LDN 193189 Inhibitor CAS No. 1062368-24-4

Cat. No.	Name	Size	Price
KI1121	LDN 193189	2 mg	$176
	LDN 193189	5 mg	$272
	LDN 193189	25 mg	$912

Chemical Characteristic

Product Name	LDN 193189
Synonyms	DM-3189
CAS No.	1062368-24-4
Molecular Weight	406.48
Formula	C₂₅H₂₂N₆
Chemical Name	4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline
Smiles	n1ccc(c2ccccc12)c1c2ncc(cn2nc1)c1ccc(cc1)N1CCNCC1
Chemical Structure

Biological activities

LDN 193189 is a potent SMAD 1/5/8 phosphorylation inhibitor. The IC50 of LDN 193189 is 4.9 nM against BMP4-induced phosphorylation of SMAD1/5/8.^[1] LDN 193189 affects not only the Smad but also the non-Smad signalling pathways induced by either BMP2, BMP6 or GDF5. LDN 193189 inhibits BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. LDN 193189 inhibits activation of Smad1/5/8, p38 and Akt by different BMP family members. LDN 193189 inhibits BMP2 mediated activation of Smad and non-Smad signalling cascades including their downstream targets. ^[2] LDN 193189 significantly prevents intersomitic vessel formation at 20 µM.^[3] LDN 193189 blocks both BMP6-mediated Hamp mRNA induction and Smad1/5/8 phosphorylation in primary rat hepatocytes in vitro.^[4] In zebrafish, LDN 193189 reduces hepcidin expression by transgenic expression of IL-6.^[5]

Protocols

In vivo LDN 193189 HCl salt is dissolved in sterile, endotoxin-free water at 1.5 mg/mL.^[5]

References

[1] Cuny GD, et al. Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorg Med Chem Lett. 2008, 18(15): 4388-4392. [2] Boergermann JH,et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J Biochem Cell Biol. 2010, 42(11): 1802-1807. [3] Hao J, et al. In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem Biol. 2010, 5(2): 245-253. [4] Theurl I, et al. Pharmacologic inhibition of hepcidin expression reverses anemia of chronic inflammation in rats. Blood. 2011, 118(18): 4977-4984. [5] Steinbicker AU, et al. Inhibition of bone morphogenetic protein signaling attenuates anemia associated with inflammation. Blood. 2011, 117(18): 4915-4923.

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