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SML2179

Sigma-Aldrich

LDC000067 hydrochloride

≥98% (HPLC)

Synonyme(s) :

3-((6-(2-Methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methanesulfonamide hydrochloride, 3-[[6-(2-Methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide, LDC067

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About This Item

Formule empirique (notation de Hill):
C18H18N4O3S · xHCl
Numéro CAS:
1073485-20-7
Poids moléculaire :
370.43 (free base basis)
Numéro MDL:
MFCD28137788
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

protect from light

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear (warmed)

Température de stockage

−20°C

Chaîne SMILES 

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)

Clé InChI

GGQCIOOSELPMBB-UHFFFAOYSA-N

Actions biochimiques/physiologiques

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Consulter la Bibliothèque de documents

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
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
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
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
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