| Identification | Back Directory | [Name]
LDC000067 | [CAS]
1073485-20-7 | [Synonyms]
LDC067
LDC-067
LDC 067
CS-1535
LDC000067
LDC000067(LDC-067)
LDC000067 USP/EP/BP
LDC067;LDC 000067;LDC-000067;LDC 067;LDC-067
(3-(6-(2-Methoxyphenyl)pyrimidin-4-ylamino)phenyl)methanesulfonamide
3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide
Benzenemethanesulfonamide, 3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]- | [Molecular Formula]
C18H18N4O3S | [MDL Number]
MFCD28137788 | [MOL File]
1073485-20-7.mol | [Molecular Weight]
370.43 |
| Chemical Properties | Back Directory | [Boiling point ]
604.1±65.0 °C(Predicted) | [density ]
1.360±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥18.52 mg/mL in DMSO | [form ]
Powder | [pka]
10.27±0.60(Predicted) |
| Hazard Information | Back Directory | [Biological Activity]
ldc000067 (ldc067) is a novel specific inhibitor of cdk9 with ic50 value of 44 ± 10 nm [1].cyclin-dependent kinase 9 (cdk9) is a cyclin-dependent kinase. cdk9 and cyclin t form the positive transcription elongation factor b (p-tefb) complex for rna polymerase ii and functions by phosphorylating the c-terminal domain of the largest subunit of rna polymerase ii [1].ldc000067 (ldc067) is a novel and highly specific cdk9 inhibitor. ldc000067 exhibited selectivity for cdk9 over other cdks in the range of 55-fold (vs. cdk2) to over 230-fold (vs. cdk6 and cdk7). ldc067 also inhibited transcription in a dose-dependent and atp-competitive manner. in whole cells, ldc000067 induced the tumor suppressor protein p53 activation and apoptosis. ldc000067 also selectively reduced short-lived mrnas, including those that encode regulators of apoptosis and proliferation such as myc and mcl1 [1]. | [in vitro]
LDC000067 reduces Ser2-P in mESCs, induces p53 activation, and leads to apoptosis. In addition, LDC067 also dose-dependently inhibited the de novo RNA synthesis of P-TEFb-dependent cellular genes. | [target]
| Target | Value | CDK9
(Cell-free assay) | 44 nM | CDK2
(Cell-free assay) | 2.441 μM |
| [storage]
Desiccate at -20°C | [References]
[1]. albert tk, 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, 2014, 171(1): 55-68. |
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