PJ34 hydrochloride is a potent, selective PARP-1 inhibitor. PJ34 displays activity at Pim-1 and Pim-2 kinases at higher concentrations (IC50 values are 3.7 and 16 μM respectively). PJ34 significantly suppresses HepG2 cell growth in a dose-dependent manner, and inhibits HepG2 cell-derived tumor growth in nude mice.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Identification of pim kinases as novel targets for PJ34 with confounding effects in PARP biology.
Antolín AA, et al. ACS Chem Biol. 2012 Dec 21;7(12):1962-7. PMID: 23025350.
PJ34, an inhibitor of PARP-1, suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells.
Huang SH, et al. Oncol Rep. 2008 Sep;20(3):567-72. PMID: 18695907.
Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke.
Abdelkarim GE, et al. Int J Mol Med. 2001 Mar;7(3):255-60. PMID: 11179503.
|Related PARP Products|
|Niraparib (MK-4827) tosylate
Niraparib (MK-4827) tosylate is an excellent PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively.
Daidzein is an inactive analogue of genistein, a tyrosine kinase inhibitor and an estrogen receptor activator.
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.
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