YKL-5-124,CAS:1957203-01-8|CDK7 inhibitor

Cas No.:	1957203-01-8
Chemical Name:	(S)-3-(4-acrylamidobenzamido)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide
SMILES:	CC1(C)N(C(N[C@@H](C2=CC=CC=C2)CN(C)C)=O)CC3=C1NN=C3NC(C4=CC=C(NC(C=C)=O)C=C4)=O
Formula:	C₂₈H₃₃N₇O₃
M.Wt:	515.61
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM; displays biochemical and cellular selectivity for CDK7 over structurally related kinases CDK12/13, and no significant activity against CDK2 and CDK9 (IC50>1 uM); targets and forms a covalent bond with CDK7- cysteine 312 (C312); inhibition of CDK7 by YKL-5-124 elicits a transcriptional signature distinct from that of THZ1, shows no discernible effect on RNA Pol II CTD phosphorylation; recapitulate THZ1-mediated effects on gene expression and CTD phosphorylation when combined with CDK12/13 inhibitor THZ531.

References:

References 1. Olson CM, et al. Cell Chem Biol. 2019 Mar 6. pii: S2451-9456(19)30067-4. View Related Products by Target Cyclin-dependent Kinase (CDK)

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.
DC75816	Nisoxetine	Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.
DC75641	GENZ-644282 TFA salt	Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.
DC75325	PSMA-617 TFA	PSMA-617, also know as vipivotide tetraxetan, is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC.
DC75202	Fosaprepitant free acid	Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4
DC74748	O4I4	O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability.
DC74684	ZH8667	ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.
DC74646	EB-PSMA-617	EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.