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Chemical Structure : YPN-005
Catalog No.: PC-47100Not For Human Use, Lab Use Only.
YPN-005 (YPN005) is a highly potent, selective inhibitor of cyclin-dependent kinase 7 (CDK7) with IC50 of 31 nM, with low inhibition for CDK2 and CDK5.
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YPN-005 (YPN005) is a highly potent, selective inhibitor of cyclin-dependent kinase 7 (CDK7) with IC50 of 31 nM, with low inhibition for CDK2 and CDK5.
YPN005 inhibits 7 kinases among 468, with over 90% at 1 uM, including CDK13, CDK19, CSNK1A1, CSNK1D, CSNK1E, MAPK15, and MAPK10.
YPN-005 treatment inhibits the phosphorylation of the CDK7 substrate RNAPII CTD at Ser-2, Ser-5, and Ser-7, completely inhibits the activity of RNAPII CTD in SCLC cells.
YPN-005 is more effective than THZ1.
YPN-005 shows antiproliferative effects in SCLC and cells with acquired resistance to conventional anticancer drugs.
YPN-005 shows a significant inhibition of tumor growth through the suppression of RNA polymerase II phosphorylation in NOD-SCID mice bearing H209, H209/CisR, or H209/EtoR cells.
| M.Wt | 488.610 | |
| Formula | C26H28N6O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yun Jung Choi, et al. Eur J Pharmacol. 2021 Sep 15;907:174298.
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