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

ASK1-IN-2 

Cat. No.: HY-131969 Purity: 98.49%
COA 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
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 580 In-stock
25 mg USD 1100 In-stock
50 mg USD 1700 In-stock
100 mg USD 2500 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All MAP3K Isoform Specific Products:

View All Isoforms
MAP3K5/ASK1 MAP3K7/TAK1 MAP3K8 ASK2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

Appearance

Solid

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 available by MCE.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

ASK1-IN-22541792-70-3MAP3KApoptosisMAP kinase kinase kinase, MEKK, MAPKKKapoptosissignal-regulatingASK1ulcerativecolitisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ASK1-IN-2
Cat. No.:
HY-131969
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email address *

Phone number

 

Department *

Organization name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.