RIPK2-IN-8
RIPK2-IN-8 is an orally active and highly selective RIPK2 inhibitor (IC50 = 11 nM). RIPK2-IN-8 is highly selective for RIPK2 over RIPK1 (IC50 > 30,000 nM) and has a moderate inhibitory effect on RIPK3 (IC50 = 44.61 nM). RIPK2-IN-8 inhibits the NOD2-RIPK2 signaling pathway and the expression of the inflammatory cytokines IL-6 and TNFα, thereby exerting anti-inflammatory effects. RIPK2-IN-8 has demonstrated anti-inflammatory and hepatoprotective effects in an acute liver injury (ALI) model and can be used in ALI research.
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- CAS No.: 3036254-29-9
- Formule: C22H20FN5OS2
- Masse moléculaire:453.56
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
RIPK2 11 nM (IC50) |
RIPK3 44.61 nM (IC50) |
IL-6 |
In Vitro
RIPK2-IN-8 (Compound HY3)(0-10 μM, 0.5-6 h) delays NF-kB and MAPK activation without affecting protein expression or cell viability in L18-MDP (HY-148690)-stimulated THP-1 cells[1].
RIPK2-IN-8 (1 μM) shows almost no inhibitory activity against inflammation-related kinases, such as BTK, FLT3, JNK2α2, SAPK3, MSK1, MAPKAP-K2[1].
RIPK2-IN-8 has weak cytotoxicity against H9C2 cells(IC50 > 40 μM)[1].
RIPK2-IN-8 inhibits IL-8 production with an IC50 of 29 nM in Muramyl dipeptide (MDP) (HY-127090)-stimulated THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells were stimulated with L18-MDP
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Concentration:0 μM, 0.001 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
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Incubation Time:0.5 h, 6 h
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Result:Delayed phosphorylation of p65, p38, and JNK. At 1 μM, did not alter the total levels of p65, p38, JNK, and β-actin.
Did not affect phosphorylation of RIPK3 or MLKL, key markers of necroptotic signaling.
Parmacokinetics
In Vivo
RIPK2-IN-8 (5-20 mg/kg, p.o., once) exerts a liver-protective effect by inhibiting the expression of inflammatory cytokines, thereby reducing serum inflammatory markers and alleviating liver damage in Acetaminophen (APAP) (HY-66005)-induced ALI model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDP-induced (100 μg, i.p.) peritonitis mice (Female C57BL/6 at 8 weeks of age) model[1]
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Dosage:7.5 mg/kg, 15 mg/kg, 30 mg/kg
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Administration:p.o., once
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Result:Reduced IL-6 levels, with IL-6 levels dropping to 23.9 pg/mL at 30 mg/kg, comparable to the RIPK2-positive compound GSK2983559 (HY-112038A).
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Animal Model:APAP-induced (500 mg/kg, i.p.) ALI mice (Female C57BL/6 at 8 weeks of age) model[1]
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Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:p.o., once
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Result:Reduced ALT and AST levels, particularly in the high-dose group, where ALT and AST levels decreased to 202 and 275 U/L, respectively.
Reduced serum and mRNA levels of IL-6 and TNFα.
Chemical Information
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CAS No. 3036254-29-9
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Masse moléculaire 453.56
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Formule C22H20FN5OS2
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SMILES
CCC(NC1CCC(C2=CC(N=CN=C3NC4=CC(N=CS5)=C5C=C4F)=C3S2)=CC1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Zhao H, et al. Development of Thieno[3,2-d]pyrimidine derivatives as potent RIPK2 inhibitors with Prominent In vitro and In vivo anti-inflammatory efficacy. Eur J Med Chem. 2025 Jul 5;297:117932. [Content Brief]
[2]. Zhao H, et al. Development of Thieno[3,2-d]pyrimidine derivatives as potent RIPK2 inhibitors with Prominent In vitro and In vivo anti-inflammatory efficacy. Eur J Med Chem. 2025 Jul 5;297:117932. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RIPK2-IN-8 Related Classifications
HY-175026 Related Classifications
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