A Cdk9 inhibitor
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LDC000067

Item No. 29419

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide
CAS Number
1073485-20-7
Synonyms
  • LDC067
Molecular Formula
C18H18N4O3S
Formula Weight
370.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 2 mg/ml
λmax
213, 265, 302 nm
SMILES
COC1=CC=CC=C1C2=NC=NC(NC3=CC(CS(N)(=O)=O)=CC=C3)=C2
InChi Code
InChI=1S/C18H18N4O3S/c1-25-17-8-3-2-7-15(17)16-10-18(21-12-20-16)22-14-6-4-5-13(9-14)11-26(19,23)24/h2-10,12H,11H2,1H3,(H2,19,23,24)(H,20,21,22)
InChi Key
GGQCIOOSELPMBB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $158

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    25 mg

    $349

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    Product Description

    LDC000067 is a cyclin-dependent kinase 9 (Cdk9) inhibitor (IC50 = 44 nM).1 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.2 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.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Albert, T.K., Rigault, C., Eickhoff, J., et al. Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br. J. Pharmacol. 171(1), 55-68 (2014).

    2. Xue, S., Zhu, L., Wang, C., et al. CDK9 attenuation exerts protective effects on catabolism and hypertrophy in chondrocytes and ameliorates osteoarthritis development. Biochem. Biophys. Res. Commun. 517(1), 132-139 (2019).

    3. Xue, S., Shao, Q., Zhu, L.-B., et al. LDC000067 suppresses RANKL-induced osteoclastogenesis in vitro and prevents LPS-induced osteolysis in vivo. Int. Immunopharmacol. 75:105826, (2019).