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AKR1C3-IN-1 

Cat. No.: HY-107379 Purity: 98.74%
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 79 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 72 In-stock
Estimated Time of Arrival: December 31
50 mg USD 216 In-stock
Estimated Time of Arrival: December 31
100 mg USD 348 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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

Molecular Weight

317.36

Formula

C₁₆H₁₅NO₄S

CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (315.10 mM)

*"≥" 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
10 mM 0.3151 mL 1.5755 mL 3.1510 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: ≥ 2.5 mg/mL (7.88 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

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

AKR1C3-IN-1OthersInhibitorinhibitorinhibit

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Product Name:
AKR1C3-IN-1
Cat. No.:
HY-107379
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