2. Apoptosis
  3. RIP kinase
  4. RIPK1-IN-35

RIPK1-IN-35 is a selective and orally active RIPK1 inhibitor with an IC50 of 5.33 nM. RIPK1-IN-35 has a potent protective effect against necroptosis in both human and murine cells. RIPK1-IN-35 shows good therapeutic effects in both TNF-α-induced systemic inflammatory response syndrome and DSS (HY-116282C)-induced inflammatory bowel disease models. RIPK1-IN-35 can be used to the study of inflammatory diseases related to necroptosis.

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RIPK1-IN-35

RIPK1-IN-35 Chemical Structure

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RIPK1-IN-35 Related Antibodies

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Description

RIPK1-IN-35 is a selective and orally active RIPK1 inhibitor with an IC50 of 5.33 nM. RIPK1-IN-35 has a potent protective effect against necroptosis in both human and murine cells. RIPK1-IN-35 shows good therapeutic effects in both TNF-α-induced systemic inflammatory response syndrome and DSS (HY-116282C)-induced inflammatory bowel disease models. RIPK1-IN-35 can be used to the study of inflammatory diseases related to necroptosis[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

IC50 & Target[1]

RIPK1

5.33 nM (IC50)

In Vitro

RIPK1-IN-35 (Compound 44) (0.01 nM-10 μM, 18 h) protects cells from TSZ (TNF-α, BV6 (HY-16701) and Z-VAD-FMK (HY-16658B))-induced necroptosis of human and mouse cell lines with EC50s of 18.1 and 11.5 nM in U937 and L929 cells[1].
RIPK1-IN-35 (0-300 nM, 5 h) significantly and dose-dependently inhibits the phosphorylation of RIPK1 as well as its downstream proteins RIPK3 and MLKL in HT-29 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RIPK1-IN-35 Related Antibodies

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 0, 1, 3, 10, 30 and 100 nM
Incubation Time: Pretreated for 1 h and added TSZ for 4 h
Result: Significantly and dose-dependently inhibited the phosphorylation of RIPK1 as well as its downstream proteins RIPK3 and MLKL.
In Vivo

RIPK1-IN-35 (Compound 44) (3-10 mg/kg, p.o., single dose) effectively counteracts the lethal systemic inflammation induced by TNF-α and significantly increase the survival rate of mice[1].
RIPK1-IN-35 (10 mg/kg, p.o., once daily for 7 days) demonstrats a significant therapeutic effect in the DSS-induced inflammatory bowel disease (IBD) model, effectively alleviating the clinical symptoms and pathological damage of the disease[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The model of systemic inflammatory response syndrome (SIRS) induced by TNF-α established in C57BL/6J mice (female, 6-8 weeks old)[1]
Dosage: 3 and 10 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Dosage-dependently alleviated the sudden drop in body temperature caused by TNF-α.
Provided 80% and 100% survival protection rates respectively at doses of 3 mg/kg and 10 mg/kg.
Animal Model: DSS-induced IBD model established in C57BL/6J mice (female, 6-8 weeks old)[1]
Dosage: 10 mg/kg
Administration: Oral administration (p.o.), once daily for 7 days
Result: Significantly reduced the weight loss caused by DSS and improved the DAI score.
Significantly improved the phenomenon of colonic shortening.
Significantly alleviated severe epithelial damage, necrosis and infiltration of inflammatory cells, with a more intact mucosal structure and reduced inflammatory infiltration.
Molecular Weight

557.50

Formula

C26H18D3F3N6O5
SMILES

O=C(NC1=NNC(C2=CC=C3N(CCOC3=C2)C(CC4=C(C=CC(OC(F)F)=C4)F)=O)=C1)C5=NN(C([2H])([2H])[2H])C(C=C5)=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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RIPK1-IN-35 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:

RIPK1-IN-35RIP kinaseReceptor-interacting protein kinasesRIPKnecroptosisinflammatory diseasestructure-activity relationshippharmacokineticsin vivo efficacyTNF-α-induced SIRSDSS-induced IBDInhibitorinhibitorinhibit

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