2. Apoptosis
  3. RIP kinase Necroptosis
  4. RIPK1-IN-41

RIPK1-IN-41 is an orally active RIPK1 inhibitor with an IC50 of 92 nM and a KD of 106.8 nM. RIPK1-IN-41 reduces the phosphorylation level of RIPK1, inhibits necrosome formation, blocks the activation of RIPK3 and MLKL, maintains mitochondrial and lysosomal functions, preserves cell membrane integrity, and suppresses necroptosis. RIPK1-IN-41 alleviates hypothermia and multi-organ damage in a mouse model of systemic inflammatory response syndrome induced by mTNF-α. RIPK1-IN-41 is applicable to research related to systemic inflammatory response syndrome.

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RIPK1-IN-41

RIPK1-IN-41 Chemical Structure

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RIPK1-IN-41 Related Antibodies

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Description

RIPK1-IN-41 is an orally active RIPK1 inhibitor with an IC50 of 92 nM and a KD of 106.8 nM. RIPK1-IN-41 reduces the phosphorylation level of RIPK1, inhibits necrosome formation, blocks the activation of RIPK3 and MLKL, maintains mitochondrial and lysosomal functions, preserves cell membrane integrity, and suppresses necroptosis. RIPK1-IN-41 alleviates hypothermia and multi-organ damage in a mouse model of systemic inflammatory response syndrome induced by mTNF-α. RIPK1-IN-41 is applicable to research related to systemic inflammatory response syndrome[1].

IC50 & Target[1]

RIPK1

92 nM (IC50)

RIPK1

106.8 nM (Kd)

In Vitro

RIPK1-IN-41 (Compound 5e) potently inhibits purified RIPK1 kinase with an IC50 of 92 nM[1].
RIPK1-IN-41 directly binds to purified RIPK1 kinase with a K0 of 106.8 nM[1].
RIPK1-IN-41 strongly inhibits purified RIPK1, moderately inhibits purified RIPK3, and retains multi-targeted activity against several other kinases including VEGFR2, PDGFRβ, and FLT3[1].
RIPK1-IN-41 dose-dependently inhibits mTNF-α/Z-VAD-FMK-induced necroptosis in L929 cells with an EC50 of 0.45 μM[1].
RIPK1-IN-41 (0.05-1 μM) can maintain, in a dose-dependent manner, the mitochondrial integrity and lysosomal integrity of mTNF-α/Z-VAD-FMK-induced necrotic apoptosis in L929 cells, inhibit the formation of RIPK1-RIPK3 necrosomes, upregulate pMLKL activation and lysosomal translocation[1].
RIPK1-IN-41 (0.5 μM; 3-6 h) time-dependently inhibits the phosphorylation of RIPK1, RIPK3, and MLKL in mTNF-α/Z-VAD-FMK-induced necroptotic L929 cells[1].
RIPK1-IN-41 (0.05-1 μM,1 h pretreatment; 6 h necroptosis induction) reduced phosphorylation of RIPK1, RIPK3, and MLKL[1].

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

RIPK1-IN-41 Related Antibodies

Western Blot Analysis[1]

Cell Line: mouse L929 fibroblast cells (induced with mTNF-α/Z-VAD-FMK)
Concentration: 0.05, 0.5, 1 μM
Incubation Time: 1 h pretreatment; 6 h necroptosis induction
Result: Dose-dependently reduced phosphorylation of RIPK1, RIPK3, and MLKL.

Western Blot Analysis[1]

Cell Line: mouse L929 fibroblast cells (induced with mTNF-α/Z-VAD-FMK)
Concentration: 0.5 μM
Incubation Time: 3 h, 6 h
Result: Time-dependently reduced phosphorylation of RIPK1, RIPK3, and MLKL.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-t AUC0-∞
Rat[1] 10 mg/kg p.o. 39.2 ng/mL 0.89 h 2.19 h 183.3 ng·h/mL 189.6 ng·h/mL
In Vivo

RIPK1-IN-41 (Compound 5e) (30-50 mg/kg; p.o.; single dose; 1 hour prior to mTNF-α injection) dose-dependently improves survival, alleviates hypothermia, reduces inflammatory cytokine release, and protects against multi-organ damage in mTNF-α-induced SIRS in C57BL/6 mice[1].

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

Animal Model: C57BL/6[1]
Dosage: 30 mg/kg; 50 mg/kg
Administration: p.o.; single dose; 1 hour prior to mTNF-α injection
Result: Achieved a 50% 48-hour survival rate.
Decreased serum IL-6 levels to 627.0 pg/mL from the model group's 1034.2 pg/mL.
Alleviated hypothermia relative to the model group.
Achieved an 83% 48-hour survival rate.
Reached a body temperature nadir of 32.5 °C at 10 hours and recovered to normal levels by 28 hours.
Decreased serum IL-6 levels to 433.9 pg/mL
Significantly reduced damage to heart, liver, spleen, lung, and kidney, with tissue morphology near that of the normal control group.
Molecular Weight

471.59

Formula

C28H33N5O2
SMILES

CCN(CCNC(C1=C(NC(/C=C2C(NC3=CC=C(C=C3\2)C4=CC(N)=CC=C4)=O)=C1C)C)=O)CC
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-41 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-41RIP kinaseNecroptosisReceptor-interacting protein kinasesRIPKRIPK1C57BL/6 micesystemic inflammatory response syndromeL929 cellsmTNF-αVEGFR2necroptosisMLKLRIPK3PDGFRβInhibitorinhibitorinhibit

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