SML2179
LDC000067 hydrochloride
≥98% (HPLC)
동의어(들):
3-((6-(2-Methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methanesulfonamide hydrochloride, 3-[[6-(2-Methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide, LDC067
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C18H18N4O3S · xHCl
CAS Number:
Molecular Weight:
370.43 (free base basis)
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77
추천 제품
분석
≥98% (HPLC)
양식
powder
저장 조건
protect from light
색상
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
저장 온도
−20°C
SMILES string
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
생화학적/생리학적 작용
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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