1. Cell Cycle/DNA Damage
  2. CDK

THZ531 

目录号: HY-103618 纯度: 99.86%
产品使用指南

THZ531 是 CDK12CDK13 的共价抑制剂,其 IC50 值分别为 158 nM 和 69 nM。

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THZ531 Chemical Structure

THZ531 Chemical Structure

CAS No. : 1702809-17-3

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥2947 In-stock
5 mg ¥2400 In-stock
10 mg ¥3800 In-stock
25 mg ¥7800 In-stock
50 mg ¥12500 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Description

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

IC50 & Target

CDK12

158 nM (IC50)

CDK13

69 nM (IC50)

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[1].

References
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
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

Cells are treated with THZ531 or DMSO for 6 hrs. Following treatment cells are washed 2-fold with cold PBS and then lysed in the following lysis buffer: 50 mM Hepes pH 7.4, 150 mM NaCl, 1% Nonidet P40 substitute, 5 mM EDTA, 1 mM DTT, and protease/phosphatase cocktails. Following clearance, lysates are treated with bio-THZ1 or bio-TH531 for pulldown overnight at 4°C. Lysates are further incubated at room temperature for 3 hrs to increase the efficiency of covalent bond formation. Lysates are then incubated with streptavidin agarose for pulldown for an additional 2 to 3 hrs at 4°C[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Jurkat cells are plated in 96-well plates at 20,000 cells/well in fresh media and treated with THZ531 or DMSO at the indicated concentrations for 72 hours. HAP1 cells are seeded in 96-well plates at 12,000 cells/well in fresh media and 24 hours later are treated with THZ531 at the indicated concentrations for 72 hours. Anti-proliferative effect of THZ531 is assessed. To assess the effect of inhibitor washout on anti-proliferation of Jurkat cells, cells are treated with THZ531 or DMSO for 6 hrs. Inhibitor-containing medium is then removed and incubated with or without THZ531 for 66 hrs. Anti-proliferative effect of THZ531 is assessed. All proliferation assays are performed in biological triplicate. IC50s are determined using non-linear regression curve fit[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

558.07

Formula

C₃₀H₃₂ClN₇O₂

CAS No.

1702809-17-3

SMILES

ClC(C(C1=CNC2=CC=CC=C12)=N3)=CN=C3N[C@@H]4CCCN(C(C5=CC=C(NC(/C=C/CN(C)C)=O)C=C5)=O)C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO:16mg/mL(Need ultrasonic and warming)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.86%

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产品名称:
THZ531
目录号:
HY-103618
需求量: