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TGF-beta&Smad

LDN193189 (1062368-24-4)

LDN193189 is a highly potent small molecule BMP inhibitor with IC50 of 5 and 30 nM for ALK2 and ALK3, respectively. LDN193189 also inhibits BMP type I receptors ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation…

Not Intended for Therapeutic Use. For research use only.

CAS: 1062368-24-4 Category

LDN193189 (1062368-24-4) Description:

LDN193189 is a small molecule inhibitor of BMP type I receptors ALK2 and ALK3 (IC50 = 5 nM and 30 nM respectively).It only weakly inhibits ALK4, ALK5, and ALK7. LDN193189 functions primarily through prevention of Smad1, Smad5, and Smad8 phosphorylation. BMP signaling coordinates developmental patterning and has essential physiological roles in mature organisms. LDN-193189 has been used to reduce ectopic ossification in a mouse model. The role of BMP2 signals in the growth and angiogenesis of non-small-cell lung carcinoma (NSCLC) also suggest LDN-193189 may be a potent inhibitor of lung tumors.

Normal development and tissue repair are controlled in part by SMADs, a family of intracellular proteins that are activated by signaling via serine/threonine kinase receptors of the TGF-β superfamily.1 LDN-193189 inhibits SMAD1/5/8 phosphorylation by the bone morphogenetic protein (BMP) type I receptors, which are known as activin receptor-like kinases (ALKs), with an IC50 value of 4.9 nM.2 In in vitro kinase assays, it shows specificity for ALK1, 2, 3, and 6 (IC50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC50s = 101 and 350 nM, respectively).3 LDN-193189 has been used to inhibit BMP type I receptor activity to study the pathogenesis of fibrodysplasia ossificans progressive, a congenital hyperossification disorder, and to examine the role of osteogenesis in prostate tumor metastases in bone.

LDN193189 (1062368-24-4) Specifications:

Product Name LDN193189
Synonyms LDN 193189; LDN-193189
Chemical Name 4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline
Purity >98%
CAS Number 1062368-24-4
Molecular Formula C25H22N6
Molecular Weight 406.493 g/mol
Monoisotopic Mass 406.191 g/mol
MDL number MFCD17169988
InChIKey CDOVNWNANFFLFJ-UHFFFAOYSA-N
InChi Code InChI=1S/C25H22N6/c1-2-4-24-22(3-1)21(9-10-27-24)23-16-29-31-17-19(15-28-25(23)31)18-5-7-20(8-6-18)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=CC=NC6=CC=CC=C56)N=C3
Form powder
Color yellow to orange
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 ALK inhibitor

 


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RIDADR NONH for all modes of transport

References:

  • Evaluation of multikinase inhibitor LDN193189 induced hepatotoxicity in teleost fish Poecilia latipinna. Ranadive I et al. Drug Chem Toxicol. (2018)
  • [Bone Morphogenetic Proteins from CT26 Regulate the Expression of PD-L1 in Murine Dendritic Cells and Macrophages]. Zhao MY et al. Sichuan Da Xue Xue Bao Yi Xue Ban. (2017)
  • Towards a defined ECM and small molecule based monolayer culture system for the expansion of mouse and human intestinal stem cells. Tong Z et al. Biomaterials. (2018).

1 review for LDN193189 (1062368-24-4)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The LDN193189 (1062368-24-4) is high purity,also customer service is pretty nice !gotta try!!

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