LDC 000067

Key Product Details

Product Description

LDC 000067 is a potent and selective CDK9 inhibitor (IC₅₀ = 44 nM at CDK9-cyclin T1). Inhibits other CDKs in the micromolar range (IC₅₀ values are 2.4, 5.5, 9.2, >10 and >10 μM for CDK2-cyclin A, CDK1-cyclin B1, CDK4-cyclin D1, CDK6-cyclin D3 and CDK7-cyclin H-MAT1, respectively). Inhibits P-TEFb-dependent in vitro transcription. Induces apoptosis in vitro and in vivo in combination with BI 894999.

Product Specifications for LDC 000067

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for LDC 000067

The following data is based on the product molecular weight 370.43.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.70 mL	13.50 mL	27.00 mL
5 mM	0.54 mL	2.70 mL	5.40 mL
10 mM	0.27 mL	1.35 mL	2.70 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Jorda How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 2018 PMID: 30234987
• Gerlach The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML. Oncogene 2018 PMID: 29491412
• Brägelmann Systematic kinase inhibitor profiling identifies CDK9 as a synthetic lethal target in NUT midline carcinoma. Cell Rep. 2017 PMID: 28930680
• Albert Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br.J.Pharmacol. 2014 PMID: 24102143

Product Documents for LDC 000067