2. Cell Cycle/DNA Damage
  3. CDK
  4. THZ531

THZ531 

Cat. No.: HY-103618 Purity: 99.57%
COA Handling Instructions

THZ531 est un inhibiteur sélectif et covalent des CDK12 et CDK13 avec des IC50 de 158 nM et 69 nM , respectivement.

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

For research use only. We do not sell to patients.

THZ531 Chemical Structure

THZ531 Chemical Structure

CAS No. : 1702809-17-3

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1 mg USD 80 In-stock
5 mg USD 140 In-stock
10 mg USD 190 In-stock
25 mg USD 420 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

THZ531 Related Antibodies

Top Publications Citing Use of Products

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively[1].

IC50 & Target[1]

CDK12

158 nM (IC50)

CDK13

69 nM (IC50)

CDK7

8.5 μM (IC50)

CDK9

10.5 μM (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

THZ531 Related Antibodies
Molecular Weight

558.07

Appearance

Solid

Formula

C30H32ClN7O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (447.97 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.43 mg/mL (2.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.43 mg/mL (2.56 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.43 mg/mL (2.56 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.86%

COA (245 KB) HNMR (229 KB) LCMS (410 KB)

Handling Instructions (2659 KB)
References
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
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THZ531 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

THZ5311702809-17-3THZ 531THZ-531CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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