LDN-214117

SKU: orb1226029

Description

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.

Key Properties

• CAS Number: 1627503-67-6
• MW: 419.5161
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₉N₃O₃
• SMILES: COC1=C(OC)C(OC)=CC(C2=C(C)N=CC(C3=CC=C(N4CCNCC4)C=C3)=C2)=C1
• Target: TGFBR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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 cells. Concentration: 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LDN214117

Quick Database Links

Gene Symbol

TGFBR