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Cat. No.: HY-183573

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PTPRO-IN-1

PTPRO-IN-1 is a selective, orally active PTPRO inhibitor with an IC₅₀ of 0.16 μM. PTPRO-IN-1 exhibits IC₅₀ values of 2.4 μM, 2.33 μM and 2.13 μM against PTPN22, PTP1B and PTPRT, respectively, and shows almost no inhibitory activity against STEP/SSH2. PTPRO-IN-1 inhibits the TLR4/NF-κB signaling pathway in macrophages, ameliorates colonic pathological conditions and suppresses the secretion of pro-inflammatory cytokines by T cells. PTPRO-IN-1 can be used for the research of inflammatory bowel disease.

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화학식: C₃₆H₂₄ClNO₆S
분자량:634.10

보관:

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

PTPRO-IN-1 Chemical Structure

사이즈

가격

재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

TLR4

IL-6

All Toll-like Receptor (TLR) Isoforms :

All NF-κB Isoforms :

All Interleukin Related Isoforms :

In Vitro

PTPRO-IN-1 (Compound 30k) (5 μM; 30 h) dose-dependently inhibits LPS (HY-D1056)-induced p-p65 expression and IL-6 secretion, as well as upregulation of TLR4 and phosphorylation of IKKα/β, in murine RAW264.7 and human THP-1 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

LPS-stimulated Raw 264.7 cells and THP-1-derived macrophages
Concentration:

5 μM
Incubation Time:

24 hours, followed by 1 μg/mL LPS stimulation for 4 hours
Result:

Dose-dependently inhibited LPS-induced p-p65 and IL-6 secretion.
Inhibited TLR4 upregulation and phosphorylation of IKKα/β.

In Vivo

PTPRO-IN-1 (Compound 30k) (20 mg/kg; p.o.; once daily for 10 consecutive days) exerts significant therapeutic effects in a DSS (HY-116282C)-induced mouse colitis model^[1].

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

Animal Model:

male C57BL/6J mice (6-8 weeks
old)^[1]
Dosage:

20 mg/kg
Administration:

i.g.; once daily for 10 days
Result:

Significantly reversed intestinal shortening and alleviated histological inflammation.
Significantly down-regulated the secretion of IFN-γ and IL-2 in CD4⁺/CD8⁺ T cells.

Chemical Information

분자량 634.10
화학식 C₃₆H₂₄ClNO₆S
SMILES

OC1=CC=C(C#CC2=CC=C(C=C2)N(S(C3=CC=C4OC(C(O)=O)=CC4=C3)(=O)=O)CC5=CC=C(C=C5)C6=CC(Cl)=CC=C6)C=C1
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Liang X, et al. Discovery of Benzofuran-2-Carboxylic Acid Derivatives as Potent PTPRO Inhibitors with Oral Efficacy for Treatment of Inflammatory Bowel Disease. J Med Chem. 2026;69(9):11167-11191. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
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PTPRO-IN-1

All Toll-like Receptor (TLR) Isoforms

All NF-κB Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

PTPRO-IN-1 Related Classifications

HY-183573 Related Classifications