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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关于此项目
经验公式（希尔记法）:
C18H18N4O3S · xHCl
化学文摘社编号:
分子量:
370.43 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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)
SMILES string
O=S(CC1=CC(NC2=NC=NC(C3=CC=CC=C3OC)=C2)=CC=C1)(N)=O
InChI key
GGQCIOOSELPMBB-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
protect from light
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
−20°C
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
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
Mercedes Prudencio et al.
Human molecular genetics, 26(17), 3421-3431 (2017-06-24)
Significant transcriptome alterations are detected in the brain of patients with amyotrophic lateral sclerosis (ALS), including carriers of the C9orf72 repeat expansion and C9orf72-negative sporadic cases. Recently, the expression of repetitive element transcripts has been associated with toxicity and, while
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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