2. Apoptosis MAPK/ERK Pathway
  3. RIP kinase Necroptosis Mixed Lineage Kinase
  4. RIPK1-IN-17

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).

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RIPK1-IN-17

RIPK1-IN-17 Chemical Structure

CAS No. : 3033385-59-7

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RIPK1-IN-17 Related Antibodies

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Description

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)[1].

In Vitro

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.

RIPK1-IN-17 Related Antibodies

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 1 μM
Incubation Time: 0 h, 2 h, 4 h, 6 h
Result: Completely inhibited RIPK1 phosphorylation and subsequently reduced downstream phosphorylation of RIPK3 and MLKL.

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 6 h
Result: Dose-dependently inhibited TSZ-induced phosphorylation of RIPK1, RIPK3, and MLKL.
In Vivo

RIPK1-IN-17 (1.25-5 mg/kg, oral gavage, once) effectively protects mice from TNFα-induced SIRS, as demonstrated by preventing hypothermia, improving survival, and reducing the levels of key proinflammatory cytokines (IL-6 and IL-1β)[1].
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.

Animal Model: Male C57BL/6 J mice aged 6-8 weeks injected mTNFα[1].
Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
Administration: Oral gavage, once, two hours before injection of mTNFα.
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).
Animal Model: Male C57BL/6 J mice aged 6-8 weeks[1].
Dosage: 100 mg/kg, 200 mg/kg
Administration: Oral gavage, once
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).
Molecular Weight

529.51

Formula

C26H19F4N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
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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RIPK1-IN-17 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-173033385-59-7RIP kinaseNecroptosisMixed Lineage KinaseReceptor-interacting protein kinasesRIPKMLKsSystemic Inflammatory Response SyndromeSIRSReceptor-Interacting Protein Kinase 1RIPK1RIPK3MLKLInhibitorinhibitorinhibit

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