RIPK1-IN-17
Based on 1 Customer Validation
RIPK1-IN-17 is an orally active, selective RIPK1 inhibitor (Kd = 17 nM) and shows no significant inhibition to RIPK3. RIPK1-IN-17 specifically inhibits necroptosis rather than apoptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation. RIPK1-IN-17 protects mice from hypothermia and death. RIPK1-IN-17 can be used for the study of necroptosis-related diseases such as inflammatory response syndrome (SIRS).
For research use only. We do not sell to patients.
- Purity: 97.09%
- CAS No.: 3033385-59-7
- Formula: C26H19F4N3O3S
- Molecular Weight:529.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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RIPK1 17 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | CC50 |
>10 μM
Compound: 10
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Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 16 to 24 hrs by CellTiter-Glo Luminescent cell viability assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 16 to 24 hrs by CellTiter-Glo Luminescent cell viability assay
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[PMID: 37917221] |
| HT-29 | EC50 |
0.017 μM
Compound: 10
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Anti-necroptic activity against human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis pretreated with compound followed by TSZ stimulation for 16 to 18 hrs by CellTiter-Glo Luminescent cell viability as
Anti-necroptic activity against human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis pretreated with compound followed by TSZ stimulation for 16 to 18 hrs by CellTiter-Glo Luminescent cell viability as
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[PMID: 37917221] |
RIPK1-IN-17 (Compound 10), which is formed by directly connecting two moieties using a biphenyl-type linker, exhibits significantly enhanced activity against necroptosis in HT-29 cells (EC50 = 0.017 μM) and demonstrates no significant cytotoxicity at the tested concentrations (CC50 > 10 μM)[1].
RIPK1-IN-17 displays significantly enhanced RIPK1 inhibitory activity (Kd = 17 nM) and demonstrates no apparent activity toward RIPK3 at a concentration of 5000 nM[1].
RIPK1-IN-17 (0.015-0.5 μM) provides dose-dependent protection against TNF-α, Cycloheximide (HY-12320), and Z-VAD-FMK (HY-16658B) (TCZ)-induced necroptosis in HT-29 cells[1].
RIPK1-IN-17 (0.015-0.5 μM) exhibits protective effects against necroptosis induced by Z-VAD-FMK (HY-16658B) at a lower concentration in murine L929 cells[1].
RIPK1-IN-17 (0.1-1 μM) shows no protection against apoptosis induced by Cycloheximide or Smac mimetic (in HT-29 cells, even at concentrations up to 1 μM[1].
RIPK1-IN-17 (1 nM-1 μM, 0-6 h) at a concentration of 1 μM over 6 hours exhibits complete inhibition of RIPK1 phosphorylation, and at doses ranging from 1 to 1000 nM for 6 hours, it inhibits the phosphorylation of RIPK1, RIPK3, and MLKL in a dose-dependent manner 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:HT-29 cells
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Concentration:1 μM
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Incubation Time:0 h, 2 h, 4 h, 6 h
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Result:Completely inhibited RIPK1 phosphorylation and subsequently reduced downstream phosphorylation of RIPK3 and MLKL.
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Cell Line:HT-29 cells
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Concentration:1 nM, 10 nM, 100 nM, 1000 nM
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Incubation Time:6 h
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Result:Dose-dependently inhibited TSZ-induced phosphorylation of RIPK1, RIPK3, and MLKL.
RIPK1-IN-17 (100 mg/kg, 200 mg/kg, oral gavage, once) shows good tolerability and safety at doses far above its effective therapeutic dose in mice, without causing acute toxic reactions or organ damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 J mice aged 6-8 weeks injected mTNFα[1].
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Dosage:1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
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Administration:Oral gavage, once, two hours before injection of mTNFα
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Result:The survival rates of the SIRS mice were indicated as 70, 80, and 100%.
Significantly shielded the SIRS mice from hypothermia and death at the dosages of 1.25, 2.5, or 5 mg/kg.
Significantly reduced the levels of IL-6 and IL-1β in different tissues.
Dose-relatedly decreased the levels of IL-6 in the heart, liver, spleen, lung, kidney, intestine, and brain.
Led to a significant decrease in IL-1β levels in the spleen, lung, and intestine, which are the main organs affected in SIRS models.
Significantly decreased serum levels of IL-1β (three doses) and IL-6 (high dose).
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Animal Model:Male C57BL/6 J mice aged 6-8 weeks[1].
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Dosage:100 mg/kg, 200 mg/kg
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Administration:Oral gavage, once
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Result:No deaths or weight loss were observed after intragastric administration of the doses. Exhibited normal behavior throughout the 2-week study period.
Hematoxylin-Eosin (HE) staining assays revealed no significant pathological damage to the six vital organs (heart, liver, spleen, lung, kidney, and brain).
Chemical Information
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CAS No. 3033385-59-7
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Appearance Solid
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Molecular Weight 529.51
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Formula C26H19F4N3O3S
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Color White to off-white
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SMILES
O=C(CC1=CC=CC(OC(F)(F)F)=C1)NC2=C(C=CC(C3=CC=C4N=C(SC4=C3)NC(C5CC5)=O)=C2)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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