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SML0965

Sigma-Aldrich

LDN-212854

≥98% (HPLC)

Sinónimos:

5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline

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About This Item

Fórmula empírica (notación de Hill):
C25H22N6
Número de CAS:
1432597-26-6
Peso molecular:
406.48
UNSPSC Code:
51111800
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 1 mg/mL, clear (warmed)

storage temp.

2-8°C

InChI

1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2

InChI key

BBDGBGOVJPEFBT-UHFFFAOYSA-N

Biochem/physiol Actions

LDN-212854 is a selective and potent inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with over 5,000-fold selectivity for BMP versus the closely related TGF-β and activin type I receptors. LDN-212854 has some selectivity for ALK2 with an IC50 of 1.3 nM in preference to other BMP type I receptors, ALK1 (IC50=2.4 nM) and ALK3 (IC50=85.8 nM). LDN-212854 shows better selectivity than LDN193189 in cell-based assays of BMP signaling. LDN-212854 inhibited BMP6-induced osteogenic differentiation, which functions primarily via ALK2, more potently than BMP4, which functions primarily with ALK3 (IC50s of 10 nM versus 40.5 nM), whereas LDN-193189 inhibited both equally. The only off target effects found against a panel of 198 kinases were for RIPK2, ABL1, and PDGFR-β with IC50 values < 100 nM.
LDN-212854 is also known as 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. LDN-212854 prevents heterotopic ossification in an inducible mutant ALK2 (activin receptor-like kinase 2).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

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The intracellular signaling mechanisms through which TGF-β regulates pulmonary development are incompletely understood. Canonical TGF-β signaling involves Smad2/3 phosphorylation, Smad2/3·Smad4 complex formation and nuclear localization, and gene regulation. Here, we show that physiologically relevant TGF-β1 levels also stimulate Smad1/5 phosphorylation
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Recent findings have shown that inhibitors targeting bromodomain and extraterminal domain (BET) proteins, such as the small molecule JQ1, are potent growth inhibitors of many cancers and hold promise for cancer therapy. However, some reports have also revealed that JQ1

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