2. Apoptosis MAPK/ERK Pathway
  3. RIP kinase Mixed Lineage Kinase Necroptosis
  4. RIPK1-IN-34

RIPK1-IN-34 is a selective, brain-penetrant RIPK1 inhibitor (IC50 = 126.70 nM) with almost no inhibitory effect on RIPK3 (IC50 ＞ 10, 000 nM). RIPK1-IN-34 offers substantial neuroprotection by inhibiting the phosphorylation of RIPK1, RIPK3, and mixed lineage kinase domain-like pseudokinase (MLKL) within the necroptosis pathway. RIPK1-IN-34 shows the neuroprotective effect in a rat middle cerebral artery occlusion (MCAO) model. RIPK1-IN-34 can be used for the study of anti-acute ischemic stroke (AIS).

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RIPK1-IN-34

RIPK1-IN-34 Chemical Structure

CAS No. : 3065634-19-4

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RIPK1-IN-34 Related Antibodies

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Description

RIPK1-IN-34 is a selective, brain-penetrant RIPK1 inhibitor (IC50 = 126.70 nM) with almost no inhibitory effect on RIPK3 (IC50 ＞ 10, 000 nM). RIPK1-IN-34 offers substantial neuroprotection by inhibiting the phosphorylation of RIPK1, RIPK3, and mixed lineage kinase domain-like pseudokinase (MLKL) within the necroptosis pathway. RIPK1-IN-34 shows the neuroprotective effect in a rat middle cerebral artery occlusion (MCAO) model. RIPK1-IN-34 can be used for the study of anti-acute ischemic stroke (AIS)[1].

IC50 & Target

RIPK1

126.7 nM (IC50)

In Vitro

RIPK1-IN-34 (Compound 9b) significantly reduces TNF-α (T), a Smac-mimetic, SM-164 (HY-15989) (S), and Z-VAD-FMK (HY-16658B) (Z)-induced apoptosis in HT-29 (EC50 = 71.61 nM) and HT-22 (EC50 = 38.45 nM) cells[1].
RIPK1-IN-34 (0.78-400 nM, 24 h) effectively counters the TSZ-induced changes and approximates the untreated control group's condition in HT-29, U937, L929 and HT-22 cells[1].
RIPK1-IN-34 (1, 10, 100 nM, 4.5 h) is effective in protecting the cells from necroptosis in L929 cells[1].
Compound RIPK1-IN-34 (0-1000 nM, 4.5 h) dose-dependently inhibits the phosphorylation of RIPK1, RIPK3, and MLKL in L929 cells[1].

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

RIPK1-IN-34 Related Antibodies

Apoptosis Analysis[1]

Cell Line: L929 cells
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: After pre-incubation with the compound for 30 minutes, cells were treated with TSZ for 4 hours
Result: Effectively protected the cells from necroptosis in L929 cells.

Western Blot Analysis[1]

Cell Line: L929 cells
Concentration: 0 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: After pre-incubation with the compound for 30 minutes, cells were treated with TSZ for 4 hours
Result: Decreased the intensities of p-RIPK1 and p-RIPK3 bands in response to increasing concentrations.
Curtailed the enhancement of MLKL phosphorylation.
Parmacokinetics
Species Dose Route Cmax T1/2 AUC0-inf CL Tmax F
Rat 0.5 mg/kg i.v. 462.6 ng/mL 6.4 h 2065.1 ng·h/mL 4 mL/min/kg / /
Rat 20 mg/kg p.o. 1221.2 ng/mL 8 h 12316.1 ng·h/mL 27.1 mL/min/kg 2 h 14.9 %
In Vivo

RIPK1-IN-34 (Compound 9b) (0.5-4.5 mg/kg, i.v., twice) dose-dependently improves neurological function, reduces cerebral infarction volume, and inhibits inflammation and oxidative stress in SD rats, demonstrating its significant neuroprotective effect[1].
RIPK1-IN-34 (78.4-160 mg/kg, i.p., two intraperitoneal injections, one hour apart) does not cause acute toxicity at the dose tested in C57BL/6 mice, and its LD50 exceeds 160 mg/kg, indicating that it has a high safety profile[1].

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

Animal Model: SPF grade male SD rats (180-200 g) were used to construct a middle cerebral occlusion model[1].
Dosage: 0.5 mg/kg, 1.5 mg/kg, 4.5 mg/kg
Administration: I.v., administered intravenously once 0.5 hours before modeling, and again after reperfusion, for a total of two administrations
Result: Significantly improved neurological outcomes 24 h post-operation, with reductions in scores exhibiting a dose-dependent trend: low dose (5.20), medium dose (5.09), and high dose (3.82).
Significantly reduced infarct volumes across all treatment groups in a dose-responsive manner: low dose (20.60), medium dose (18.32), and high dose (16.51).
Diminished MDA, TNF-α, and IL-1β levels while slightly increasing SOD levels.
Animal Model: SPF grade male C57BL/6 mice (aged 6-8 weeks, weighing 18-22 g)[1].
Dosage: 160 mg/kg, 112 mg/kg, 78.4 mg/kg
Administration: I.p., two intraperitoneal injections, one hour apart
Result: No abnormal behaviors or deaths were observed, and the body weight of mice in all groups steadily increased over 7 days with no significant differences.
Molecular Weight

491.54

Formula

C28H25N7O2
CAS No.
SMILES

O=C(C1=C2C=C(C3=CC4=NC(NC(C5CC5)=O)=NN4C=C3)C=CC2=NC(C)=N1)N[C@H](C6=CC=CC=C6)C
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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-34 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-343065634-19-4RIP kinaseMixed Lineage KinaseNecroptosisReceptor-interacting protein kinasesRIPKMLKsRIPK1 inhibitorQuinazoline coreNeuroprotectantsAnti acute ischemic strokeInhibitorinhibitorinhibit

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