RIPK1-IN-38
RIPK1-IN-38 is an orally active RIPK1 inhibitor with an IC50 value of 27 nM. RIPK1-IN-38 can inhibit the phosphorylation of RIPK1 and its downstream signaling molecules RIPK3 and MLKL. RIPK1-IN-38 exhibits anti-necroptotic activity. RIPK1-IN-38 has excellent anti-inflammatory efficacy in both the SIRS model and GVHD model. RIPK1-IN-38 can be used for the research of inflammatory and immune-related diseases.
For research use only. We do not sell to patients.
- CAS No.: 3092834-30-2
- Formula: C27H22FN5O2S
- Molecular Weight:499.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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RIPK1 27 nM (IC50) |
IL-6 |
RIPK1-IN-38 (Compound 2q) (0.01-10 nM; 24 h) can effectively block TSZ/TZ-induced necroptosis in U937, HT-29, and L929 cells, with EC50 values of 0.75 nM, 0.54 nM, and 0.13 nM, respectively[1].
RIPK1-IN-38 (1.25-5 μM; 72 h) exhibits no significant cytotoxicity in HepG2, LX-2, hPBMC, and H9c2 cells[1].
RIPK1-IN-38 (30 nM; 2 h) completely inhibits the phosphorylation of RIPK1, RIPK3, and MLKL in TSZ-treated HT-29 cells[1].
RIPK1-IN-38 (1.25-5 nM; 9 h) significantly inhibits lactate dehydrogenase (LDH) release from necrotic cells in HT-29 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TSZ-treated HT-29 cells
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Concentration:0.3,3,30,300 nM
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Incubation Time:2,4,6 h
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Result:Inhibited the phosphorylation of RIPK1 and its downstream signal proteins RIPK3 and MLKL in a dose- and time-dependent manner.
RIPK1-IN-38 (15-30 mg/kg, oral administration, Days 16-84) significantly alleviates symptoms and increases survival rate in the humanized acute graft-versus-host disease (GVHD) model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (TNF-Induced SIRS model)[1]
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Dosage:2.5 mg/kg, 5 mg/kg, 10 mg/kg
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Administration:Oral
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Result:Exhibited dose-dependent protection from hypothermia.
Improved mouse survival rate and reduce the level of pro-inflammatory cytokine IL-6 in serum.
Reduced inflammatory damage in the liver and kidneys.
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Animal Model:NOG mice transplanted with human PBMCs (humanized acute GVHD model)[1]
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Dosage:15 mg/kg, 30 mg/kg
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Administration:Oral
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Result:Improved the overall survival rate of mice.
Significantly relieved symptoms such as weak autonomic activity, piloerection, hunchback and weight loss.
Improved colon length and reduced hepatocyte necrosis and periportal lymphocyte infiltration.
Chemical Information
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CAS No. 3092834-30-2
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Molecular Weight 499.56
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Formula C27H22FN5O2S
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SMILES
O=C(N[C@@H](C)C1=CC=C(F)C=C1)C2=C3N(C=CC(C4=CC5=C(N=C(NC(C6CC6)=O)S5)C=C4)=C3)N=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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