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LDN 214117 - ≥98%(HPLC), high purity , CAS No.1627503-67-6, Inhibitor of activin A receptor type 1;Inhibitor of activin A receptor type IL;Inhibitor of bone morphogenetic protein receptor type IA;Inhibitor of transforming growth factor beta receptor 1

Moligand™
≥98%(HPLC)

CAS#: 1627503-67-6
Formula: C₂₅H₂₉N₃O₃
Molecular Weight: 419.52
PubChem CID: 91754554

Item Number

L288873

Grouped product items
SKU	Size	Availability	Price
L288873-5mg	5mg	In stock	$64.90
L288873-10mg	10mg	In stock	$118.90
L288873-25mg	25mg	In stock	$238.90
L288873-50mg	50mg	In stock	$412.90
L288873-100mg	100mg	In stock	$641.90

Potent and selective ALK2 inhibitor

View related series

activin A receptor type 1 Inhibitor activin A receptor type IL Inhibitor bone morphogenetic protein receptor type IA Inhibitor transforming growth factor beta receptor 1 Inhibitor

Basic Description

Synonyms	LDN-214117；1-(4-(6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Potent and selective inhibitor of type I bone morphogenic protein (BMP) receptor ALK2 (IC50= 24 nM). Shows preference for ALK1 and ALK2 over ALK3 and 164-fold selectivity for BMP6 inhibition (IC50= 100 nM) over TGF-β1. Exhibits improved kinome selectivity
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of activin A receptor type 1;Inhibitor of activin A receptor type IL;Inhibitor of bone morphogenetic protein receptor type IA;Inhibitor of transforming growth factor beta receptor 1

Associated Targets

TGFBR1 Tchem TGF-beta receptor type-1 1 Activities

Discover Target: TGFBR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RIPK2 Tchem Receptor-interacting serine/threonine-protein kinase 2 0 Activities

Discover Target: RIPK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BMPR1A Tchem Bone morphogenetic protein receptor type-1A 1 Activities

Discover Target: BMPR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ACVR1 Tchem Activin receptor type-1 1 Activities

Discover Target: ACVR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ACVRL1 Tchem Serine/threonine-protein kinase receptor R3 1 Activities

Discover Target: ACVRL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NOD2 Tclin Nucleotide-binding oligomerization domain-containing protein 2 0 Activities

Discover Target: NOD2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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
InChi Key	BHUXVRVMMYAXKN-UHFFFAOYSA-N
Canonical SMILES	CC1=C(C=C(C=N1)C2=CC=C(C=C2)N3CCNCC3)C4=CC(=C(C(=C4)OC)OC)OC
Isomeric SMILES	CC1=C(C=C(C=N1)C2=CC=C(C=C2)N3CCNCC3)C4=CC(=C(C(=C4)OC)OC)OC
PubChem CID	91754554
Molecular Weight	419.52

Certificates

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5 results found

Lot Number	Certificate Type	Date	Item
K2219489	Certificate of Analysis	Sep 05, 2022	L288873
K2219490	Certificate of Analysis	Sep 05, 2022	L288873
K2219496	Certificate of Analysis	Sep 05, 2022	L288873
K2219505	Certificate of Analysis	Sep 05, 2022	L288873
K2219506	Certificate of Analysis	Sep 05, 2022	L288873

References

1. Shore EM, Xu M, Feldman GJ, Fenstermacher DA, Cho TJ, Choi IH, Connor JM, Delai P, Glaser DL, LeMerrer M et al.. (2006) A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and sporadic fibrodysplasia ossificans progressiva.. Nat Genet, 38 (5): (525-7). [PMID:16642017]
2. Kaplan FS, Xu M, Seemann P, Connor JM, Glaser DL, Carroll L, Delai P, Fastnacht-Urban E, Forman SJ, Gillessen-Kaesbach G et al.. (2009) Classic and atypical fibrodysplasia ossificans progressiva (FOP) phenotypes are caused by mutations in the bone morphogenetic protein (BMP) type I receptor ACVR1.. Hum Mutat, 30 (3): (379-90). [PMID:19085907]
3. Pignolo RJ, Shore EM, Kaplan FS. (2011) Fibrodysplasia ossificans progressiva: clinical and genetic aspects.. Orphanet J Rare Dis, 6 (3): (80). [PMID:22133093]
4. Nakahara Y, Katagiri T, Ogata N, Haga N. (2014) ACVR1 (587T>C) mutation in a variant form of fibrodysplasia ossificans progressiva: second report.. Am J Med Genet A, 164A (1): (220-4). [PMID:24259422]
5. Mohedas AH, Wang Y, Sanvitale CE, Canning P, Choi S, Xing X, Bullock AN, Cuny GD, Yu PB. (2014) Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.. J Med Chem, 57 (19): (7900-15). [PMID:25101911]

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