LDN-214117
SIGMA/SML1119 - ≥98% (HPLC)
Synonym: 1-
Empirical Formula (Hill Notation): C25H29N3O3
Molecular Weight: 419.52
Linear Formula: C25H29N3O3
Product Type: Chemical
| assay | ≥98% (HPLC) |
| color | white to beige |
| form | powder |
| InChI | 1S/C25H29N3O3/c1-17-22(19 |
| InChI key | BHUXVRVMMYAXKN-UHFFFAOYSA |
| Quality Level | 100  |
| SMILES string | CC(C(C1=CC(OC)=C(OC)C(OC) |
| solubility | DMSO: 10 mg/mL, clear |
| storage temp. | 2-8°C |
| Application: | LDN-214117 has been used in structure-activity relationship (SAR) study to evaluate its potency on selective inhibition of activin receptor-like kinase-2 (ALK2) through the kinome-wide selectivity of (LDN-214117) via enzymatic kinase profiling. |
| Biochem/physiol Actions: | LDN-214117 is a selective inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with high selectivity for BMP versus TGF-β signaling, and low cytotoxicity. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM, followed by TNIK, RIPK2, and ABL1. LDN-214117 has a cell-based IC50 for BMP6 of approximately 100 nM and 164-fold selectivity for BMP6 versus TGF-β1. Fibrodysplasia ossificans progressiva (FOP) is a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 had nearly identical binding affinity for wild-type ALK2 and each of the FOP-causing mutants tested. |
| Packaging: | 5, 25 mg in glass bottle |
| Symbol |  GHS06 |
| Signal word | Danger |
| Hazard statements | H301 |
| Precautionary statements | P301 + P310 |
| RIDADR | UN 2811 6.1 / PGIII |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 51111800 |