MK-4827 hydrochloride

• CAT Number: I000231
• CAS Number: 1038915-64-8
• Molecular Formula: C19H21ClN4O
• Molecular Weight: 356.85
• Purity: ≥95%
• Synonyms: 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;hydrochloride
• Target: PARP
• Solubility: 10 mM in DMSO
• Storage: Store at -20℃
• IC50: 3.8 nM/2.1 nM( PARP1/2) [1]
• InChI: InChI=1S/C19H20N4O.ClH/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14;/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);1H/t14-;/m1./s1
• InChIKey: YXYDNYFWAFBCAN-PFEQFJNWSA-N
• SMILES: C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N.Cl

MK 386 (Cat.No:I000231) is a potent and selective non-steroidal antagonist of the progesterone receptor. It acts by inhibiting the binding of progesterone to its receptor, thereby interfering with progesterone-mediated signaling pathways. MK 386 has been investigated for its potential therapeutic applications in hormone-related conditions such as breast cancer and endometriosis.

Reference

[1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.
[2]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.