LDN-214117

SKU: orb1307025

Description

LDN-214117

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1627503-67-6
• MW: 419.52
• Purity: 99.85%
• Formula: C₂₅H₂₉N₃O₃
• SMILES: COc1cc(cc(OC)c1OC)-c1cc(cnc1C)-c1ccc(cc1)N1CCNCC1
• Target: ALK,TGF-beta/Smad
• Solubility: DMSO:4.2 mg/mL (10.01 mM);Ethanol:42 mg/mL (100.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.38 mM)

Bioactivity

• Target IC50:
  ALK2:24 nM
• In Vivo:
  LDN-214117 exhibits Selective Inhibition towards BMP6 over BMP2 or BMP4. In cell-based assays, it preferentially inhibits BMP6 with an IC50 around 100 nM, being 164 times more Selective for BMP6 than for TGF-β1. Among kinases, LDN-214117 most effectively inhibits ALK2 IC50 = 24 nM), followed by TNIK, RIPK2, and ABL1. It specifically inhibit the kinase activity of ALK2 and ALK1 more than that of ALK3.
• Cell Research:
  Cells are seeded at 25000 cells per well in 96-well plates and incubated for 2 h at 37℃nd 5% CO2. Compounds of LDN-214117 or DMSO are diluted in DMEM and added at final compound concentration of 1, 10, and 100 μM. Cells are incubated for 4 and 24 h, after whic the media is discarded. Cells are lysed by adding 30 μL of passive lysis buffer and shaken at RT for 15 min. Cell viability is determined by quantifyin the ATP present in Each well by adding 10 μL of Cell Titer Glo per well and measurin the light output by Spectramax L luminometer. Data is normalized to 100% viability for cells receiving only DMSO.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ALK3, ALK2, ALK5, ALK1, bone morphogenetic proteins (BMPs), BMP6, BMP4, BMP2, diffuse intrinsic pontine glioma(DIPG), oral, fibrodysplasia ossificans progressiva (FOP), LDN 214117, LDN214117, LDN-214117, Transforming growth factor beta receptors, TGFβ, TGFbeta/Smad, TGF-β Receptor, TGF-β/Smad, TGF-b/Smad, TGFb, TGFbeta, TGF-beta, Smad, type I receptor kinases

Compound Identifiers

PubChem CID

91754554