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ChemicalBook--->CAS DataBase List--->1073485-20-7

1073485-20-7

1073485-20-7 Structure

1073485-20-7 Structure
IdentificationBack 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 PropertiesBack 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)
[color ]

White to off-white
Spectrum DetailBack Directory
[Spectrum Detail]

LDC000067(1073485-20-7)1HNMR
Hazard InformationBack 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]

TargetValue
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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