JNJ26854165 Inhibitor CAS No. 881202-45-5

Cat. No.	Name	Size	Price
KI3714	JNJ26854165	5 mg	$188
	JNJ26854165	25 mg	$630
	JNJ26854165	100 mg	$1650

Chemical Characteristic

Product Name	JNJ26854165
CAS No.	881202-45-5
Molecular Weight	328.42
Formula	C₂₁H₂₀N₄
Chemical Name	N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine
Smiles	c1(ccc(cc1)Nc1ccncc1)NCCc1c[nH]c2c1cccc2
Chemical Structure

Biological activities

JNJ-26854165 is one of p53-activating agents and synergizes with AraC or doxorubicin to induce p53-mediated apoptosis and may provide a novel therapeutic approach for the treatment of acute leukemias ^[1]. JNJ-26854165, also named as Serdemetan, is now regarded as a novel oral Human Double Minute-2 (HDM-2) ubiquitin ligase antagonist. It can increase the level of HDM-2 client proteins, such as p53, by inhibiting the association of HDM-2-client protein complex with the proteosome. In vitro, it can be used by 0.44 ?M in REH cells ^[2]. In vivo, it can be used by 20 mg/kg/day in mice ^3].

References

[1] J. Tabernero, et al. Phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of HDM-2 antagonist JNJ-26854165 in patients with advanced refractory solid tumors. Journal of Clinical Oncology (Meeting Abstracts). 2009, 27. [2] Malcolm A. Smith, Gorlick R, Kolb EA, et al. Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program. Pediatric Blood & Cancer. 2012, 59(2): 329??32. [3] Lehman JA, Hauck PM, Gendron JM, et al. Serdemetan antagonizes the Mdm2-HIF1? axis leading to decreased levels of glycolytic enzymes. PLoS One. 2013, 8(9): e74741.

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