2. Apoptosis NF-κB MAPK/ERK Pathway Immunology/Inflammation
  3. RIP kinase NF-κB p38 MAPK Interleukin Related
  4. 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.

For research use only. We do not sell to patients.

RIPK2-IN-8 Chemical Structure

RIPK2-IN-8 Chemical Structure

CAS No. : 3036254-29-9

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RIPK2-IN-8 Related Antibodies

Top Publications Citing Use of Products

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RIPK1 RIPK2 RIPK3

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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Description

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[1].

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.

RIPK2-IN-8 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 cells were stimulated with L18-MDP
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
Incubation Time: 0.5 h, 6 h
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.
In Vivo

RIPK2-IN-8 (Compound HY3) (7.5-30 mg/kg, p.o., once) inhibits RIPK2 kinase activity, thereby blocking the activation of downstream inflammatory signals, and further affecting the synthesis and release of the cytokine IL-6 in MDP-induced peritonitis mice model[1].
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.

Animal Model: MDP-induced (100 μg, i.p.) peritonitis mice (Female C57BL/6 at 8 weeks of age) model[1]
Dosage: 7.5 mg/kg, 15 mg/kg, 30 mg/kg
Administration: p.o., once
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).
Animal Model: APAP-induced (500 mg/kg, i.p.) ALI mice (Female C57BL/6 at 8 weeks of age) model[1]
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: p.o., once
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.
Molecular Weight

453.56

Formula

C22H20FN5OS2
CAS No.
SMILES

CCC(NC1CCC(C2=CC(N=CN=C3NC4=CC(N=CS5)=C5C=C4F)=C3S2)=CC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RIPK2-IN-8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RIPK2-IN-83036254-29-9RIP kinaseNF-κBp38 MAPKInterleukin RelatedReceptor-interacting protein kinasesRIPKNuclear factor-κBNuclear factor-kappaBILInhibitorH9C2 cellsTHP-1 cellsALIMDP-induced peritonitisC57BL/6 miceAcute liver injuryinhibitorinhibit

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