2. Apoptosis MAPK/ERK Pathway
  3. RIP kinase Mixed Lineage Kinase Apoptosis
  4. WJH-C19

WJH-C19 is an orally active RIPK1 inhibitor with an IC50 of 5.7 nM. WJH-C19 inhibits the RIPK1/RIPK3/MLKL signaling axis, blocks RIPK1 phosphorylation, suppresses the phosphorylation of downstream RIPK3 and MLKL, disrupts necrosome formation, and exhibits protective effects against necroptosis (Apoptosis) in multiple cell lines. WJH-C19 ameliorates symptoms of inflammatory bowel disease in a mouse colitis model by regulating the necroptosis pathway. WJH-C19 alleviates inflammation and bone destruction in a mouse model of rheumatoid arthritis. WJH-C19 is applicable to research related to inflammatory bowel disease and rheumatoid arthritis.

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WJH-C19

WJH-C19 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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WJH-C19 Related Antibodies

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Description

WJH-C19 is an orally active RIPK1 inhibitor with an IC50 of 5.7 nM. WJH-C19 inhibits the RIPK1/RIPK3/MLKL signaling axis, blocks RIPK1 phosphorylation, suppresses the phosphorylation of downstream RIPK3 and MLKL, disrupts necrosome formation, and exhibits protective effects against necroptosis (Apoptosis) in multiple cell lines. WJH-C19 ameliorates symptoms of inflammatory bowel disease in a mouse colitis model by regulating the necroptosis pathway. WJH-C19 alleviates inflammation and bone destruction in a mouse model of rheumatoid arthritis. WJH-C19 is applicable to research related to inflammatory bowel disease and rheumatoid arthritis[1].

IC50 & Target[1]

RIPK1

5.7 nM (IC50)

RIPK3

 

In Vitro

WJH-C19 (Compound 10e12) (25 h) exerts potent, concentration-dependent protective effects against necroptosis in multiple cell lines, with EC50 values of 0.28 nM in L929 cells, 4.0 nM in HT22 cells, 1.6 nM in HT29 cells, and 2.0 nM in U937 cells; in addition, this compound reduces necroptotic L929 cells in a dose-dependent manner[1].
WJH-C19 potently inhibits the kinase activity of RIPK1, with an IC50 value of 5.7 nM[1].
WJH-C19 (0.5-50 nM) concentration-dependently inhibits the TNFα/z-VAD-FMK (HY-16658BG) (TZ)-induced phosphorylation of RIPK1, RIPK3 and MLKL in L929 cells, as well as the mTNFα/Smac mimetic/z-VAD-FMK (TSZ)-induced phosphorylation in HT29 cells, thereby blocking necrosome formation and the downstream necroptotic signaling pathway[1].

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

WJH-C19 Related Antibodies
Parmacokinetics
Species Dose Route CL Vss T1/2 AUC0-t Tmax Cmax AUC0-∞ MRT0-∞ Bioavailability
Mice[1] 1 mg/kg i.v. 0.11 L/h/kg 0.93 L/kg 5.89 h 8914.61 ng·h/mL 0.083 h 10495 ng/mL 9205.63 ng·h/mL 4.77 h /
Mice[1] 10 mg/kg p.o. / / 6.54 h 10906.26 ng·h/mL 6 h 1051 ng/mL 11864.51 ng·h/mL / 12.89 %
In Vivo

WJH-C19 (1.25-2.5 mg/kg; p.o.; daily; 7 days) potently ameliorates dextran sulfate sodium (DSS, HY-116282C)-induced colitis in female C57BL/6 mice, leading to 47.5% body weight recovery, 42.9% reduction in disease activity index (DAI), and robust inhibition of the RIPK1/RIPK3/MLKL signaling axis[1].
WJH-C19 (10-20 mg/kg; p.o.; daily; 14 days) potently ameliorates complete Freund's adjuvant (CFA, HY-153808)-induced rheumatoid arthritis in female C57BL/6 mice, reduces paw swelling, joint inflammation and bone destruction, and inhibits the RIPK1/RIPK3/MLKL signaling axis[1].

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

Animal Model: C57BL/6 (female, 10-12 weeks old, ~28 g, DSS-induced colitis)[1]
Dosage: 2.5 mg/kg; 1.25 mg/kg
Administration: p.o.; daily; 7 days
Result: Achieved 47.5% body weight recovery, 42.9% disease activity index (DAI) reduction, and 60.5% colon length recovery at 2.5 mg/kg.
Achieved 33.2% body weight recovery, 32.1% DAI reduction, and 35.1% colon length recovery at 1.25 mg/kg.
Reduced proinflammatory cytokine levels (IL-1β, IL-6, TNFα) and increased anti-inflammatory cytokine IL-10 levels in colon tissue at both doses.
Inhibited phosphorylation of RIPK1, RIPK3, and MLKL in colonic proteins at both doses, with the high dose showing the most robust inhibition.
Reduced mucosal damage, maintained intact glandular architecture, and restored zonula occludens-1 (ZO-1) and Occludin expression at both doses, with the high-dose group exhibiting near-normal morphology.
Animal Model: C57BL/6 (female, 8 weeks old, CFA-induced rheumatoid arthritis)[1]
Dosage: 20 mg/kg; 10 mg/kg
Administration: p.o.; daily; 14 days
Result: Reduced paw swelling percentage, ankle joint temperature, and arthritis index scores in a dose-dependent manner at both doses, with efficacy comparable or superior to celecoxib.
Reduced osteophyte formation and reversed bone destructive changes, including improvements in bone mineral density (BMD), cortical BMD, trabecular number (Tb.N), connectivity density (Conn.D), bone volume (BV), cortical volume (CV), trabecular separation (Tb.Sp), pore number (Po.N), cortical area (Ct.Ar), and cortical thickness (Ct.Th) at both doses, with the high dose showing the most pronounced improvement.
Reduced inflammatory cell infiltration, synovial hyperplasia, and cartilage erosion at both doses, with the high-dose group achieving histological scores approaching normal levels.
Reduced the M1/M2 macrophage ratio in spleens in a dose-dependent manner at both doses, shifting toward the anti-inflammatory M2 phenotype.
Suppressed expression of phosphorylated RIPK1, RIPK3, and MLKL in ankle joints at both doses, with the high dose showing the strongest inhibition.
Molecular Weight

516.01

Formula

C27H22ClN5O2S
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C2C=CC(C3=CC=C4N=C(NC(C5CC5)=O)SC4=C3)=CN21)N[C@H](C6=CC=C(Cl)C=C6)C
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
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (96.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9379 mL 9.6897 mL 19.3795 mL
5 mM 0.3876 mL 1.9379 mL 3.8759 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9379 mL 9.6897 mL 19.3795 mL 48.4487 mL
5 mM 0.3876 mL 1.9379 mL 3.8759 mL 9.6897 mL
10 mM 0.1938 mL 0.9690 mL 1.9379 mL 4.8449 mL
15 mM 0.1292 mL 0.6460 mL 1.2920 mL 3.2299 mL
20 mM 0.0969 mL 0.4845 mL 0.9690 mL 2.4224 mL
25 mM 0.0775 mL 0.3876 mL 0.7752 mL 1.9379 mL
30 mM 0.0646 mL 0.3230 mL 0.6460 mL 1.6150 mL
40 mM 0.0484 mL 0.2422 mL 0.4845 mL 1.2112 mL
50 mM 0.0388 mL 0.1938 mL 0.3876 mL 0.9690 mL
60 mM 0.0323 mL 0.1615 mL 0.3230 mL 0.8075 mL
80 mM 0.0242 mL 0.1211 mL 0.2422 mL 0.6056 mL
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WJH-C19 Related Classifications

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:

WJH-C19RIP kinaseMixed Lineage KinaseApoptosisReceptor-interacting protein kinasesRIPKMLKsRIPK1 inhibitorL929 cellsHT22 cellsHT29cellsU937 cellsinflammatory bowel diseaserheumatoid arthritisC57BL/6 mice
Inhibitorinhibitorinhibit

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