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说明： Potent and selective CDK9 inhibitor
化学名： 3-[[6-(2-Methoxyphenyl)-4-pyrimidinyl]amino]benzenemethanesulfonamide
纯度： ≥98% (HPLC)
生物活性 for LDC 000067
LDC 000067 is a potent and selective CDK9 inhibitor (IC50 = 44 nM at CDK9-cyclin T1). Inhibits other CDKs in the micromolar range (IC50 values are 2.4, 5.5, 9.2, >10 and >10 μM for CDK2-cyclin A, CDK1-cyclin B1, CDK4-cyclin D1, CDK6-cyclin D3 and CDK7-cyclin H-MAT1, respectively). Inhibits P-TEFb-dependent in vitro transcription. Induces apoptosis in vitro and in vivo in combination with BI 894999.
技术数据 for LDC 000067
| 分子量 | 370.43 |
| 公式 | C18H18N4O3S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1073485-20-7 |
| PubChem ID | 25104564 |
| InChI Key | GGQCIOOSELPMBB-UHFFFAOYSA-N |
| Smiles | COC1=C(C2=NC=NC(NC3=CC(CS(N)(=O)=O)=CC=C3)=C2)C=CC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for LDC 000067
参考文献 for LDC 000067
参考文献是支持产品生物活性的出版物。
Albert et al (2014) Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br.J.Pharmacol. 171 55 PMID: 24102143
Gerlach et al (2018) The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML. Oncogene 37 2687 PMID: 29491412
Brägelmann et al (2017) Systematic kinase inhibitor profiling identifies CDK9 as a synthetic lethal target in NUT midline carcinoma. Cell Rep. 20 2833 PMID: 28930680
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
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关键词: LDC 000067, LDC 000067 supplier, LDC000067, LDC67, LDC067, potent, selective, CDK9, inhibitors, inhibits, Cyclin-dependent, Kinase, Transcriptional, CDKs, 6752, Tocris Bioscience
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