|
Back to products
Browse products
Approved anticancer agents
Anticancer agents in trials
Anticancer agents
in preclinical trials
Anticancer molecular libraries
Other drug agents
Drug intermediates
Bio-reagents and biochemicals
|
MedKoo product information:
LDN-193189
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.
|
MedKoo Code#: 501105
|
|
Name: LDN-193189
|
|
CAS#: 1062368-24-4
Synonym:
LDN-193189
IUPAC/Chemical name:
4-[6-(4-Piperazin-1-yl-phenyl)-pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
|
|
Chemical structure
|
Theoretical analysis
|
|

|
MedKoo Code#: 501105
Name: LDN-193189
CAS#: 1062368-24-4
Chemical Formula: C25H22N6
Exact Mass: 406.19059
Molecular Weight: 406.48238
Elemental Analysis: C, 73.87; H, 5.46; N,
20.67
|
|
Availability and price:
This agent is available in
stock.
To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
|
|
Information about this agent
|
LDN193189 is a highly potent BMP inhibitor, prevents
Smad1, Smad5, and Smad8 phosphorylation through inhibition of BMP type I
receptors ALK2 (IC50=5nM) and ALK3 (IC50=30 nM). Its inhibition of ALK4,
ALK5, and ALK7 is weak (IC50 >500 nM). As BMP signaling coordinates
developmental patterning and has essential physiological roles in mature
organisms, LDN-193189 is used to reduce ectopic ossification in a mouse
model.
1: Saeed O, Otsuka F, Polavarapu R, Karmali V, Weiss
D, Davis T, Rostad B, Pachura K, Adams L, Elliott J, Taylor WR, Narula
J, Kolodgie F, Virmani R, Hong CC, Finn AV. Pharmacological Suppression
of Hepcidin Increases Macrophage Cholesterol Efflux and Reduces Foam
Cell Formation and Atherosclerosis. Arterioscler Thromb Vasc Biol. 2011
Nov 17. [Epub ahead of print] PubMed PMID: 22095982.
2: Kudo TA, Kanetaka H, Mizuno K, Ryu Y, Miyamoto Y, Nunome S, Zhang Y,
Kano M, Shimizu Y, Hayashi H. Dorsomorphin stimulates neurite outgrowth
in PC12 cells via activation of a protein kinase A-dependent MEK-ERK1/2
signaling pathway. Genes Cells. 2011 Nov;16(11):1121-32. doi:
10.1111/j.1365-2443.2011.01556.x. Epub 2011 Oct 12. PubMed PMID:
21988724.
3: Vogt J, Traynor R, Sapkota GP. The specificities of small molecule
inhibitors of the TGFß and BMP pathways. Cell Signal. 2011
Nov;23(11):1831-42. Epub 2011 Jun 29. PubMed PMID: 21740966.
4: Cross EE, Thomason RT, Martinez M, Hopkins CR, Hong CC, Bader DM.
Application of small organic molecules reveals cooperative TGFβ and BMP
regulation of mesothelial cell behaviors. ACS Chem Biol. 2011 Sep
16;6(9):952-61. Epub 2011 Jul 20. PubMed PMID: 21740033; PubMed Central
PMCID: PMC3177035.
5: Theurl I, Schroll A, Sonnweber T, Nairz M, Theurl M, Willenbacher W,
Eller K, Wolf D, Seifert M, Sun CC, Babitt JL, Hong CC, Menhall T,
Gearing P, Lin HY, Weiss G. Pharmacologic inhibition of hepcidin
expression reverses anemia of chronic inflammation in rats. Blood. 2011
Nov 3;118(18):4977-84. Epub 2011 Jul 5. PubMed PMID: 21730356; PubMed
Central PMCID: PMC3208302.
6: Lee YC, Cheng CJ, Bilen MA, Lu JF, Satcher RL, Yu-Lee LY, Gallick GE,
Maity SN, Lin SH. BMP4 promotes prostate tumor growth in bone through
osteogenesis. Cancer Res. 2011 Aug 1;71(15):5194-203. Epub 2011 Jun 13.
PubMed PMID: 21670081; PubMed Central PMCID: PMC3148283.
7: Yonezawa T, Lee JW, Hibino A, Asai M, Hojo H, Cha BY, Teruya T, Nagai
K, Chung UI, Yagasaki K, Woo JT. Harmine promotes osteoblast
differentiation through bone morphogenetic protein signaling. Biochem
Biophys Res Commun. 2011 Jun 3;409(2):260-5. Epub 2011 May 6. PubMed
PMID: 21570953.
8: Steinbicker AU, Sachidanandan C, Vonner AJ, Yusuf RZ, Deng DY, Lai
CS, Rauwerdink KM, Winn JC, Saez B, Cook CM, Szekely BA, Roy CN, Seehra
JS, Cuny GD, Scadden DT, Peterson RT, Bloch KD, Yu PB. Inhibition of
bone morphogenetic protein signaling attenuates anemia associated with
inflammation. Blood. 2011 May 5;117(18):4915-23. Epub 2011 Mar 10.
PubMed PMID: 21393479; PubMed Central PMCID: PMC3100698.
9: Wang L, Trebicka E, Fu Y, Ellenbogen S, Hong CC, Babitt JL, Lin HY,
Cherayil BJ. The bone morphogenetic protein-hepcidin axis as a
therapeutic target in inflammatory bowel disease. Inflamm Bowel Dis.
2012 Jan;18(1):112-9. doi: 10.1002/ibd.21675. Epub 2011 Feb 23. PubMed
PMID: 21351217; PubMed Central PMCID: PMC3139830.
10: Shi S, Hoogaars WM, de Gorter DJ, van Heiningen SH, Lin HY, Hong CC,
Kemaladewi DU, Aartsma-Rus A, ten Dijke P, 't Hoen PA. BMP antagonists
enhance myogenic differentiation and ameliorate the dystrophic phenotype
in a DMD mouse model. Neurobiol Dis. 2011 Feb;41(2):353-60. Epub 2010
Oct 16. PubMed PMID: 20940052.
11: Katagiri T, Kamizono J, Nakashima Y, Kitoh H, Susami T, Haga N.
[Cytokines in bone diseases. BMP signaling and fibrodysplasia ossificans
progressiva]. Clin Calcium. 2010 Oct;20(10):1510-7. Review. Japanese.
PubMed PMID: 20890033.
12: Cannon JE, Upton PD, Smith JC, Morrell NW. Intersegmental vessel
formation in zebrafish: requirement for VEGF but not BMP signalling
revealed by selective and non-selective BMP antagonists. Br J Pharmacol.
2010 Sep;161(1):140-9. PubMed PMID: 20718746; PubMed Central PMCID:
PMC2962823.
13: Boergermann JH, Kopf J, Yu PB, Knaus P. Dorsomorphin and LDN-193189
inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J
Biochem Cell Biol. 2010 Nov;42(11):1802-7. Epub 2010 Aug 5. PubMed PMID:
20691279.
14: Yu PB, Deng DY, Lai CS, Hong CC, Cuny GD, Bouxsein ML, Hong DW,
McManus PM, Katagiri T, Sachidanandan C, Kamiya N, Fukuda T, Mishina Y,
Peterson RT, Bloch KD. BMP type I receptor inhibition reduces
heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9.
Epub 2008 Nov 30. Erratum in: Nat Med. 2009 Jan;15(1):117. PubMed PMID:
19029982; PubMed Central PMCID: PMC2846458.
15: Cuny GD, Yu PB, Laha JK, Xing X, Liu JF, Lai CS, Deng DY,
Sachidanandan C, Bloch KD, Peterson RT. Structure-activity relationship
study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorg
Med Chem Lett. 2008 Aug 1;18(15):4388-92. Epub 2008 Jun 27. PubMed PMID:
18621530; PubMed Central PMCID: PMC2570262.
|
Contact MedKoo:
Email:
sales@medkoo.com
(Keyword; CAS#; MedKoo code#)
|