OD36 hydrochloride 是一种RIPK2抑制剂，IC50为 5.3 nM。OD36 hydrochloride 是一种大环抑制剂，可与ALK2激酶 ATP 口袋有效结合。OD36 hydrochloride 靶向作用于 ALK2，KD为 37 nM。

OD36hydrochloride is a RIPK2 inhibitor with an IC 50 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 K D s of 37 nM [1] [2].

OD36 also inhibits ALK2 and ALK2 R206H with IC 50 s of 47 and 22 nM, respevtively [1]. OD36 shows activity against ALK1 with a K D 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.

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.

2387510-88-3

C16H16Cl2N4O2

367.23

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years