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AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC50 of 13 nM.

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

AKR1C3-IN-1 Chemical Structure

AKR1C3-IN-1 Chemical Structure

CAS No. : 327092-81-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 79 In-stock
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Solid
5 mg USD 46 In-stock
10 mg USD 72 In-stock
50 mg USD 216 In-stock
100 mg USD 348 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

AKR1C3-IN-1 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC50 of 13 nM.

IC50 & Target

IC50: 13 nM (AKR1C3)[1]
In Vitro

AKR1C3-IN-1 shows less potent activities with 20.3±3.8 μM against AKR1C1 and >30 μM against AKR1C2 and AKR1C4. AKR1C3-IN-1 inhibits AKR1C3 activity (inhibiting PR-104H formation) with an IC50 of 0.027±0.002 μM[1].

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

AKR1C3-IN-1 Related Antibodies
Molecular Weight

317.36

Formula

C16H15NO4S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(N1CC2=CC=CC=C2CC1)(C3=CC(C(O)=O)=CC=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (315.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1510 mL 15.7550 mL 31.5100 mL
5 mM 0.6302 mL 3.1510 mL 6.3020 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
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: ≥ 2.5 mg/mL (7.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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
Kinase Assay
[1]

A competitive fluorescence assay is used to measure AKR1C enzyme activity, where a nonfluorescent ketone probe (probe 5) selective for the AKR1C enzyme isoforms is reduced to a fluorescent alcohol in the presence of AKR1C enzyme and NADPH. Briefly, purified protein (2 μg/mL AKR1C1, 1 μg/mL AKR1C2, 2 μg/mL AKR1C3, and 5 μg/mL AKR1C4) are incubated with 40 μM probe 5, AKR1C3-IN-1, and 50 μM NADPH in an assay buffer of 10 mM MOPS (pH=7.2), 130 mM NaCl, 1 mM DTT, and 0.01% Triton-X-100 for 1 h at 37°C. The reaction is stopped by addition of 35 mM NaOH, and fluorescence is read in a SpectraMax M2 microplate reader at excitation/emission wavelengths of 420/510 nM. The compounds and known AKR1C3 inhibitors (flufenamic acid, indomethacin, naproxen, meclofenamic acid, S(+)-ibuprofen and flurbiprofen) are tested at multiple concentrations between 0.1 nM and 100 μM in 2% DMSO to generate AKR1C enzyme inhibition data. Compound IC50 values are calculated by fitting the inhibition data to a four-parameter logistic sigmoidal dose-response curve using Prism 5.02.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1510 mL 15.7550 mL 31.5100 mL 78.7749 mL
5 mM 0.6302 mL 3.1510 mL 6.3020 mL 15.7550 mL
10 mM 0.3151 mL 1.5755 mL 3.1510 mL 7.8775 mL
15 mM 0.2101 mL 1.0503 mL 2.1007 mL 5.2517 mL
20 mM 0.1575 mL 0.7877 mL 1.5755 mL 3.9387 mL
25 mM 0.1260 mL 0.6302 mL 1.2604 mL 3.1510 mL
30 mM 0.1050 mL 0.5252 mL 1.0503 mL 2.6258 mL
40 mM 0.0788 mL 0.3939 mL 0.7877 mL 1.9694 mL
50 mM 0.0630 mL 0.3151 mL 0.6302 mL 1.5755 mL
60 mM 0.0525 mL 0.2626 mL 0.5252 mL 1.3129 mL
80 mM 0.0394 mL 0.1969 mL 0.3939 mL 0.9847 mL
100 mM 0.0315 mL 0.1575 mL 0.3151 mL 0.7877 mL
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AKR1C3-IN-1 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:

AKR1C3-IN-1327092-81-9OthersInhibitorinhibitorinhibit

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