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

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

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Customer Review

Based on 1 publication(s) in Google Scholar

ASK1-IN-2 Related Antibodies

Top Publications Citing Use of Products

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MAP3K7/TAK1 MAP3K8 ASK2 MAP3K5/ASK1

  • 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].

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

ASK1-IN-2 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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; 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 2.7444 mL 13.7219 mL 27.4439 mL
5 mM 0.5489 mL 2.7444 mL 5.4888 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.7444 mL 13.7219 mL 27.4439 mL 68.6097 mL
5 mM 0.5489 mL 2.7444 mL 5.4888 mL 13.7219 mL
10 mM 0.2744 mL 1.3722 mL 2.7444 mL 6.8610 mL
15 mM 0.1830 mL 0.9148 mL 1.8296 mL 4.5740 mL
20 mM 0.1372 mL 0.6861 mL 1.3722 mL 3.4305 mL
25 mM 0.1098 mL 0.5489 mL 1.0978 mL 2.7444 mL
30 mM 0.0915 mL 0.4574 mL 0.9148 mL 2.2870 mL
40 mM 0.0686 mL 0.3430 mL 0.6861 mL 1.7152 mL
50 mM 0.0549 mL 0.2744 mL 0.5489 mL 1.3722 mL
60 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1435 mL
80 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8576 mL
100 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
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ASK1-IN-2 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:

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

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