2. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation
  3. PARP Interleukin Related
  4. PARP14 inhibitor 1

PARP14 inhibitor 1 is an orally active, selective PARP14 inhibitor with an IC50 of 5.52 nM. PARP14 inhibitor 1 exhibits favorable pharmacokinetic properties and in vivo safety. PARP14 inhibitor 1 enhances and stabilizes intracellular endogenous PARP14 protein levels, while effectively reducing the expression levels of IL-4, IL-13 and IL-17A. PARP14 inhibitor 1 can be used in research related to atopic dermatitis.

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PARP14 inhibitor 1

PARP14 inhibitor 1 Chemical Structure

CAS No. : 3035493-13-8

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PARP14 inhibitor 1 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

PARP14 inhibitor 1 is an orally active, selective PARP14 inhibitor with an IC50 of 5.52 nM. PARP14 inhibitor 1 exhibits favorable pharmacokinetic properties and in vivo safety. PARP14 inhibitor 1 enhances and stabilizes intracellular endogenous PARP14 protein levels, while effectively reducing the expression levels of IL-4, IL-13 and IL-17A. PARP14 inhibitor 1 can be used in research related to atopic dermatitis[1].

IC50 & Target

PARP14

5.52 nM (IC50)

IL-4

 

IL-13

 

IL-17A

 

PARP3

2024 nM (IC50)

PARP5A

1964 nM (IC50)

PARP5B

1330 nM (IC50)

PARP7

1973 nM (IC50)

PARP10

5232 nM (IC50)

human PARP12

3752 nM (IC50)

PARP15

916 nM (IC50)

In Vivo

PARP14 inhibitor 1 (Q22) (30-270 mg/kg; p.o.; once daily; for approximately 14 days) dose-dependently reduces DNCB-induced dermatitis scores, skin histopathological damage, and levels of inflammatory cytokines/mediators in a mouse model of atopic dermatitis. The 90 mg/kg dose group shows better efficacy than RBN-3143 (HY-150207), while the efficacy of the 270 mg/kg dose group is comparable to that of Upadacitinib (HY-19569)[1].
PARP14 inhibitor 1 (2000 mg/kg; p.o.; single administration) exhibits favorable in vivo safety in BALB/c mice, with no toxicity observed within 10 days[1].

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

Animal Model: BALB/c mice with Atopic dermatitis (male, n=6 per group, DNCB-induced atopic dermatitis model)[1]
Dosage: 30 mg/kg; 90 mg/kg; 270 mg/kg
Administration: p.o.; daily; ~14 days
Result: Reduced dermatitis scores in a dose-dependent manner, with the 90 mg/kg group showing greater improvement than a positive control reference group, and the 270 mg/kg group showing efficacy comparable to another positive control reference group.
Mitigated histopathological skin changes (thickened epidermis/dermis, hyperkeratosis, collagen degeneration, vasodilation, inflammatory cell infiltration) in a dose-dependent manner, with the 270 mg/kg group achieving a histological score similar to the Upadacitinib reference group and superior to the RBN-3143 reference group.
Significantly decreased skin protein levels of IL-4, IL-13, and IL-17A, and serum IgE levels in 90 mg/kg and 270 mg/kg groups, with the 270 mg/kg group showing the lowest cytokine levels.
Reduced skin mRNA expression of IL-4, IL-13, and IL-17A in a dose-dependent manner; the 90 mg/kg group showed greater efficacy than the RBN-3143 (HY-150207) group, and the 270 mg/kg group showed efficacy comparable to the Upadacitinib (HY-19569) group.
Most effectively reduced skin mRNA expression of TSLP and GATA3 in the 270 mg/kg group, with weak regulation of IL-33 mRNA levels.
Showed no significant body weight loss during the study.
Molecular Weight

426.48

Formula

C23H27FN4O3
CAS No.
SMILES

O=C1NC(N2CC3(C2)CCN(CC3)C(C4CC4)=O)=NC5=CC(OCC6CC6)=CC(F)=C51
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
References
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PARP14 inhibitor 1 Related Classifications

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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:

PARP14 inhibitor 13035493-13-8PARPInterleukin Relatedpoly ADP ribose polymerase ILJAK1 inhibitorPARP14BALB/c miceIL-17AIL-13inflammatory cytokineatopic dermatitisIL-4DNCB-induced atopic dermatitis miceInhibitorinhibitorinhibit

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