2387510-88-3

2387510-88-3 structure

Name: OD36 hydrochloride
Chemical Name: OD36 hydrochloride
CAS Number: 2387510-88-3
Molecular Formula: C₁₆H₁₆Cl₂N₄O₂
Molecular Weight: 367.23
Catalog: Signaling Pathways Apoptosis RIP kinase
Create Date: 2022-10-11 20:25:04
Modify Date: 2024-01-12 19:01:32
OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM[1][2].

Name	OD36 hydrochloride

Description	OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM[1][2].
Related Catalog	Signaling Pathways >> Apoptosis >> RIP kinase Research Areas >> Inflammation/Immunology
Target	RIPK2:5.3 nM (IC50) ACVR1:37 nM (Kd) ACVR1:47 nM (IC50) ALK2 R206H:22 nM (IC50)
In Vitro	OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively[1]. OD36 shows activity against ALK1 with a KD of 90 nM[2]. OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation[2]. OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells[2]. Preincubation of fibrodysplasia ossificans progressiva (FOP) endothelial colony-forming cells (ECFCs) with OD36 (0.5 μM) completely prevents the activation of Smad1/5 and gene targets ID-1 and ID-3 in response to activin A[2]. Western Blot Analysis[2] Cell Line: KS483 cells Concentration: 0.1, 0.2, and 1 μM Incubation Time: 24 h Result: Inhibited BMP-6 induced p-Smad1/5.
In Vivo	OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model[3]. Animal Model: C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis[3] Dosage: 6.25 mg/kg Administration: Intraperitoneal injection, 30 min prior to MDP Result: Inhibited the recruitment of inflammatory cells to the peritoneum, specifically that of neutrophils, and, to a lesser extent, lymphocytes. Decreased RIPK2-specific genes as well as inflammatory cytokine and chemokine gene expression.
References	[1]. Justine T Tigno-Aranjuez, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease. J Biol Chem. 2014 Oct 24;289(43):29651-64. [2]. Gonzalo Sánchez-Duffhues, et al. Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva-Derived Endothelial Cells. JBMR Plus. 2019 Oct 7;3(11):e10230. [3]. Tigno-Aranjuez JT, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease. J Biol Chem. 2014 Oct 24;289(43):29651-64.

Molecular Formula	C₁₆H₁₆Cl₂N₄O₂
Molecular Weight	367.23

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