[CAS NO. 1702809-17-3] THZ531

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PRODUCTS SPECIFICATIONS [1702809-17-3]

Catalog

SLK-S6595

Brand

Selleck

CAS

1702809-17-3

DESCRIPTION [1702809-17-3]

Overview

MDL	MFCD31563595
Molecular Weight	558.07
Molecular Formula	C30H32ClN7O2
SMILES	O=C(NC1=CC=C(C(N2C[C@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)CCC2)=O)C=C1)/C=C/CN(C)C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.7919 mL	8.9594 mL	17.9189 mL
5 mM	0.3584 mL	1.7919 mL	3.5838 mL
10 mM	0.1792 mL	0.8959 mL	1.7919 mL
50 mM	0.0358 mL	0.1792 mL	0.3584 mL

Description

THZ531 is a selective covalent inhibitor of and with IC50 values of 158 and 69 nM, respectively.

Targets

CDK13 ^[1]	CDK12 ^[1]
69 nM	158 nM

In vitro

THZ531 treatment leads to a dramatic and irreversible decrease in Jurkat cell proliferation with an IC50 of 50 nM. THZ531 induces apoptosis in a dose- and time-dependent manner with low doses (<350 nM) leading to slow onset of apoptosis over several cell doublings, while doses exceeding 350 nM induce rapid apoptosis which may result from a combination of on- and off- target effects. THZ531 reduces Pol II CTD Ser2 phosphorylation (pSer2) in a concentration-dependent manner.

References

[1] Zhang T, et al. Nat Chem Biol. 2016, 12(10):876-84.