2. Apoptosis MAPK/ERK Pathway Metabolic Enzyme/Protease Immunology/Inflammation
  3. RIP kinase Necroptosis Mixed Lineage Kinase Lactate Dehydrogenase Interleukin Related
  4. 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.

RIPK1-IN-38

RIPK1-IN-38 Chemical Structure

CAS No. : 3092834-30-2

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RIPK1-IN-38 Related Antibodies

Top Publications Citing Use of Products

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RIPK1 RIPK2 RIPK3

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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[1].

IC50 & Target[1]

RIPK1

27 nM (IC50)

IL-6

 

In Vitro

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.

RIPK1-IN-38 Related Antibodies

Western Blot Analysis[1]

Cell Line: TSZ-treated HT-29 cells
Concentration: 0.3,3,30,300 nM
Incubation Time: 2,4,6 h
Result: Inhibited the phosphorylation of RIPK1 and its downstream signal proteins RIPK3 and MLKL in a dose- and time-dependent manner.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 CL AUC0-t V F
Mice[1] 10 mg/kg i.v. 4364.87 μg/L 0.08 h 8.63 h 0.21 L/h/kg 39926.93 μg/L·h 2.61 L/kg /
Mice[1] 10 mg/kg p.o. 2971.36 μg/L 3.33 h 10.35 h 0.19 L/h/kg 42886.31 μg/L·h 2.71 L/kg 107.41 %
In Vivo

RIPK1-IN-38 (2.5-10 mg/kg, oral administration, single dose) significantly attenuates inflammation and improves survival rate in the TNFα-induced systemic inflammatory response syndrome (SIRS) mouse model[1].
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.

Animal Model: C57BL/6 mice (TNF-Induced SIRS model)[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration: Oral
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.
Animal Model: NOG mice transplanted with human PBMCs (humanized acute GVHD model)[1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: Oral
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.
Molecular Weight

499.56

Formula

C27H22FN5O2S
CAS No.
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
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-38 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-383092834-30-2RIP kinaseNecroptosisMixed Lineage KinaseLactate DehydrogenaseInterleukin RelatedReceptor-interacting protein kinasesRIPKMLKsLDHILsystemic inflammatory response syndromeRIPK1 inhibitornecroptosisSIRSGVHDInhibitorinhibitorinhibit

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