1. MAPK/ERK Pathway
    Apoptosis
  2. MAP3K
    Apoptosis
  3. ASK1-IN-2

ASK1-IN-2 

Cat. No.: HY-131969 Purity: 98.49%
Handling Instructions

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.

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

ASK1-IN-2 Chemical Structure

ASK1-IN-2 Chemical Structure

CAS No. : 2541792-70-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis[1].

IC50 & Target[1]

ASK1

32.8 nM (IC50)

In Vitro

ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%[1].

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

In Vivo

ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice[1].
ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues[1].
ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats[1].
ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h•ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats[1].

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

Animal Model: Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water[1]
Dosage: 25 mg/kg
Administration: P.o. daily for 7 days
Result: Induced a significant recovery of body weight loss, with an increase of +11.2%.
Decreased the disease activity index (DAI) score about a 2 unit.
Significantly prevented colon shortening.
Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.
Animal Model: Male SD rats [1]
Dosage: 1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: I.v. and p.o. administration
Result: I.v.: CL=1.38 L/h/kg; T1/2=1.45 h.
P.o.: AUClast=4517 h•ng/mL; F=62.2%; T1/2=2.31 h.
Molecular Weight

364.38

Formula

C₁₉H₁₇FN₆O

CAS No.
SMILES

O=C(C(N1)=CC2=C1C=C(F)C=C2)NC3=NC(C4=NN=CN4C(C)C)=CC=C3

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 : 250 mg/mL (686.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7444 mL 13.7219 mL 27.4439 mL
5 mM 0.5489 mL 2.7444 mL 5.4888 mL
10 mM 0.2744 mL 1.3722 mL 2.7444 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ASK1-IN-2MAP3KApoptosisMAP kinase kinase kinase, MEKK, MAPKKKapoptosissignal-regulatingASK1ulcerativecolitisInhibitorinhibitorinhibit

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ASK1-IN-2
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