868066-26-6
Chemical Structure
SNX631
- CAS No.: 868066-26-6
- Formula:C22H26N6O2S
- Molecular Weight:438.55
IUPAC Name: 3-amino-4-(4-(4-(dimethylcarbamoyl)phenyl)-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2-carboxamide
InChIKey: CYLDJPVEBVIXNB-UHFFFAOYSA-N
SMILES: O=C(N)C=1SC2=NC=CC(=C2C1N)N3CCN(C4=CC=C(C=C4)C(=O)N(C)C)CCC3
Biological Activity: SNX631 is an orally active and selective CDK8/CDK19 inhibitor. SNX631 reduces the phosphorylation of STAT1/STAT3 S727, and upregulates miR-21-5p, miR-21-3p and miR-221 in cancer cells. SNX631 transcription-independently inhibits meiotic resumption in mouse oocytes, blocks nuclear envelope breakdown, first polar body extrusion and mitochondrial expansion and aggregation, with no cytotoxicity. SNX631, in combination with Lapatinib (HY-50898) or Trastuzumab (HY-P9907), synergistically inhibits cancer cell growth, upregulates the tumor suppressor BTG2, prevents Lapatinib-induced upregulation of oncogenic miRNAs, overcomes drug resistance, reduces the infiltration of αSMA+ stromal fibroblasts and ARG1+ M2 macrophages, and exhibits favorable biosafety. SNX631 can be used in studies related to HER2-positive breast cancer and cancer[1][2][3].
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SNX631 | SNX631 is an orally active and selective CDK8/CDK19 inhibitor. SNX631 reduces the phosphorylation of STAT1/STAT3 S727, and upregulates miR-21-5p, miR-21-3p and miR-221 in cancer cells. SNX631 transcription-independently inhibits meiotic resumption in mouse oocytes, blocks nuclear envelope breakdown, first polar body extrusion and mitochondrial expansion and aggregation, with no cytotoxicity. SNX631, in combination with Lapatinib (HY-50898) or Trastuzumab (HY-P9907), synergistically inhibits cancer cell growth, upregulates the tumor suppressor BTG2, prevents Lapatinib-induced upregulation of oncogenic miRNAs, overcomes drug resistance, reduces the infiltration of αSMA+ stromal fibroblasts and ARG1+ M2 macrophages, and exhibits favorable biosafety. SNX631 can be used in studies related to HER2-positive breast cancer and cancer. | |||||||||||||||||||||
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References
- [1]. Ding X, et al. Inhibition of CDK8/19 Mediator kinase potentiates HER2-targeting drugs and bypasses resistance to these agents in vitro and in vivo. Proceedings of the National Academy of Sciences of the United States of America. 2022 Aug 09;119(32):e2201073119. [Content Brief]
- [2]. Okulova Y, et al. Cyclin dependent kinases CDK8/19 are required for PKA inactivation during meiosis resumption. Biochimica et biophysica acta. Molecular cell research. 2026 Mar;1873(3):120114.
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[3]. Bi F, et al. CDK inhibitor. International Patent Application No. WO 2024/193640 A1. Published September 26, 2024.
