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TGF-beta&Smad

K02288 (1431985-92-0)

K02288 is a potent inhibitor of BMP signaling. K02288 has in vitro activity against ALK2 at low nanomolar concentrations similar to the current lead compound LDN-193189. K02288 specifically inhibited the BMP-induced Smad pathway without affecting TGF-β signaling and induced dorsalization of zebrafish embryos.

Not Intended for Therapeutic Use. For research use only.

CAS: 1431985-92-0 Category

K02288 (1431985-92-0) Description:

K02288 is a selective and potent inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with IC50s in the range 1–2 nM against ALK1 and ALK2. K02288 has IC50 values of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6 respectively and IC50s of 34.4, 302, 321 and 220 nM for other ALKs (3, 4, 5) and ActRIIA. K02288 specifically inhibited the BMP-induced Smad pathway without affecting TGF-β signaling and induced dorsalization of zebrafish embryos.

K02288 is functionally similar to dorsomorphin, which is known to be the first small-molecule for BMP signaling inhibition.[2][3]

BMP signalling is associated with many important physiological processes. It acts a central regulator of developmental processes such as organogenesis, gastrulation, mesoderm induction and endochondral bone formation. BMP signals are also related to diseases including pulmonary hypertension, juvenile polyposis syndrome, fibrodysplasia ossificans progressiva and hereditary hemorrhagic telangiectasia syndrome. BMP signaling inhibition might serve as a tool to study its role in other biological processes

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. K02288 is a 2-aminopyridine-based inhibitor of ALK1 and ALK2 with IC50 values of 1.8 and 1.1 nM, respectively.2 It is less selective for ALK3, 4, 5, and 6 subtypes and the type II BMP receptor ActRIIA, demonstrating IC50 values of 34.4, 302, 321, 6.4, and 220 nM, respectively. K02288 can prevent BMP4-induced SMAD1/5/8 pathway activation in vitro (IC50 = 100 nM) without affecting TGF-β signaling. Furthermore, at 8-10 µM, K02288 has been used to induce the dorsalization of zebrafish embryos. Through specific inhibition of BMP signaling, this compound can be used to research stem cell biology and disease models of musculoskeletal dysplasia and cancer.

K02288 (1431985-92-0) Specifications:

Product Name K02288
Synonyms K-02288; K 02288;
Chemical Name 3-[6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol
Purity >98%
CAS Number 1431985-92-0
Molecular Formula C20H20N2O4
Molecular Weight 352.39 g/mol
Monoisotopic Mass 352.142 g/mol
MDL number MFCD26936347
InChIKey CJLMANFTWLNAKC-UHFFFAOYSA-N
InChi Code InChI=1S/C20H20N2O4/c1-24-17-9-13(10-18(25-2)19(17)26-3)16-8-14(11-22-20(16)21)12-5-4-6-15(23)7-12/h4-11,23H,1-3H3,(H2,21,22)
SMILES COC1=CC(=CC(=C1OC)OC)C2=C(N=CC(=C2)C3=CC(=CC=C3)O)N
Form powder
Color white to beige
Solubility  Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).
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 inhibitor

 


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RIDADR NONH for all modes of transport

References:

1.Transforming growth factor β-inhibitor Repsox downregulates collagen expression of scleroderma dermal fibroblasts and prevents bleomycin-induced mice skin fibrosis. Ide M, Jinnin M, Tomizawa Y, Wang Z, Kajihara I, Fukushima S, Hashizume Y, Asano Y, Ihn H. Exp Dermatol. 2017 Nov;26(11):1139-1143. doi: 10.1111/exd.13366. Epub 2017 Aug 25.

2.[Bushen Tiaojing Recipe Regulated Expressions of BMPR I[/ALK6-Smads in Mouse Oocytes Cul- ture in vitro]. Sun XH, Fan LJ, Li L, Wei XC, Liu YH, Geng DD, Gu XX, Du HL. Zhongguo Zhong Xi Yi Jie He Za Zhi. 2016 Oct;36(10):1241-1246. Chinese.

3.Rac1 promotes chondrogenesis by regulating STAT3 signaling pathway. Kim H, Sonn JK. Cell Biol Int. 2016 Sep;40(9):976-83. doi: 10.1002/cbin.10635. Epub 2016 Jun 28.

4.BMP Signaling Regulates Bone Morphogenesis in Zebrafish through Promoting Osteoblast Function as Assessed by Their Nitric Oxide Production. Windhausen T, Squifflet S, Renn J, Muller M. Molecules. 2015 Apr 24;20(5):7586-601. doi: 10.3390/molecules20057586.

1 review for K02288 (1431985-92-0)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The K02288 (1431985-92-0) is high purity,also customer service is pretty nice !gotta try!!

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