Search Result
Results for "
anti-proliferation
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-129071
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Microtubule/Tubulin
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Cancer
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Vindesine sulfate is a potent tubulin inhibitor with an Ki of 0.110 µM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo .
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- HY-P2272A
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Wnt
β-catenin
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Cancer
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NLS-StAx-h TFA is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. NLS-StAx-h TFA efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h TFA shows anti-proliferation of cancer cells .
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- HY-149970
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Estrogen Receptor/ERR
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Cancer
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ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer .
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- HY-149061
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Apoptosis
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Cancer
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Anticancer agent 99 (compound 2p) has good anticancer activity against HepG2 cells, with an IC50 value of 35.9 μM. Anticancer agent 99 can induce apoptosis and has anti-proliferation effect .
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- HY-N11438
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Estrogen Receptor/ERR
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Cancer
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3'-Hydroxymirificin (compound 3) is a naural compound that can be isolated from Pueraria lobata roots. 3'-Hydroxymirificin (compound 3) possesses estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
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- HY-152468
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Apoptosis
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Cancer
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Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro .
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- HY-144314
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Estrogen Receptor/ERR
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Cancer
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PSDalpha is an ERα degrader conjugating photosensitizer (PS), triphenylamine benzothiadiazole (TB) and 17β-estradiol via an acetylene bond. PSDalpha shows excellent anti-proliferation performance on MCF-7 cells. The maximum absorption wavelength of PSDalpha in the visible region is located at 465 nm .
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- HY-N3940
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Others
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Neurological Disease
Cancer
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Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC50 values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively .
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- HY-N4272
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Others
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Cancer
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Protodeltonin is a steroidal saponin from Dioscorea zingiberensis Wright, with anti-proliferation activity .
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- HY-127103
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Apoptosis
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Cancer
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FB23-2 is a potent and selective inhibitor of mRNA N 6-methyladenosine (m 6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML) .
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- HY-N6885
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Others
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Cancer
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Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
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- HY-149726
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Histone Methyltransferase
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Cancer
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EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively) .
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- HY-161268
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- HY-14507
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DNA/RNA Synthesis
Apoptosis
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Cancer
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YK-4-279 blocks RNA Helicase A (RHA) binding with EWS-FLI1 (oncogenic protein). YK-4-279 induces apoptosis and shows anti-proliferation activities towards various cancer cells. YK-4-279 has a chiral center and it can be separated into two enantiomers. YK-4-279 can be used for the research of cancer .
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- HY-147722
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Carbonic Anhydrase
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Cancer
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hCAIX-IN-8 (compound 7i) is a potent and selective hCAIX inhibitor with IC50s of 1.99, 0.024, 1.10 µM for CAII, CAIX, CAVA respectively. hCAIX-IN-8 shows anti-proliferation activity with low toxicity. hCAIX-IN-8 decreases the epithelial to mesenchymal transitions and induces apoptosis. hCAIX-IN-8 inhibits cell migration and colonization potential .
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- HY-142946
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Ras
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Cancer
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KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo .
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- HY-146022
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PROTACs
Anaplastic lymphoma kinase (ALK)
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Cancer
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SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer .
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- HY-108391
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N-Octanoyl-D-erythro-sphingosine
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Apoptosis
PKC
Autophagy
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Inflammation/Immunology
Cancer
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C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
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- HY-155770
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FLT3
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Cancer
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FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor with IC50 values of 1 and 4 nM for FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-20 has anti-proliferation efficacy in FLT3-ITD-positive AML cell lines MV4-11 and MOLM-13 (7 and 9 nM, respectively) and the MOLM-13 variant (4 nM) with the FLT3-ITD-D835Y mutation. FLT3-IN-20 can be used in research of cancer .
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- HY-N0839
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Quillaja sapogenin
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Apoptosis
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Neurological Disease
Inflammation/Immunology
Cancer
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Quillaic acid (Quillaja sapogenin)It is an anti-gastric cancer and anti-proliferation agent that can promote apoptosis of cancer cells. (apoptosis). Quillaic acidAlso has analgesic and local anti-inflammatory activity .
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- HY-155066
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PI3K
mTOR
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Cancer
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FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
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- HY-150401
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ADC Cytotoxin
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Cancer
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Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively .
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- HY-B1360
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Chloquinan
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Antibiotic
Bacterial
Fungal
β-catenin
Apoptosis
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Infection
Cancer
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Chlorquinaldol (Chloquinan) is an antibacterial agent with the potential use in topical skin conditions and vaginal infections. Chlorquinaldol is a β-catenin/TCF4 inhibitor, showing anti-proliferation, anti-migration, and apoptosis-inducing activity in cancer cells .
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- HY-N12534
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Apoptosis
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Cancer
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Monaspin B is a natural product produced by the co-culture of Monascus purpureus and Aspergillus oryzae. Monaspin B exerts anti-proliferation activity by inducing apoptosis of HL-60 cells, IC50 160 nM. Monaspin B has antitumor activity .
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- HY-155178
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EGFR
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Cancer
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Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition .
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- HY-N0211
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EGFR
Apoptosis
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Cancer
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Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .
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- HY-144627
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PROTACs
TAM Receptor
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Cancer
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PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .
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- HY-144624
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PROTACs
TAM Receptor
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Cancer
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PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 µM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .
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- HY-151934
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Apoptosis
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Cancer
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ERK-IN-6 (compound 6g) is an potent anti-proliferation agent against esophageal squamous cell carcinoma (ESCC). ERK-IN-6 induces cell apoptosis via ERK pathway. ERK-IN-6 can be used for the research of ESCC .
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- HY-P2272
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Wnt
β-catenin
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Cancer
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NLS-StAx-h is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. NLS-StAx-h efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h shows anti-proliferation of cancer cells .
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- HY-110329
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Others
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Cancer
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ML179 (SR-1309) is a inverse LRH1 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
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- HY-101990
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Others
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Others
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IMS2186 is an antichoroidal neovascularization (CNV) reagent. IMS2186 can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. IMS2186 has no intraocular toxicity and reduces the amount of eye leakage and diseased cells .
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- HY-B0715
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BL-191; PTX; Oxpentifylline
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Phosphodiesterase (PDE)
Autophagy
HIV
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Cardiovascular Disease
Cancer
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Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
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- HY-155526
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Histone Demethylase
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Cancer
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FY-21 is a selective inhibitor of LSD1 (IC50=340 nM), with anti-proliferation and anti-colony formation activities. FY-21 enhances p53 expression, down-regulates HOXA9 and MEIS1 expression. FY-21 also induces leukemia cell differentiation to exhibts antitumor activity .
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- HY-144131
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Apoptosis
RET
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Cancer
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RET-IN-11 is a potent and selective RET inhibitor with IC50s of 6.20 nM, 18.68 nM for RET and RET V804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis .
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- HY-N9228
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Others
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Cancer
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5,7,3',4'-Tetrahydroxy-3-methoxy-8-geranylflavone is a prenylflavone with anti-proliferation effect on breast cancer cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8-geranylflavone can be isolated from an ethyl acetate-soluble extract of the barks of Broussonetia papyrifera .
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- HY-N0155
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ROR
Reactive Oxygen Species
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis .
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- HY-B0715S
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BL-191-d6; PTX-d6; Oxpentifylline-d6
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Phosphodiesterase (PDE)
Autophagy
HIV
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Cardiovascular Disease
Cancer
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Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
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- HY-B0715S2
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BL-191-d5; PTX-d5; Oxpentifylline-d5
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Phosphodiesterase (PDE)
Autophagy
HIV
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Cardiovascular Disease
Cancer
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Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
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- HY-153863
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MEK
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Cancer
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MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma .
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- HY-155072
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Btk
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Cancer
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PROTAC BTK degraders-5(compound 3e) is a selective BTK degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research 1.
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- HY-143241
-
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HDAC
MDM-2/p53
Apoptosis
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Cancer
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HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM .
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- HY-146208
-
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
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- HY-145737
-
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PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
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- HY-155727
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Sirtuin
Apoptosis
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Cancer
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Sirt1/2-IN-2 (compound hsa55) is a dual inhibitor of SIRT1/2 with IC50s of 1.8 μM (SIRT1) and 2.4 μM (SIRT2), respsectivley. Sirt1/2-IN-2 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-2 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines .
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- HY-155728
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Sirtuin
Apoptosis
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Cancer
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Sirt1/2-IN-3 (compound PS9) is a dual inhibitor of SIRT1/2 with IC50s of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respsectivley. Sirt1/2-IN-3 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-3 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines .
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- HY-145737A
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PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
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- HY-119312
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PKC
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Cancer
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C8 Dihydroceramide is a negative control of C8 Ceramide. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
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- HY-144099
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E1/E2/E3 Enzyme
Apoptosis
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Cancer
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Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity .
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- HY-N0060BS
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(E)-Coniferic acid-d3
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β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
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Cancer
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(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299[1].
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- HY-143234
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Isocitrate Dehydrogenase (IDH)
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Cancer
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mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
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- HY-N9174
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Others
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Cancer
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5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
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- HY-153359
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Others
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Cancer
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M3913 is an antitumor compound. M3913 has antiproliferation activity against cancer cells .
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- HY-146095
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
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Cancer
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p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
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- HY-154809
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Others
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Others
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(compound C-155) is a enantiomer of M3913. M3913 (HY-153359) is an antitumor compound. M3913 has antiproliferation activity against cancer cells .
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- HY-N2434
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COX
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Cancer
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[10]-Shogaol is an antioxidant from Zingiber officinale for human skin cell growth and a migration enhancer. [10]-Shogaol inhibits COX-2 with an IC50 of 7.5 μM and has antiproliferation activity .
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![[10]-Shogaol](//file.medchemexpress.com/product_pic/hy-n2434.gif)
- HY-150605
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ERK
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Cancer
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ERK5-IN-3 (compound 33j) is a potent and selective ERK5 (extracellular signal-related kinase 5) inhibitor, with an IC50 of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC50 of 31 nM .
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- HY-149261
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Autophagy
CDK
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Cancer
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H1k, a Eudistomin Y derivative, is a lysosome-targeted antiproliferation agent. H1k increases the autophagy signal and downregulate the expression of cyclin-dependent kinase (CDK1) and cyclin B1. H1k can be used in research of cancer .
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- HY-103380
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CDK
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Cancer
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NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2 .
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- HY-160530
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Wee1
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Cancer
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WEE1-IN-6 (compound 110) is a orally active WEE1 inhibitor with an DC50 value of ≦ 100 nM. WEE1-IN-6 inhibits cell proliferation .
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- HY-N0189
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Rhabarberone; 3-Hydroxymethylchrysazine
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mTOR
Influenza Virus
Apoptosis
Autophagy
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Cancer
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Aloe emodin (Rhabarberone) is a natural hydroxyanthraquinone with antitumor activities. aloe-emodin can bind with mTORC2 and inhibit its kinase activity. Aloe emodin exerts antiproliferation effects and induces cellular apoptosis . Aloe emodin also exhibits antiviral activity that against influenza A virus .
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- HY-N12617
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Bacterial
Apoptosis
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Infection
Cancer
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Bipolaricin R (Compound 6) is a compound that can be isolated from Bipolaris maydis. Bipolaricin R exhibits noticeable antimicrobial ability against Bacillus cereus, Staphylococcus aureus, and Staphylococcus epidermidis. Bipolaricin R has excellent antiproliferation and apoptosis induction effects against A549 cell line .
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- HY-147932
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Acetyl-CoA Carboxylase
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Cancer
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ACC1/2-IN-2 (compound PF-3) is a potent ACC1/2 inhibitor with IC50 values of 22 and 48 nM for ACC1 and ACC2, respectively. ACC1/2-IN-2 has antiproliferation activity and can be used for cancer research .
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- HY-145688
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HDAC
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Cancer
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HDAC-IN-33 is a potent HDAC inhibitor with IC50s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
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- HY-N10335
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FAK
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Inflammation/Immunology
Cancer
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Harringtonolide is a potent RACK1 inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities .
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- HY-154973
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Oxidative Phosphorylation
Mitochondrial Metabolism
AMPK
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Metabolic Disease
Cancer
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AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research .
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- HY-155554
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Oxidative Phosphorylation
Mitochondrial Metabolism
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Cancer
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SCAL-255 is a potent mitochondrial complex I (CI) inhibitor with IC50 of 1.14 μM. SCAL-255 blocks mitochondrial function, inhibits OCR, induces ROS production, and reduces MMP. SCAL-255 displays a considerable antiproliferation effect against oxidative phosphorylation (OXPHOS)-dependent cancer cells .
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- HY-155555
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Oxidative Phosphorylation
Mitochondrial Metabolism
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Cancer
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SCAL-266 is a potent mitochondrial complex I (CI) inhibitor with IC50 of 0.83 μM. SCAL-266 blocks mitochondrial function, inhibits OCR, induces ROS production, and reduces MMP. SCAL-266 displays a considerable antiproliferation effect against oxidative phosphorylation (OXPHOS)-dependent cancer cells .
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- HY-145687
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HDAC
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Cancer
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HDAC-IN-32 is a potent HDAC inhibitor with IC50s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
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- HY-151533
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Epigenetic Reader Domain
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Cancer
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PBRM1-BD2-IN-6 is a potent PBRM1 bromodomain inhibitor with an IC50 value of 0.22 µM. PBRM1-BD2-IN-6 shows antiproliferation activity. PBRM1-BD2-IN-6 has the potential for the research of PBRM1-dependent cancer .
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- HY-135805A
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EGFR
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Cancer
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(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor .
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- HY-148259
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Others
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Cancer
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SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC50 value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer .
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- HY-147935
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Akt
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Cancer
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NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model .
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- HY-142680
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EGFR
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Cancer
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EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8) .
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- HY-146660
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c-Myc
Epigenetic Reader Domain
Apoptosis
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Cancer
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BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .
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- HY-146136
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EGFR
Apoptosis
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Cancer
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EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis .
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- HY-155993
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PARP
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Cancer
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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 .
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- HY-162264
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Microtubule/Tubulin
Proton Pump
Apoptosis
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Inflammation/Immunology
Cancer
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Tubulin polymerization/V-ATPase-IN-1 (compound F10) is a Tubulin polymerization/V-ATPase inhibitor. Tubulin polymerization/V-ATPase-IN-1 shows robust antiproliferation activity against four human cancer cell lines, and exerts antiproliferative activity by inhibiting tubulin and V-ATPase. Tubulin polymerization/V-ATPase-IN-1 induces immunogenic cell death in addition to apoptosis, and inhibits tumor growth in an RM-1 homograft model with enhanced T lymphocyte infiltration .
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- HY-15994
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ACY241
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HDAC
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Cancer
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Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects .
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- HY-103019
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(+)-Enitociclib; (+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib
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CDK
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Cancer
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Enitociclib ((+)-Enitociclib) is an enanthiomer of BAY-1251152 with rotation (+). Enitociclib is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. Enitociclib has anti-tumour activity .
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- HY-110244
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BRK
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Cancer
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Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour .
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- HY-130538
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HDAC
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Cancer
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1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity .1-Naphthohydroxamic acid can induce tubulin acetylation .
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- HY-136427
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Nuclear Factor of activated T Cells (NFAT)
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Inflammation/Immunology
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KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity .
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- HY-135691
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c-Myc
Apoptosis
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Cancer
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hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with Kd values of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibits c-myc transcription by disrupting the binding of hnRNPK and c-myc promoter. hnRNPK-IN-1 induces Hela cells apoptosis and has strongly anti-tumor activities .
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- HY-N7385
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MMP
Apoptosis
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Cancer
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Nudol is a phenanthrene compound that has anti-cancer activity. Nudol inhibits cell proliferation, induces cell apoptosis. Nudol inhibits MMP-2M and MMP-9 activity (Ki: 988.9 nM, 1.76 μM, respectively). Nudol can be used in the research of cancers, such as osteosarcoma .
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- HY-163001
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Autophagy
p62
Atg8/LC3
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Cancer
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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 .
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- HY-150510
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Histone Methyltransferase
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Neurological Disease
Cancer
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MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
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- HY-19745
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PD-1/PD-L1
Apoptosis
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Cancer
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BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity .
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- HY-108601A
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PKC
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Neurological Disease
Inflammation/Immunology
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(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
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- HY-124748A
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Protease Activated Receptor (PAR)
Apoptosis
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Inflammation/Immunology
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ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis .
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- HY-142517
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EGFR
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Cancer
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EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively .
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- HY-133618
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Wee1
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Cancer
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Pomalidomide-C3-adavosertib is a rapid and selective Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis .
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- HY-N11643
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GA-Mk
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Apoptosis
Reactive Oxygen Species
MMP
Caspase
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Cancer
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Ganoderic acid Mk (GA-Mk) is a triterpenoid acid, that can be isolated from the mycelia of Ganoderma lucidum. Ganoderic acid Mk is efficiently anti-proliferative and can induce apoptosis of HeLa cells by mitochondria-mediated pathway. Ganoderic acid Mk can be used for cervical cancer research .
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- HY-108601
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PKC
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Inflammation/Immunology
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(S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 free base for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 free base is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
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- HY-110021
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SKF 82526 hydrochloride
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Dopamine Receptor
Histone Demethylase
Apoptosis
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Cardiovascular Disease
Cancer
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Fenoldopam (SKF 82526) hydrochloride is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam hydrochloride shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis .
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- HY-124748
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Protease Activated Receptor (PAR)
Apoptosis
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Inflammation/Immunology
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ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis .
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- HY-15456
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c-Met/HGFR
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Cancer
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NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer .
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- HY-17502
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- HY-12653
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LDC4297
5 Publications Verification
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CDK
HIV
HSV
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Infection
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LDC4297 is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 value of 0.02-1.21 μM. LDC4297 can be used for the research of infection .
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- HY-116147
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LPL Receptor
Apoptosis
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Cancer
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Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity .
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- HY-17499
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EGFR
Apoptosis
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Cancer
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EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .
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- HY-100912
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Phosphodiesterase (PDE)
Myosin
Apoptosis
Calmodulin
|
Cancer
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|
W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively . W-7 hydrochloride induces apoptosis and has antitumor activity .
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- HY-113618A
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CRAC Channel
Interleukin Related
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Cardiovascular Disease
|
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RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
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- HY-113618B
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CRAC Channel
Interleukin Related
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Cardiovascular Disease
|
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RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
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- HY-135805
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EGFR
|
Cancer
|
|
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
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-
- HY-136145
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Wnt
|
Cancer
|
|
FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities .
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-
- HY-151172
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MDM-2/p53
Apoptosis
|
Cancer
|
|
MDM2-p53-IN-15 is a MDM2-p53 inhibitor with an IC50 value of 26.1 nM. MDM2-p53-IN-15 inhibits the proliferation of various cancer cells and induces cell apoptosis. MDM2-p53-IN-15 can be used for the research of cancer .
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-
- HY-151434
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Glutaminase
Apoptosis
|
Cancer
|
|
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis .
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-
- HY-12653A
-
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CDK
HIV
HSV
|
Infection
|
|
LDC4297 hydrochloride is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection .
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-
- HY-163396
-
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EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
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-
- HY-156292
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Histone Methyltransferase
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Cancer
|
|
IHMT-EZH2-426 (compound 38) is a potent and covalent EZH2 degrader with IC50s of 1.3 nM, 1.2 nM, and 1.7-3.5 nM against EZH2 wild-type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 exhibits potent antiproliferation effects against both B-cell lymphoma and triple negative breast cancer (TNBC) cell lines by reducing the levels of H3K27me3 and EZH2 .
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-
- HY-13751A
-
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Sigma Receptor
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Inflammation/Immunology
|
|
SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase .
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-
- HY-10409
-
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TG-101348; SAR 302503
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JAK
Apoptosis
|
Cancer
|
|
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
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-
- HY-16705
-
BRD4770
2 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
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-
- HY-13751
-
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|
Sigma Receptor
|
Inflammation/Immunology
|
|
SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase .
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-
- HY-136144
-
FIDAS-5
2 Publications Verification
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities .
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-
- HY-19356A
-
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Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
|
Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity .
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-
- HY-10409A
-
|
TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
|
JAK
Apoptosis
|
Cancer
|
|
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
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-
- HY-143317
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
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-
- HY-139606
-
|
|
p97
|
Cancer
|
|
VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS) .
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-
- HY-109169
-
|
IMG-7289
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-109169A
-
|
IMG-7289 ditosylate
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
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-
- HY-143468
-
|
|
Apoptosis
MEK
|
Cancer
|
|
MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
|
-
- HY-146782
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
|
-
- HY-109169B
-
|
IMG-7289 hydrochloride
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-152099
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-19 (compound 4a) is an anti-cancer agent that exerts anti-proliferative effects on lung cancer cells by inducing apoptosis. antiproliferative agent-19 also induces cell cycle arrest in the G2/M phase .
|
-
- HY-109169C
-
|
IMG-7289 dihydrochloride
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-B0735A
-
|
Fenoldopam methanesulfonate; SKF-82526 mesylate
|
Dopamine Receptor
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Fenoldopam mesylate (SKF-82526) is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam mesylate shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis .
|
-
- HY-112724
-
|
SHR0302
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
|
-
- HY-101989
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-24 (compound HMBA) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-24 inhibits MCF-7 cells proliferation. Tubulin polymerization-IN-24 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-24 increase the GTP hydrolysis rate and inhibits microtubule assembly .
|
-
- HY-112724A
-
|
SHR0302 sulfate
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Ivarmacitinib (SHR0302) sulfate is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
|
-
- HY-19831A
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity .
|
-
- HY-15128
-
-
- HY-15154
-
NG 52
4 Publications Verification
Compound 52
|
CDK
|
Cancer
|
|
NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p .
|
-
- HY-120275
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
|
-
- HY-147368
-
|
|
Pyruvate Kinase
|
Cancer
|
|
PKM2 activator 2 (compound 28) is a pyruvate kinase M2 (PKM2) activitor with an AC50 value of 66 nM. PKM2 activator 2 can restore normal glycolytic metabolism in cells .
|
-
- HY-U00447
-
|
|
MDM-2/p53
DNA Alkylator/Crosslinker
|
Cancer
|
|
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2272A
-
|
|
Wnt
β-catenin
|
Cancer
|
|
NLS-StAx-h TFA is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. NLS-StAx-h TFA efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h TFA shows anti-proliferation of cancer cells .
|
-
- HY-P2272
-
|
|
Wnt
β-catenin
|
Cancer
|
|
NLS-StAx-h is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. NLS-StAx-h efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h shows anti-proliferation of cancer cells .
|
-
- 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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-129071
-
-
-
- HY-N3940
-
-
-
- HY-N11438
-
-
-
- HY-N4272
-
-
-
- HY-N6885
-
-
-
- HY-N0839
-
-
-
- HY-N12534
-
-
-
- HY-N0211
-
-
-
- HY-B0715
-
|
BL-191; PTX; Oxpentifylline
|
Classification of Application Fields
Disease Research Fields
Cancer
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
-
- HY-N9228
-
-
-
- HY-N0155
-
-
-
- HY-N9174
-
|
|
Structural Classification
Flavonoids
Flavones
Source classification
Plants
Moraceae
Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat
|
Others
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
-
- HY-N2434
-
-
-
- HY-N0189
-
-
-
- HY-N12617
-
-
-
- HY-N10335
-
-
-
- HY-N7385
-
-
-
- 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-N11643
-
-
-
- HY-15128
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0715S
-
|
|
|
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
|
-
-
- HY-B0715S2
-
|
|
|
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
|
-
-
- HY-N0060BS
-
|
|
|
(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299[1].
|
-
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