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| | LDC000067 Basic information |
| Product Name: | LDC000067 | | Synonyms: | LDC000067;LDC 067;LDC067;LDC-067;(3-(6-(2-Methoxyphenyl)pyrimidin-4-ylamino)phenyl)methanesulfonamide;3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide;LDC067;LDC 000067;LDC-000067;LDC 067;LDC-067;CS-1535 | | CAS: | 1073485-20-7 | | MF: | C18H18N4O3S | | MW: | 370.43 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 1073485-20-7.mol |  |
| | LDC000067 Chemical Properties |
| Boiling point | 604.1±65.0 °C(Predicted) | | density | 1.360±0.06 g/cm3(Predicted) | | storage temp. | under inert gas (nitrogen or Argon) at 2–8 °C | | solubility | insoluble in H2O; insoluble in EtOH; ≥18.52 mg/mL in DMSO | | form | Powder | | pka | 10.27±0.60(Predicted) |
| | LDC000067 Usage And Synthesis |
| 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 | Store 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. |
| | LDC000067 Preparation Products And Raw materials |
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