RIPK2 inhibitor OD36

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RIPK2 抑制剂 OD36 是一种有效、特异性、ATP 竞争性的 RIPK2 抑制剂，IC50 为 5.3 nM。

RIPK2 inhibitor OD36 is a potent, specific, ATP-competitive inhibitor of RIPK2 with IC50 of 5.3 nM, inhibits Tyr and Ser/Thr-directed activities of RIPK2; inhibits both RIPK2 tyrosine autophosphorylation as well as downstream NF-κB and MAPK signaling induced by MDP, downregulates a panel of RIPK2 kinase-dependent genes; reduces cellular infiltration in an in vivo MDP-induced peritonitis model; also shows high affinity for cyclin G-associated kinase (GAK) with Ki of 3.8 nM.

OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively.OD36 shows activity against ALK1 with a KD of 90 nM.OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation.OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells.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.Western Blot Analysis Cell Line:KS483 cells Concentration:0.1, 0.2, and 1 μM Incubation Time:Result:Inhibited BMP-6 induced p-Smad1/5.

OD36 (6.25 mg/kg; i.p.; once) alleviates inflammation in an acute peritonitis mice model. Animal Model:C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitisDosage: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.

OD36 | OD-36 | OD 36

Apoptosis

RIP kinase

RIP kinase

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1638644-62-8

330.772

C16H15ClN4O2

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (100.76 mM)

ClC1=CC(C2=C3N=C(C=CN3N=C2)NCCOCCO4)=CC4=C1

(13Z,14E)-25-chloro-3,6-dioxa-9-aza-1(3,5)-pyrazolo[1,5-a]pyrimidina-2(1,3)-benzenacyclononaphane

(-20℃)

With Ice Pack

≥ 2 years