SML2179
LDC000067 hydrochloride
≥98% (HPLC)
别名:
3-((6-(2-Methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methanesulfonamide hydrochloride, 3-[[6-(2-Methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide, LDC067
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所有图片(1)
About This Item
经验公式（希尔记法）:
C18H18N4O3S · xHCl
CAS号:
分子量:
370.43 (free base basis)
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
价格与库存信息目前不能提供
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方案
≥98% (HPLC)
表单
powder
储存条件
protect from light
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear (warmed)
储存温度
−20°C
SMILES字符串
O=S(CC1=CC(NC2=NC=NC(C3=CC=CC=C3OC)=C2)=CC=C1)(N)=O
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
生化/生理作用
ATP-competitive, potent and selective cyclin-dependent kinase 9 (CDK9) inhibitor.
LDC000067 (LDC067) is an ATP-competitive, potent and selective cyclin-dependent kinase 9 (CDK9) inhibitor (IC50 = 44 nM/CDK9-CycT1 vs. 5.51 μM/CDK1-CycB1, 2.44 μM/CDK2-CycA, 9.24 μM/CDK4-CycD1, >10 μM/CDK6-CycD3 & CDK7-CycH-MAT1; Kd = 32.7 nM/CDK9-CycT1 vs. 1.01 μM/CDK2-CycA, 16.0 μM/CDK7-CycH-MAT1) with much reduced or little potency against a panel of 28 non-CDK kinases. LDC067 selectively inhibits cellular RNA polymerase II CTD Ser2 phosphorylation (by 40% in HeLa; 60-min, 10 μM LDC067), but not CDK9-independent pSer5 or pSer7, causing apoptosis induction (by 239% and 200% of untreated control in A549 and MCF7 cultures) as a result of blocking RNAPII-mediated mRNA synthesis.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
T K Albert et al.
British journal of pharmacology, 171(1), 55-68 (2013-10-10)
The cyclin-dependent kinase CDK9 is an important therapeutic target but currently available inhibitors exhibit low specificity and/or narrow therapeutic windows. Here we have used a new highly specific CDK9 inhibitor, LDC000067 to interrogate gene control mechanisms mediated by CDK9. The
Xinli Qu et al.
Kidney international, 88(6), 1323-1335 (2015-07-30)
Transforming growth factor-β1 (TGF-β1)/Smad signaling has a central role in the pathogenesis of renal fibrosis. Smad3 and Smad4 are pro-fibrotic, while Smad2 is anti-fibrotic. However, these Smads form heterogeneous complexes, the functions of which are poorly understood. Here we studied
Wanhua Xie et al.
Genome biology, 18(1), 32-32 (2017-02-18)
Monoubiquitination of H2B (H2Bub1) is a largely enigmatic histone modification that has been linked to transcriptional elongation. Because of this association, it has been commonly assumed that H2Bub1 is an exclusively positively acting histone modification and that increased H2Bub1 occupancy
Ke Ren et al.
PLoS pathogens, 12(10), e1005950-e1005950 (2016-10-21)
The human HSV-1 and -2 are common pathogens of human diseases. Both host and viral factors are involved in HSV lytic infection, although detailed mechanisms remain elusive. By screening a chemical library of epigenetic regulation, we identified bromodomain-containing protein 4
Nadine Löschmann et al.
Oncotarget, 7(36), 58051-58064 (2016-08-16)
The CDK inhibitor SNS-032 had previously exerted promising anti-neuroblastoma activity via CDK7 and 9 inhibition. ABCB1 expression was identified as major determinant of SNS-032 resistance. Here, we investigated the role of ABCB1 in acquired SNS-032 resistance. In contrast to ABCB1-expressing
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