Stemolecule™ BMP Inhibitor LDN-193189

Stemolecule™ BMP Inhibitor LDN-193189

Stemolecule^TM BMP Inhibitor LDN-193189 was derived from structure-activity relationship studies of Dorsomorphin¹ and functions primarily through inhibition of BMP type I receptors ALK2 and ALK3 (IC₅₀ = 5 nM and 30 nM respectively), thereby preventing Smad 1, Smad5, and Smad8 phosphorylation^2,3. LDN-193189 only weakly inhibits ALK4, ALK5, and ALK7 (IC50 >500 nM)². BMP signaling coordinates developmental patterning and has essential physiological roles in mature organisms^4,5. LDN-193189 has been used to reduce ectopic ossification in a mouse model of fibrodysplasia ossificans progressiva².

References

1. Yu, P.B., Hong, C.C., Sachidanandan, C., Babitt, J.L., Deng, D.Y., Hoyng, S.A., Lin, H.Y., Bloch, K.D., Peterson, R.T. (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol 4: 33-41.
2. Yu, P.B., Deng, D.Y., Lai, C.S., Hong, C.C., Cuny, G.D., Bouxsein, M.L., Hong, D.W., McManus, P.M., Katagiri, T., Sachidanandan, C., Kamiya, N., Fukuda, T., Mishina, Y., Peterson, R.T., Bloch, K.D. (2008) BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med 14: 1363-9.
3. Cuny, G.D., Yu, P.B., Laha, J.K., Xing, X., Liu, J.F., Lai, C.S., Deng, D.Y., Sachidanandan, C., Bloch, K.D., Peterson, R.T. (2008) Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorg Med Chem Lett 18: 4388-92.
4. Heisenberg, C.P., Solnica-Krezel, L. (2008) Back and forth between cell fate specification and movement during vertebrate gastrulation. Curr Opin Genet Dev 18: 311-6.
5. Cain, J.E., Hartwig, S., Bertram, J.F., Rosenblum, N.D. (2008) Bone morphogenetic protein signaling in the developing kidney: present and future. Differentiation 76: 831-42.

For research use only. Not for use in diagnostic procedures. Not for resale.

Stemolecule™ BMP Inhibitor LDN-193189

Size / Quantity	2 mg
Alternate Name	4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline, DM-3189
Chemical Formula	C25H22N6
Structure
Formulation	Yellow powder
Molecular Weight	406.48
Purity	>95%
Solubility	Soluble in Chloroform (10 mM). For a 10 mM concentrated stock solution, reconstitute the compound by adding 500 µl of Chloroform to the entire contents of the vial. Subsequently, dilute the stock solution 1 to 10 into DMSO prior to adding to an aqueous solution. Note: for most cells, the maximum tolerance to Chloroform is <10 µM.
Storage	Store at 4oC. Protect from light. Following reconstitution, store aliquots at -20C.
Stability	Stock solutions stable at -20°C for 6 months.
Quality Control	The purity of BMP Inhibitor LDN-193189 was determined by HPLC analysis. The accurate mass and structure of BMP Inhibitor LDN-193189 was determined by mass spectrometry and NMR, respectively. Cellular toxicity of BMP Inhibitor LDN-193189 was tested on mouse ES cells.
References	Yu, P.B., Hong, C.C., Sachidanandan, C., Babitt, J.L., Deng, D.Y., Hoyng, S.A., Lin, H.Y., Bloch, K.D., Peterson, R.T. (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol 4: 33-41. Yu, P.B., Deng, D.Y., Lai, C.S., Hong, C.C., Cuny, G.D., Bouxsein, M.L., Hong, D.W., McManus, P.M., Katagiri, T., Sachidanandan, C., Kamiya, N., Fukuda, T., Mishina, Y., Peterson, R.T., Bloch, K.D. (2008) BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med 14: 1363-9. Cuny, G.D., Yu, P.B., Laha, J.K., Xing, X., Liu, J.F., Lai, C.S., Deng, D.Y., Sachidanandan, C., Bloch, K.D., Peterson, R.T. (2008) Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorg Med Chem Lett 18: 4388-92. Heisenberg, C.P., Solnica-Krezel, L. (2008) Back and forth between cell fate specification and movement during vertebrate gastrulation. Curr Opin Genet Dev 18: 311-6. Cain, J.E., Hartwig, S., Bertram, J.F., Rosenblum, N.D. (2008) Bone morphogenetic protein signaling in the developing kidney: present and future. Differentiation 76: 831-42.
Notice to Purchaser	Purchaser represents and warrants that it will use Stemolecule™ BMP Inhibitor LDN-193189 purely for research purposes, not for diagnostic use, not for resale, and not for use in humans or veterinary applications. Stemgent will not be held responsible for patent infringement or other violations that may occur with the use of our products.

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