Pifithrin-Î¼

Description

Name: Pifithrin-Î¼
Brand: Selleckchem
SKU: S2930

Description

Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.

In vitro

Pifithrin-μ interferes with p53 binding to mitochondria and inhibits rapid p53-dependent apoptosis of primary cell cultures of mouse thymocytes in response to gamma radiation. ^[1] Pifithrin-μ, as an inhibitor of inducible HSP70, significantly inhibited cell viability with IC50 values ranging from 2.5 to 12.7 μM in acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines, as well as in primary AML blasts. Pifithrin-μ is also highly active in primary AML blasts with a median IC50 of 8.9 μ M(range 5.7-37.2 μ M) and induces apoptosis and cell cycle arrest in a dose-dependent fashion. In addition, Pifithrin-μ also increases the active form of caspase-3 and reduces AKT and ERK1/2 in NALM-6 cells. ^[2] Pifithrin-μ increases Annexin V(+) cells in both caspase-dependent and -independent manners and promotes TRAIL-induced apoptosis and arrested cancer cell growth. ^[3]

Pifithrin-μ (40 mg/kg, ip) produces protective effect from p53-dependent apoptosis in C57B1/6J mice of 8 or 9 Gy of total body gamma radiation. ^[1] In a xenograft mouse model, Pifithrin-μ significantly enhances the inhibition of TRAIL on MiaPaca-2 tumor growth. ^[3]

Pifithrin-μ

Catalog No.S2930

Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.

Size

Price

Stock

Quantity

10mg	USD 122	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Cell lines	Primary thymocytes
Concentrations	0-10 μM
Incubation Time	24 hours
Method	The number of attached cells is estimated by staining with 0.5% methylene blue and measuring optical density using a Multiscan Ascent microplate reader. Cell viability is determined in suspension of short-term culture of primary thymocytes by staining them with 0.1% trypan blue2 or by analysis of annexin- or propidium iodide (PI)-positive cells by FACScan.

Animal Models	C57B1/6J mice.
Dosages	~40 mg/kg
Administration	i.p.
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 10 mg/mL

Solubility (25°C) *	In vitro	DMSO	36 mg/mL (198 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	36 mg/mL (198 mM)
	In vivo	1% DMSO/30% polyethylene glycol/1% Tween 80,	10 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.