A Cdk9 inhibitor (IC50 = 44 nM); selective for Cdk9 over Cdk1

LDC000067 – 5 mg

Brand:
Cayman
CAS:
1073485-20-7
Storage:
-20
UN-No:
Non-Hazardous - /

LDC000067 is a cyclin-dependent kinase 9 (Cdk9) inhibitor (IC50 = 44 nM).{46601} It is selective for Cdk9 over Cdk1, -2, -4, -6, and -7 (IC50s = 5.5, 2.44, 9.24, >10, and >10 μM, respectively), as well as a panel of 28 additional kinases at 10 μM. LDC000067 (10 μM) inhibits transcription dependent on the Cdk9-cyclin T complex positive transcription elongation factor b (P-TEFb) in vitro and de novo RNA synthesis in A549 cells. It induces apoptosis in A549 and MCF-7 cancer cells. LDC000067 prevents IL-1β-induced production of matrix metalloproteinase-3 (MMP-3), MMP-9, MMP-13, IL-6, IL-8, and TNF-α and NF-κB activation in SW 1353 chondrocytes.{46602} In vivo, LDC000067 (7.5 mg/kg) delays cartilage degeneration in a mouse model of anterior cruciate ligament transection (ACLT). It also prevents bone resorption in mouse models of ACLT- or LPS-induced osteoarthritis.{46603}  

 

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Description

A Cdk9 inhibitor (IC50 = 44 nM); selective for Cdk9 over Cdk1, -2, -4, -6, and -7 (IC50s = 5.5, 2.44, 9.24, >10, and >10 μM, respectively) and a panel of 28 additional kinases at 10 μM; inhibits P-TEFb-dependent transcription in vitro and de novo RNA synthesis in A549 cells at 10 μM; induces apoptosis in A549 and MCF-7 cancer cells; prevents IL-1β-induced production of MMP-3, MMP-9, MMP-13, IL-6, IL-8, and TNF-α and NF-κB activation in SW 1353 chondrocytes; delays cartilage degeneration in a mouse model of ACLT at 7.5 mg/kg; prevents bone resorption in mouse models of ACLT- or LPS-induced osteoarthritis

Formal name: 3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide

Synonyms:  LDC067

Molecular weight: 370.4

CAS: 1073485-20-7

Purity: ≥98%

Formulation: A crystalline solid

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