Name | Pifithrin-mu |
Synonyms | CS-1119 Pifithrin-u Pifithrin-- Pifithrin-mu PIFITHRIN-MU PHENYLETHYNESULFONAMIDE PHENYLETHYNSULFONIC ACID AMIDE Phenyl-ethynesulfonic Acid Amide |
CAS | 64984-31-2 |
InChIKey | ZZUZYEMRHCMVTB-UHFFFAOYSA-N |
Molecular Formula | C8 H7 N O2 S |
Molar Mass | 181.21 |
Density | 1.39±0.1 g/cm3(Predicted) |
Melting Point | 135.0 to 139.0 °C |
Boling Point | 351.7±25.0 °C(Predicted) |
Solubility | DMSO: soluble >10mg/mL, clear |
Appearance | solid |
Color | White or off-white |
pKa | 7.96±0.60(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
In vitro study | Pifithrin-μ interferes with p53 binding to mitochondria and inhibits the rapid apoptosis of p53-dependent mouse thymocyte primary cells in response to gamma irradiation. Pifithrin-μ, as an inducible inhibitor of HSP70, acts on cell lines of acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL), its IC50 value for significantly inhibiting cell activity ranges from 2.5 to 12.7 μm, and it can also act on primary AML mother cells. Pifithrin-μ can also efficiently act on primary AML mother cells with an intermediate value of IC50 (range 5.7-37.2 μm) 8.9 μm, and induce apoptosis and cell cycle arrest in a dose-dependent manner. In addition, pifithrin-μ acts on NALM-6 cells to enhance activated Caspase-3 and reduce AKT and ERK1/2. Pifithrin-μ increases Annexin V (+) cells in both a Caspase-dependent and independent manner, promotes TRAIL-induced apoptosis, and prevents cancer cell growth. |
In vivo study | Pifithrin-μ (40 mg/kg, ip) produced a protective effect against p53-dependent apoptosis in C57B1/6J mice 8 or 9 irradiated with Gy whole body gamma. In a mouse model bearing xenografts, pifithrin-μ significantly enhanced the inhibitory effect of TRAIL on MIAPACA-2 tumor growth. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
Hazard Class | IRRITANT |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 5.518 ml | 27.592 ml | 55.184 ml |
5 mM | 1.104 ml | 5.518 ml | 11.037 ml |
10 mM | 0.552 ml | 2.759 ml | 5.518 ml |
5 mM | 0.11 ml | 0.552 ml | 1.104 ml |
biological activity | pifithrin-μ (NSC 303580, pftμ, 2-phenylethenesulfonamide) is a specific p53 inhibitor, by reducing its affinity to Bcl-xL and Bcl-2, it also inhibits HSP70 function and autophagy. |
Target | Value |