[CAS NO. 1354825-58-3]  WEHI-345

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PRODUCTS SPECIFICATIONS [1354825-58-3]

Catalog
HY-18937
Brand
MCE
CAS
1354825-58-3

DESCRIPTION [1354825-58-3]

Overview

MDLMFCD29472247
Molecular Weight401.46
Molecular FormulaC22H23N7O
SMILESO=C(C1=CC=NC=C1)NCC(C)(N2N=C(C3=CC=C(C)C=C3)C4=C(N)N=CN=C42)C

For research use only. We do not sell to patients.


Summary

WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC 50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation [1] .


IC50 & Target

IC 50 : 0.13 μM (RIPK2 kinase) [1]


In Vitro

WEHI-345 (500 nM; Raw 267.4 cells) is able to inhibit MDP-induced autophosphorylation activity of RIPK2 in cells [1] .
WEHI-345 (500 nM; 0 hour, 2 hours, 4 hours, 8 hours; BMDMs or THP-1 cells) potently blocks MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in bone marrow-derived macrophages (BMDMs). In THP-1 cells, WEHI-345 reduces mRNA levels of NF-kB targets such as TNF, IL-8, IL-1b and A20 [1] .

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

Western Blot Analysis [1]

Cell Line: Raw 267.4 cells
Concentration: 500 nM
Incubation Time:
Result: Inhibited MDP-induced autophosphorylation activity of RIPK2 in cells.

RT-PCR [1]

Cell Line: BMDMs or THP-1 cells
Concentration: 500 nM
Incubation Time: 0 hour, 2 hours, 4 hours, 8 hours
Result: Blocked MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in BMDMs. And reduced mRNA levels of NF-kB targets in THP-1 cells.

In Vivo

WEHI-345 (20 mg/kg; intraperitoneal injection; twice daily; for 6 days; C57BL/6 male mice) treatment reduces disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improves body weight and reduces cytokine and chemokine levels, indicating an overall improvement of the condition in experimental autoimmune encephalomyelitis (EAE)-induced wild-type C57Bl/6 mice [1] .

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

Animal Model: C57BL/6 male mice (8-week-old) [1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; twice daily; for 6 days
Result: Reduced disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improved body weight and reduced cytokine and chemokine levels.

Appearance

Solid


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 : 25 mg/mL ( 62.27 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4909 mL 12.4545 mL 24.9091 mL
5 mM 0.4982 mL 2.4909 mL 4.9818 mL
10 mM 0.2491 mL 1.2455 mL 2.4909 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

* All of the co-solvents are available by MCE.