BiochemProbe — Life Science Research Reagents

THZ531 free base · Synonyms: THZ-531 · THZ 531

THZ531 is a selective and covalent inhibitor of both CDK12.

For research use only. Not for human or veterinary use.

Target CDK
Research area Cancer
Purity >98% Stock Inquire

THZ531 structure

CAS No.: 1702809-17-3

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
50 mg USD 425.00 BP-02326-50mg In stock Get quote
100 mg USD 650.00 BP-02326-100mg In stock Get quote
250 mg USD 850.00 BP-02326-250mg In stock Get quote
500 mg USD 1,150.00 BP-02326-500mg In stock Get quote
1 g USD 1,650.00 BP-02326-1g In stock Get quote
5 g Inquire BP-02326-5g In stock Inquire

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Description

THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.

Biological activity

In Vitro The results from Kinase assays demonstrate that THZ531 potently inhibits CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively; whereas inhibition of CDK7 and CDK9 is more than 50-fold weaker with IC50s of 8.5 and 10.5 μM, respectively. THZ531 treatment leads to a dramatic and irreversible decrease in Jurkat cell proliferation with an IC50 of 50 nM. FACS cell cycle analysis following treatment with escalating doses of THZ531 displays a dose and time-dependent increase in the number of cells exhibiting sub-G1 content. At 50 nM THZ531, no increase in the percentage of apoptotic cells is observed over DMSO control for the time course of the experiment. Higher doses of THZ531 leads to pronounced Annexin V signal with 30 to 40% annexin V-positively stained cells by 72 hrs. A dramatic reduction in elongating Pol II following THZ531 treatment is also observed

Identifiers

SMILES
CN(C)C\C=C\C(=O)NC1=CC=C(C=C1)C(=O)N1CCC[C@H](C1)NC1=NC(C2=CNC3=C2C=CC=C3)=C(Cl)C=N1
InChIKey
RUBYHLPRZRMTJO-MOVYNIQHSA-N

Specifications

MW (average)
558.0740
Formula
C30H32ClN7O2
CAS No.
1702809-17-3
Physical state
Other
Color
White to light yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Zhang T, et al. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nat Chem Biol. 2016 Oct;12(10):876-84.

Same target

Search CDK

Same research area

Search Cancer