YPN-005 | CDK7 inhibitor | Probechem Biochemicals

Chemical Structure : YPN-005

YPN-005 (YPN005)

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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Biological Activity

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.

Physicochemical Properties

M.Wt	488.610
Formula	C26H28N6O2S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S,E)-N-(3-cyano-5-(3-(1-((5-ethylthiazol-2-yl)amino)-1-oxopropan-2-yl)phenyl)pyridin-2-yl)-4-(dimethylamino)but-2-enamide

References

1. Yun Jung Choi, et al. Eur J Pharmacol. 2021 Sep 15;907:174298.

YPN-005 (YPN005)

Biological Activity

Physicochemical Properties

References

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