LDN-214117

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

一种有效的选择性 ALK2 抑制剂，生化 IC50 为 24 nM，BMP6 的细胞 IC50 为 100 nM。

A potent and selective ALK2 inhibitor with a biochemical IC50 of 24 nM, a cell-based IC50 for BMP6 of 100 nM; displays 164-fold selectivity for BMP6 versus TGF-β1; a highly selective probes of BMP-mediated cellular physiology.

LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC50 value of 24 nM.LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC50 values of 27 nM, 1,171 nM and 3,000 nM, respectively.LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC50 values of 100 nM, 1,022 nM and 960 nM, respectively.LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC50 values of 16,000 nM.LDN-214117 (5 μM, 30 min, 3 h and 24 h) has time-dependent effect activity on gene regulation level and/ or a BMP signaling pathway other than SMAD-dependent that is responsible for ID1 targeting.LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H.LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells.LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids. Cell Viability Assay Cell Line:LCLC-103H cells Concentration:5 μM Incubation Time:24 h, 48 h, 72 h and 96 h Result:Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point.Western Blot Analysis Cell Line:LCLC-103H cells Concentration:5 μM Incubation Time:30 min, 3 h and 24 h Result:Diminished the increase of ID1 protein.Apoptosis Analysis Cell Line:LCLC-103H cellsConcentration:5 μM Incubation Time:24 h, 48 h, 72 h and 96 h Result:Induced considerable death of LCLC-103H cells.RT-PCR Cell Line:LCLC-103H cells Concentration:5 μM Incubation Time:24 h, 48 h and 72 h Result:Induced distinct gene expression patterns for the two EMTTFs.Cell Migration Assay Cell Line:LCLC-103H cells Concentration:5 μM Incubation Time:0 h, 24 h and 48 h Result:Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling.

LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice. Animal Model:NOD.SCID mice Dosage:25 mg/kg Administration:p.o., daily, for 14 days Result:Showed good-tolerated in mice.

LDN214117

TGF-beta/Smad

TGFBR

ALK2

Cancer

——

1627503-67-6

419.5161

C25H29N3O3

>98% (HPLC)

10 mM in DMSO

COC1=C(OC)C(OC)=CC(C2=C(C)N=CC(C3=CC=C(N4CCNCC4)C=C3)=C2)=C1

Piperazine, 1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years