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TGF-beta&Smad

LDN-212854 (1432597-26-6)

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

Not Intended for Therapeutic Use. For research use only.

CAS: 1432597-26-6 Category

LDN-212854 (1432597-26-6) Description:

LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. 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).[1]

Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair. LDN-212854 inhibits ALK2 (IC50 = 1.3 nM) in preference to other BMP type I receptors, ALK1 (IC50 = 2.4 nM) and ALK3 (IC50 = 85.8 nM) and with over 1,500-fold selectivity against the closely related activin and TGF-β type I receptors (i.e., ALK4 and ALK5).1 It has been shown to inhibit BMP6-induced osteogenic differentiation, which functions predominantly via ALK2, with an IC50 value of 10 nM.1 LDN-212854 also demonstrates off-target activity against RIPK2, ABL1, and PDGFRβ kinases with IC50 values less than 100 nM.1

LDN-212854 (1432597-26-6) Specifications:

Product Name LDN-212854
Synonyms LDN 212854; LDN 212854;BMP Inhibitor III
Chemical Name 5-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline
Purity >98%
CAS Number 1432597-26-6
Molecular Formula C25H22N6
Molecular Weight 406.493 g/mol
Monoisotopic Mass 406.191 g/mol
MDL number MFCD28099808
InChIKey BBDGBGOVJPEFBT-UHFFFAOYSA-N
InChi Code 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
SMILES C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=C6C=CC=NC6=CC=C5)N=C3
Form powder
Color white to beige
Solubility  Soluble in DMSO
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application BMP receptor inhibitor

 


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RIDADR NONH for all modes of transport

References:

1.Pharmacologic Strategies for Assaying BMP Signaling Function. Dinter T, Bocobo GA, Yu PB. Methods Mol Biol. 2019;1891:221-233. doi: 10.1007/978-1-4939-8904-1_16.

2.Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2. Williams E, Bullock AN. Bone. 2018 Apr;109:251-258. doi: 10.1016/j.bone.2017.09.004. Epub 2017 Sep 12. Review.

3.Strategic Targeting of Multiple BMP Receptors Prevents Trauma-Induced Heterotopic Ossification. Agarwal S, Loder SJ, Breuler C, Li J, Cholok D, Brownley C, Peterson J, Hsieh HH, Drake J, Ranganathan K, Niknafs YS, Xiao W, Li S, Kumar R, Tompkins R, Longaker MT, Davis TA, Yu PB, Mishina Y, Levi B. Mol Ther. 2017 Aug 2;25(8):1974-1987. doi: 10.1016/j.ymthe.2017.01.008. Epub 2017 Jul 15.

4.Metformin inhibits ALK1-mediated angiogenesis via activation of AMPK. Ying Y, Ueta T, Jiang S, Lin H, Wang Y, Vavvas D, Wen R, Chen YG, Luo Z. Oncotarget. 2017 May 16;8(20):32794-32806. doi: 10.18632/oncotarget.15825.

1 review for LDN-212854 (1432597-26-6)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The LDN-212854 (1432597-26-6) is high purity,also customer service is pretty nice !gotta try!!

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