CDK Inhibitor
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IRAK4-IN-35
0 ImagesCat. No.: HY-187692CAS No.: 3112339-39-3IRAK4-IN-35 is an orally active IRAK4 inhibitor with an IRAK4 IC50 of 9.88 nM. IRAK4-IN-35 also inhibits JAK3, EGFR, CDK2 with IC50 values of 6.72 nM, 32.35 nM, and 39.08 nM, respectively. IRAK4-IN-35 inhibits the production of proinflammatory cytokines, blocks inflammatory signaling pathways, and reduces serum TNF-α levels and spleen index in mouse models of acute inflammation. IRAK4-IN-35 decreases the disease activity index, paw swelling degree, and spleen index in a collagen-induced arthritis mouse model. IRAK4-IN-35 can be used for the research of rheumatoid arthritis.
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CDK8-IN-19
0 ImagesCat. No.: HY-176282CDK8-IN-19 (Compound 3d) is a CDK8 inhibitor with an IC50 of 25.08 nM. CDK8-IN-19 has a broad-spectrum anticancer activity, such as leukemia, melanoma and breast cancer, without significant cytotoxic effect on the normal Vero cells (mean IC50s of 2.87, 3.65, 3.79 and 45.48 μM, respectively).
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Autophagy agonist-1
0 ImagesCat. No.: HY-170992Autophagy agonist-1 (compound 22) is an Autophagy agonist. Autophagy agonist-1 exhibits significant anticancer activity against HepG2 cells and normal cells with IC50s of 8.8 μM and > 50 μM. Autophagy agonist-1 induces G1/S phase cell cycle arrest and inhibits CDK4 and CyclinD1 expression while upregulating P21. Autophagy agonist-1 promotes the accumulation of autophagosomes and the proteins LC3 and PINK1, enhancing autophagy and mitophagy in HepG2 cells.
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3-Methylthienyl-carbonyl-JNJ-7706621
0 ImagesCat. No.: HY-141685CAS No.: 443798-09-23-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.
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EGFR/HER2/CDK9-IN-3
0 ImagesCat. No.: HY-147798CAS No.: 422276-47-9
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CDK7-IN-8
0 ImagesCat. No.: HY-143586CAS No.: 2654003-64-0
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CDK11-IN-1
0 ImagesCat. No.: HY-182764CDK11-IN-1 is an orally active cyclin-dependent kinase 11 (CDK11) inhibitor with an IC50 of 4 nM, and it exhibits high selectivity against other kinases including CDK7 and CDK9. CDK11-IN-1 inhibits tumor growth in lung cancer xenograft models. CDK11-IN-1 can be used for lung cancer research.
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EGFR/HER2/CDK9-IN-1
0 ImagesCat. No.: HY-147796CAS No.: 879730-44-6
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SC-60
0 ImagesCat. No.: HY-W717425CAS No.: 1421677-31-7SC-60 is a derivative of Sorafenib (HY-10201). SC-60 exerts its anti-tumor effect by activating the phosphatase activity of SHP-1, thereby inhibiting the STAT3 signaling pathway. SC-60 exhibits strong proliferation inhibitory activity in various hepatocellular carcinoma (HCC) cell lines. SC-60 downregulates the expression of downstream anti-apoptotic proteins (such as Bcl-2, Cyclin D1, Survivin), ultimately inducing caspase-dependent apoptosis. SC-60 significantly inhibits tumor growth in xenograft tumor models. SC-60 can be used for the study of HCC.
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CDK4-IN-6
0 ImagesCat. No.: HY-184418CAS No.: 3120500-44-6
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STAT3-IN-32
0 ImagesCat. No.: HY-164445CAS No.: 2591440-71-8STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a Kd of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer.
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MFDCH016
0 ImagesCat. No.: HY-178350MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer.
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Cdc7-IN-19
0 ImagesCat. No.: HY-143433CAS No.: 2606780-39-4Cdc7-IN-19 (compound 1-1) is a potent CDC7 inhibitor with an IC50 of 1.49 nM.
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SY-5102
0 ImagesCat. No.: HY-180355CAS No.: 2365230-48-2SY-5102 is a potent, selective, and orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd value of 0.03 nM. SY-5102 occupies the ATP-binding pocket of CDK7 via non-covalent binding to inhibit CDK7 activity, and downregulates its phosphorylation of cyclin CDK and RNA polymerase II. SY-5102 inhibits cancer cell proliferation, and induces tumor growth inhibition and regression. SY-5102 can be used in research related to triple-negative breast cancer.
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SB-1295
0 ImagesCat. No.: HY-155065SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrial membrane potential and inducing apoptosis. SB-1295 has the potential to study cancer.
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EGFR-IN-182
0 ImagesCat. No.: HY-178955EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer.
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CDK9-IN-31 dimaleate
0 ImagesCat. No.: HY-160171ACDK9-IN-31 dimaleate (Compound Z1) is a CDK9 inhibitor that inhibits cancer cell growth. CDK9-IN-31 dimaleate has the potential to be developed as an anticancer agent.
