An inhibitor of Cdk12 and Cdk13
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THZ531

Item No. 26386

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-[4-[[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-1-piperidinyl]carbonyl]phenyl]-4-(dimethylamino)-2-butenamide
CAS Number
1702809-17-3
Molecular Formula
C30H32ClN7O2
Formula Weight
558.1
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 25 mg/ml
λmax
214, 251, 352 nm
SMILES
ClC1=CN=C(N[C@@H]2CCCN(C(C3=CC=C(NC(/C=C/CN(C)C)=O)C=C3)=O)C2)N=C1C4=CNC5=C4C=CC=C5
InChi Code
InChI=1S/C30H32ClN7O2/c1-37(2)15-6-10-27(39)34-21-13-11-20(12-14-21)29(40)38-16-5-7-22(19-38)35-30-33-18-25(31)28(36-30)24-17-32-26-9-4-3-8-23(24)26/h3-4,6,8-14,17-18,22,32H,5,7,15-16,19H2,1-2H3,(H,34,39)(H,33,35,36)/b10-6+/t22-/m1/s1
InChi Key
RUBYHLPRZRMTJO-MOVYNIQHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

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    10 mg

    $525

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    25 mg

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    Product Description

    THZ531 is an inhibitor of cyclin-dependent kinase 12 (Cdk12) and Cdk13 (IC50s = 158 and 69 nM for Cdk12/cyclin K and Cdk13/cyclin K, respectively).1 It is selective for Cdk12/cyclin K and Cdk13/cyclin K over Cdk9/cyclin T1 and Cdk7/cyclin H/MAT1 (IC50s = 10.5 and 8.5 μM, respectively). THZ531 inhibits proliferation of Jurkat cells with an IC50 value of 50 nM and induces apoptosis in a concentration-dependent manner. It also reduces expression of genes associated with the DNA damage response, including BRCA1, FANCF, and ERCC4, in Jurkat cells when used at a concentration of 50 nM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, T., Kwiatkowski, N., Olson, C.M., et al. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nat. Chem. Biol. 12(10), 876-884 (2016).