| Identification | Back Directory | [Name]
PARP1-IN-5 (dihydrochloride) | [CAS]
2823308-89-8 | [Synonyms]
PARP1-IN-5 (dihydrochloride)
PARP1 IN 5 dihydrochloride?,PARP-1-IN-5 (dihydrochloride),PARP1IN5 dihydrochloride | [Molecular Formula]
C25H25ClN2O5S | [MOL File]
2823308-89-8.mol | [Molecular Weight]
500.99 |
| Hazard Information | Back Directory | [Uses]
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer[1]. | [in vivo]
PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1].
PARP1-IN-5 dihydrochloride (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg[1].
PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1].
PARP1-IN-5 dihydrochloride can upregulate the expression of γ-H2AX and decrease the expression of PAR[1]. | Animal Model: | Mice[1] | | Dosage: | 1000 mg/kg | | Administration: | P.o. | | Result: | There was no significant difference in the body weight and blood routine.
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| Animal Model: | Mice[1] | | Dosage: | 25 and 50 mg/kg | | Administration: | P.o.; 12 days | | Result: | Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg.
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| Animal Model: | Male Sprague?Dawley (SD) rats[1] | | Dosage: | 50 mg/kg (Pharmacokinetic Analysis) | | Administration: | P.o. | | Result: | Positively correlated with the expression of PARP-1.
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| [IC 50]
PARP-1: 14.7 nM (IC50); PARP-2: 0.9 μM (IC50) | [References]
[1] Long H, et al. Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer. J Med Chem. 2021;64(16):12089-12108. DOI:10.1021/acs.jmedchem.1c00735 |
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| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 19945035818 |
| Website: |
www.topule.com/ |
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