country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-149254

Copy Link Print Information

PTP1B/AKR1B1-IN-1

PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC₅₀s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC₅₀ value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels.

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

Formula: C₂₂H₂₁NO₄S₂
Molecular Weight:427.54

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

PTP1B/AKR1B1-IN-1 Chemical Structure

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 0.06 μM (Protein tyrosine phosphatase 1B, PTP1B); 4.3 μM (Aldose reductase, AKR1B1); 9 μM (TC-PTP)^[1]

In Vitro

PTP1B/AKR1B1-IN-1 (compound 6f) tightly binds to PTP1B and AKR1B1 with K_i values of 4.6 μM, and 0.08 μM, respectively^[1].
PTP1B/AKR1B1-IN-1 (20 μM; 24 h) shows insignificant cytotoxicity in differentiated murine C2C12 cells^[1].
PTP1B/AKR1B1-IN-1 (20 μM; 24 h) enhances the increases of Akt phosphorylation in murine C2C12 cell line with insulin (10 μM; 15 min)^[1].
PTP1B/AKR1B1-IN-1 (2 μM; 24 h) results significant impairment of sorbitol accumulation in human lens epithelial line B3 (HLE) cells, induced with 75 mM d-glucose for 24 h^[1].

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

Western Blot Analysis^[1]

Cell Line:

Murine C2C12 cell
Concentration:

20 μM; with or without 10 μM insulin for 15 min
Incubation Time:

24 h
Result:

Increased Akt phosphorylation, and was enhanced by insulin.

Chemical Information

Molecular Weight 427.54
Formula C₂₂H₂₁NO₄S₂
SMILES

O=C(CN1C(/C(SC1=S)=C/C2=CC=CC(OCCCCC3=CC=CC=C3)=C2)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Maccari R, et al. Designed multiple ligands for the treatment of type 2 diabetes mellitus and its complications: Discovery of (5-arylidene-4-oxo-2-thioxothiazolidin-3-yl)alkanoic acids active as novel dual-targeted PTP1B/AKR1B1 inhibitors. Eur J Med Chem. 2023 Apr 5;252:115270. [Content Brief]

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote