LDN-193189 2HCl

Research use only, not for human use.

LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.

LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.

LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 has weake effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7 with IC50 values of ≥ 500 nM.LDN-193189 binds ActRIIA with Kd value of 14 nM.LDN-193189 (0.5 μM; 30 min) targets GDF8 induced Smad2/3 signaling and repression of myogenic transcription factors.LDN-193189 (0.05, 0.5, 5 μM) efficiently inhibits GDF8 induced Smad3/4 reporter gene activity.LDN-193189 (0-5 μM) rescues myogenesis in myoblasts treated with GDF8.

LDN-193189 (i.p.; 3 mg/kg; daily; for 35 days) might affect the interaction between breast cancer cells and the bone environment.LDN-193189 (i.p.; 3 mg/kg; single) shows a reduction in ectopic ossification and functional impairment.

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Others

Other Targets

TGF-beta/Smad | ALK

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1435934-00-1

479.4

C25H24Cl2N6

>98% (HPLC)

In Vitro:?H2O : 11.11 mg/mL (23.17 mM; Ultrasonic)DMSO : 10 mg/mL (20.86 mM; Ultrasonic (<60°C)

C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=C6C=CC=CC6=NC=C1.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years