LDC067 MedChemExpress (MCE)

Product Name	LDC000067
Synonyms	LDC067 LDC 067 LDC-067 CS-1535 LDC000067 LDC-000067 LDC 000067 Synonyms LDC067 LDC 067 LDC-067 CS-1535 LDC000067 LDC-000067 LDC 000067 (3-(6-(2-Methoxyphenyl)pyrimidin-4-ylamino)phenyl)methanesulfonamide 3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide
CAS	1073485-20-7
EINECS
Chemical Formula	C18H18N4O3S
Molecular Weight	370.43
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	LDC000067 LDC000067 MedChemExpress (MCE) HY-15878 1073485-20-7 LDC067 98.09% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions LDC000067 LDC000067 MedChemExpress (MCE) HY-15878 1073485-20-7 LDC067 98.09% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro. The selectivity of LDC000067 for CDK9 over other CDKs exceeds that of the known inhibitors flavopiridol and DRB. LDC000067 displayed 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7. LDC000067 inhibits in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrates a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis[1]. The fluorescence resonance energy transfer (FRET)-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the Km values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are then recorded[1]. CDK9- Cyclin T1 44 nM (IC50) cdk2-cyclin A 2441 nM (IC50) cdk1-cyclin B1 5513 nM (IC50) cdk4-cyclin D1 9242 nM (IC50) GSK3A 1460 nM (IC50) HGK/MAP4K4 820 nM (IC50) ABL2/ARG 3640 nM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Albert TK, et al. Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br J Pharmacol. 2014 Jan 171(1):55-68. [Content Brief]
Last Update	2025-04-01 14:45:47

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