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Merck
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SML2179

Sigma-Aldrich

LDC000067 hydrochloride

≥98% (HPLC)

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C18H18N4O3S · xHCl
Numero CAS:
1073485-20-7
Peso molecolare:
370.43 (free base basis)
Numero MDL:
MFCD28137788
Codice UNSPSC:
12352200
NACRES:
NA.77

Saggio

≥98% (HPLC)

Forma fisica

powder

Condizioni di stoccaggio

protect from light

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear (warmed)

Temperatura di conservazione

−20°C

Stringa SMILE

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)
GGQCIOOSELPMBB-UHFFFAOYSA-N

Azioni biochim/fisiol

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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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
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
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