LDC 000067

Discontinued Product

LDC 000067 (Cat. No. 6752) has been withdrawn from sale for commercial reasons.
Description: Potent and selective CDK9 inhibitor
Chemical Name: 3-[[6-(2-Methoxyphenyl)-4-pyrimidinyl]amino]benzenemethanesulfonamide
Purity: ≥98% (HPLC)

Biological Activity for LDC 000067

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.

Technical Data for LDC 000067

M. Wt 370.43
Formula C18H18N4O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1073485-20-7
PubChem ID 25104564
Smiles COC1=C(C2=NC=NC(NC3=CC(CS(N)(=O)=O)=CC=C3)=C2)C=CC=C1

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for LDC 000067

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

Albert et al (2014) Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br.J.Pharmacol. 171 55 PMID: 24102143

Gerlach et al (2018) The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML. Oncogene 37 2687 PMID: 29491412

Brägelmann et al (2017) Systematic kinase inhibitor profiling identifies CDK9 as a synthetic lethal target in NUT midline carcinoma. Cell Rep. 20 2833 PMID: 28930680

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987

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Keywords: LDC 000067, LDC 000067 supplier, LDC000067, LDC67, LDC067, potent, selective, CDK9, inhibitors, inhibits, Cyclin-dependent, Kinase, Transcriptional, CDKs, 6752, Tocris Bioscience

Citations for LDC 000067

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Currently there are no citations for LDC 000067.

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