC-SIGN dendritic cells, promote the selective co-binding of DC-SIGN and TLR7, and lead to a Th1-type immune response. VLP-ArMan-OvaI/II can significantly inhibit tumor growth in the mouse melanoma model .
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- HY-181849
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Alkynes
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MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma .
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- HY-180200
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Alkynes
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RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
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Classification |
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- HY-N0171A
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β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
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Cholesterol
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Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
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- HY-N0171
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Cholesterol
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Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
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- HY-147081
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AS 1411
2 Publications Verification
AGRO-100
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Aptamers
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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 .
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- HY-N0538
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Xylite
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Fillers
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Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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- HY-145729
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AZD9150
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Antisense Oligonucleotides
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Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
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- HY-154974
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Cationic Lipids
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LNP Lipid-8 (11-A-M) is an ionizable single-tail multi-head lipid that can be used as a lipid nanoparticle (LNP) to deliver siRNA to T cells without targeting ligands. LNP Lipid-8 is more selective for T cells than other cell types such as hepatocytes. LNP Lipid-8 selectively delivers siRNA/sgRNA to T cells (especially CD8+ T cells) through endogenous lipid transport pathways, and can enter cells and release RNA through endocytosis to achieve gene silencing. LNP Lipid-8 loaded with GFP siRNA (siGFP) significantly led to GFP gene silencing in mouse models. LNP Lipid-8 showed good efficacy and safety in both cells and animals, without obvious liver targeting and toxicity. LNP Lipid-8 can be used for RNA delivery research in the fields of tumor immunotherapy and T cell-mediated autoimmune diseases .
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- HY-145729A
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AZD9150 sodium
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Antisense Oligonucleotides
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Danvatirsen sodium (AZD9150 sodium) is an antisense oligonucleotide targeting STAT3. Danvatirsen sodium reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen sodium inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen sodium inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen sodium achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen sodium can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
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- HY-147081A
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AGRO-100 sodium
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Aptamers
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AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium 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 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-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
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- HY-155887
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DSPE-PEG-NH2, MW 3400 ammonium
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Pegylated Lipids
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DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
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- HY-153482
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siRNAs
siRNA drugs
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ATU027 is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
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- HY-153482A
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siRNAs
siRNA drugs
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ATU027 sodium is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 sodium has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
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- HY-160061
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Aptamers
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P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model .
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- HY-169478
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Cationic Lipids
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Lipid N2-3L is an ionizable cationic lipid (pKa = 8.99) that can be used to generate supramolecular lipid nanoparticles (SMLNPs) for mRNA delivery. Lipid nanoparticles formed by encapsulating a luciferase reporter gene with Lipid N2-3L were detected to accumulate in the lymph nodes of mice, indicating that they can effectively enter the mouse immune system. Lipid nanoparticles formed by encapsulating ovalbumin mRNA and the TLR7/8 agonist Resiquimod (HY-13740) with Lipid N2-3L were able to reduce tumor volume and increase survival in the MC-38-OVA mouse colon cancer model. Lipid N2-3L can be used in the research of drug delivery for cancer-related therapies .
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- HY-112817A
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8-Oxo-Deoxyguanosine triphosphate trisodium
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Nucleotide Analogs
Guanine Nucleotide
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8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP trisodium solution (100mM) acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP trisodium solution (100mM) causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP trisodium solution (100mM) in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP trisodium solution (100mM) is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
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