Key Specifications Table
|Empirical Formula||CAS #|
|C₂₅H₂₂N₆ • 4HCl•3H₂O||1062368-62-0|
Pricing & Availability
An invalid quantity was specified. The product quantity has been adjusted.
|5.09882.0001||Glass bottle||10 mg||
This product has been discontinued.
A cell-permeable pyrazoloquinoline analog of Dorsomorphin (AMPK Inhibitor, Compound C, Cat. No. 480066) that potently inhibits the transcriptional activity of BMP type 1 receptors ALK 2 and 3 (IC50 = 5 and 30 nM, respectively) with minimal effect on activin and the TGF-β type 1 receptors ALK4, 5, and 7 (IC50 ~500 nM). Also reported to block the activity of RIPK2 (IC50 = 25 nM) and germinal central kinase (GCK; IC50 = 80 nM). At higher concentration, it inhibits the activity of ALK6 (IC50 = 150 nM). Also reported to block BMP-4- induced phosphorylation of SMAD 1, 5, and 8 (IC50 ~ 5 nM) in murine pulmonary artery smooth muscle cells. Shown to be about 200-fold more potent when compared to Dorsomorphin. Exhibits desirable pharmacokinetic properties with a half life of 1.6 h, low clearance in liver microsomes (CLint = 16.9 ml/min/mg protein), and a satisfactory exposure following a single intraperitoneal dose of 3 mg/kg in mice (AUC∞ = 1000 ng . h/ml). Directs differentiation of pluripotent stem cells toward a specified lineage.
|Synonyms||DM-3189, ALK2/3/6 Inhibitor, LDN193189, RIP2 Inhibitor II, Bone Morphogenetic Protein Inhibitor IV, RIPK2 Inhibitor II|
|Formulation||Supplied as a 10 mM solution (10 mg in 1.65 ml) in H₂O.|
|Hill Formula||C₂₅H₂₂N₆ • 4HCl•3H₂O|
|Chemical formula||C₂₅H₂₂N₆ • 4HCl•3H₂O|
|Secondary target||RIPK2, GCK|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Mohedas, A.H., et al. 2013. ACS Chem. Biol. 8, 1291.
Chambers, S.M., et al. 2012. Nat. Biotechnol. 30, 715.
Vogt, J., et al. 2011. Cell. Signal. 23, 1831.
Hao, J., et al. 2010. ACS Chem. Biol. 5, 245.
Cuny, G.D., et al. 2008. Bioorg. Med. Chem. Lett. 18, 4388.
Yu, P.B., et al. 2008. Nat. Med. 14, 1363.
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.