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Cat. No.: HY-183548

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XW-17

XW-17 is a PARP14 inhibitor with an IC₅₀ of 3.03 nM and selectivity over other PARP family members.XW-17 suppresses PARP14-mediated mono-ADP-ribosylation, engages and stabilizes endogenous PARP14 protein.XW-17 attenuates skin lesions and decreases expression of IL-4, IL-13, IgE, and IL-17A in an atopic dermatitis-like mouse model.XW-17 can be used for the research of atopic dermatitis.

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화학식: C₂₄H₃₀N₆O₃
분자량:450.53

보관:

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

XW-17 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

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

PARP14

All PARP Isoforms :

In Vitro

XW-17 (1 h) potently and selectively inhibits purified PARP14 enzyme activity with an IC₅₀ of 3.03 nM, showing a selectivity index exceeding 9900 over PARP1^[1].
XW-17 shows excellent metabolic stability across rat plasma, mouse liver microsomes, rat liver microsomes, and human liver microsomes, with T_1/2 values greater than 240 min in all tested systems^[1].
XW-17 (5 μM; 2 h) exhibits satisfactory membrane permeability and low efflux in MDCK and Caco-2 cell models, with P_app A→B values of 16.32 × 10^-6 cm/s and 20.49 × 10^-6 cm/s, respectively^[1].
XW-17 (0.001-3 μM; unspecified duration) engages and stabilizes endogenous PARP14 in IFN-γ-stimulated CFPAC-1 cells with an EC₅₀ of 59.5 nM^[1].
XW-17 (0.01-1 μM; 6 h pretreatment, 24 h IFN-γ stimulation) potently inhibits PARP14-mediated MARylation in a concentration-dependent manner in IFN-γ-stimulated CFPAC-1 and RAW264.7 cells^[1].
XW-17 (up to at least 30 μM; 72 h) shows no significant cytotoxicity toward MCF-10A and AML-12 cells, with IC₅₀ values greater than 30 μM^[1].
XW-17 (5-30 μM) has low hERG potassium channel inhibitory activity, with 3.15% inhibition at 5 μM and 5.56% inhibition at 30 μM, indicating low cardiotoxicity risk^[1].

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

Western Blot Analysis^[1]

Cell Line:

CFPAC-1 cells
Concentration:

0.001-3 μM
Incubation Time:

unspecified duration (IFN-γ stimulation)
Result:

Induced a concentration-dependent upregulation of PARP14 protein expression, confirming target binding and stabilization, with an EC₅₀ of 59.5 nM.

Western Blot Analysis^[1]

Cell Line:

CFPAC-1 cells, RAW264.7 cells
Concentration:

0.01-1 μM
Incubation Time:

6 h pretreatment; 24 h IFN-γ stimulation
Result:

Reduced intracellular MARylation signals in a concentration-dependent manner in both cell lines, indicating inhibition of endogenous PARP14 catalytic activity.

Cell Cytotoxicity Assay^[1]

Cell Line:

MCF-10A human mammary epithelial cells, AML-12 mouse hepatocytes
Concentration:

up to at least 30 μM
Incubation Time:

72 h
Result:

Did not exhibit significant cytotoxicity, with IC₅₀ values exceeding 30 μM in both cell lines.

In Vivo

XW-17 (25-100 mg/kg; i.p.; twice daily; 11 days) dose-dependently ameliorates DNCB-induced atopic dermatitis in male BALB/c mice, with the 100 mg/kg i.p. twice daily dose achieving the greatest reduction in dermatitis scores, histopathological damage, and Th2/Th17-associated inflammatory mediators, outperforming positive controls RBN-3143 and Upadacitinib^[1].

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

Animal Model:

BALB/c (male, 18−22 g, DNCB-induced atopic dermatitis)^[1]
Dosage:

25 mg/kg; 50 mg/kg; 100 mg/kg
Administration:

i.p.; twice daily; 11 days
Result:

Significantly reduced dermatitis score compared to model group at 25 mg/kg (P < 0.05), 50 mg/kg (P < 0.01), and 100 mg/kg (P < 0.001).
Achieved lower dermatitis score than positive controls RBN-3143 and Upadacitinib at 100 mg/kg.
Dose-dependently reduced histopathological abnormalities in dorsal skin, with 100 mg/kg dose achieving lowest histological score and outperforming Upadacitinib.
Significantly reduced protein levels of IL-4, IL-13, IL-17A in skin homogenates and serum IgE at 50 mg/kg and 100 mg/kg, with most pronounced inhibition at 100 mg/kg.
Dose-dependently suppressed mRNA levels of IL-31, TSLP, and GATA3 in dorsal skin.
Showed no significant effect on Th1 pathway-related cytokines (TNF-α, IL-6, IL-1β) at any dose.
Caused no significant body weight loss or histological abnormalities in major organs (heart, liver, spleen, lung, kidney).

Chemical Information

분자량 450.53
화학식 C₂₄H₃₀N₆O₃
SMILES

CN1C=C(C=N1)CN2CCC(CC2)NC(CC3=NNC(C4=CC=C(C=C43)OCC5CC5)=O)=O
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]. Wu S, et al. Discovery of Highly Potent Phthalazinone Derivatives as PARP14 Inhibitors: From Structure-Based Virtual Screening to In Vivo Pharmacodynamic Activity. J Med Chem. 2026;69(9):10715-10733. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

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

상품명:
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XW-17

All PARP Isoforms