LDN193189

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LDN193189 是一种有效的选择性 BMP I 型受体，可抑制 BMP4 诱导的 SMAD1/5/8 磷酸化，IC50 为 5 nM。

LDN193189 is a potent, selective BMP type I receptor that inhibits BMP4-induced phosphorylation of SMAD1/5/8 with IC50 of 5 nM, displays >200-fold selectivity for BMP signaling over TGF-β signaling (IC50>1,000 nM); efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7; also blocks the transcriptional activity induced by either constitutively active ALK2 R206H or ALK2 Q207D mutant proteins, affects BMP-induced osteoblast differentiation, attenuates ectopic ossification in vivo.(In Vitro):LDN193189 (GMP) (250 nM; 0-7 d) induces human pluripotent stem cells (hPSC) directly differentiates into midbrain dopamine neurons (mDA).LDN193189 (GMP) (200 nM) induces the generation of glucose-responsive β cells from hPSCs in vitro.

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. Western Blot Analysis Cell Line:Primary human myoblasts, C2C12 cells Concentration:0.5 μM Incubation Time:30 min Result:Inhibited GDF8-induced signaling pathways in undifferentiated and in differentiated primary human myoblasts and in C2C12 premyoblasts.

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. Animal Model:Ahymic NMRI nude female mice (6-week-old)Dosage:3 mg/kg Administration:Itraperitoneal, daily, for 35 days Result:Ehanced etastases development in vivo.Animal Model:C57BL/6 mice Dosage:3 mg/kg Administration:Intraperitoneal, single Result:Diminished ectopic bone formation and preserved joint spaces over the same interval without inducing fractures, osteopenia or skeletal abnormalities.

LDN 193189 | LDN-193189 | DM-3189

Angiogenesis

ALK

ALK2|ALK3

Cancer

——

1062368-24-4

406.4824

C25H22N6

>98% (HPLC)

Ethanol: 0.25 mg/mL (Need ultrasonic and warming); DMSO: < 0.1 mg/mL; H2O: < 0.1 mg/mL

C1CN(CCN1)C1=CC=C(C=C1)C1=CN2N=CC(=C2N=C1)C1=CC=NC2=CC=CC=C12

Quinoline, 4-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-

(-20℃)

With Ice Pack

≥ 2 years