Product Name :
LDN-214117
Description:
LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. There are currently no effective therapies for fibrodysplasia ossificans progressiva (FOP), a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 shows a high degree of selectivity for ALK2 and low cytotoxicity that could provide a template for preclinical development.
CAS:
1627503-67-6
Molecular Weight:
419.52
Formula:
C25H29N3O3
Chemical Name:
1-(4-(6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine
Smiles :
CC1=NC=C(C=C1C1=CC(OC)=C(OC)C(=C1)OC)C1C=CC(=CC=1)N1CCNCC1
InChiKey:
BHUXVRVMMYAXKN-UHFFFAOYSA-N
InChi :
InChI=1S/C25H29N3O3/c1-17-22(19-14-23(29-2)25(31-4)24(15-19)30-3)13-20(16-27-17)18-5-7-21(8-6-18)28-11-9-26-10-12-28/h5-8,13-16,26H,9-12H2,1-4H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Adenosine receptor antagonist 2} web|{Adenosine receptor antagonist 2} Antagonist|{Adenosine receptor antagonist 2} TGF-beta/Smad|{Adenosine receptor antagonist 2} Technical Information|{Adenosine receptor antagonist 2} Formula|{Adenosine receptor antagonist 2} manufacturer}
Shelf Life:
≥12 months if stored properly.{{Stavudine} MedChemExpress|{Stavudine} HIV|{Stavudine} Purity & Documentation|{Stavudine} Formula|{Stavudine} supplier|{Stavudine} Epigenetics}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:35227773
Additional information:
LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. There are currently no effective therapies for fibrodysplasia ossificans progressiva (FOP), a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 shows a high degree of selectivity for ALK2 and low cytotoxicity that could provide a template for preclinical development.|Product information|CAS Number: 1627503-67-6|Molecular Weight: 419.52|Formula: C25H29N3O3|Synonym:|LDN 214117|LDN214117|LDN-214117|Chemical Name: 1-(4-(6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine|Smiles: CC1=NC=C(C=C1C1=CC(OC)=C(OC)C(=C1)OC)C1C=CC(=CC=1)N1CCNCC1|InChiKey: BHUXVRVMMYAXKN-UHFFFAOYSA-N|InChi: InChI=1S/C25H29N3O3/c1-17-22(19-14-23(29-2)25(31-4)24(15-19)30-3)13-20(16-27-17)18-5-7-21(8-6-18)28-11-9-26-10-12-28/h5-8,13-16,26H,9-12H2,1-4H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 100 mg/mL (238.37 mM)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|The kinase most highly inhibited by LDN-214117 is ALK2 (IC50, 24 nM), followed by TNIK, RIPK2, and ABL1. LDN-214117 demonstrates selective inhibition of ALK2 and ALK1 in preference to ALK3 kinase activity. LDN-214117 exhibits relatively selective inhibition of BMP6 versus BMP2 or BMP4. In a cell-based assay, LDN-214117 exhibits a selective inhibition on BMP6 with IC50 of approximately 100 nM, and 164-fold selectivity for BMP6 versus TGF-β1.|References:|Mohedas AH, et al. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15.Products are for research use only. Not for human use.|
