Pifithrin-¦Á (PFT¦Á)
Cat.No.£º
IC-012036
Product Information
Biological Activity
Pifithrin-¦Á (PFTalpha) is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. It prevents p53-mediated apoptosis induced by cytotoxic compounds in C8 cells at 10 ¦ÌM and in human umbilical vein endothelial cells at 30 ¦ÌM. Pifithrin-¦Á enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin, etopoxide, paclitaxel, and cytosine-¦Â-D-arabinofuranoside. Pifithrin-¦Á protects mice from lethal whole body ¦Ã-irradiation without an increase in cancer incidence. Pifithrin-¦Á can also protect cells from DNA damage-induced apoptosis by a p53-independent mechanism that might involve cyclin D1. In addition to p53, PFTalpha can suppress heat shock and glucocorticoid receptor signaling but has no effect on nuclear factor-kappaB signaling. Pifithrin-¦Á (PFTalpha) reduces activation of heat shock transcription factor (HSF1) and increases cell sensitivity to heat. Moreover, Pifithrin-¦Á reduces activation of glucocorticoid receptor and rescues mouse thymocytes in vitro and in vivo from apoptotic death after dexamethasone treatment.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species
Mouse
Rat
Rabbit
Guinea pig
Hamster
Dog
Weight (kg)
0.02
0.15
1.8
0.4
0.08
10
Body Surface Area (m2)
0.007
0.025
0.15
0.05
0.02
0.5
Km factor
3
6
12
8
5
20
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.
Chemical Information
Molecular Weight
367.3
Formula
C16H18N2OS.HBr
CAS Number
63208-82-2
Purity
>98%
Solubility
>DMSO 57mg/mL
Storage
at -20¡ãC
| Cell experiment [1]: | |
|
Cell lines |
Murine embryonic stem (ES) cells |
|
Preparation method |
The solubility of this compound in DMSO is >17.45mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37¡æ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20¡æ for several months. |
|
Reacting condition |
10 ¦ÌM and 20 ¦ÌM; 24 or 48 h |
|
Applications |
In murine ES cells, pifithrin-¦Á significantly reduced the number and colony size of the ES cells in a dose dependent way. In ES cells seeded at low density in the presence of LIF, pifithrin-¦Á significantly reduced the number of formed secondary ES cell colonies. |
| Animal experiment [2]: | |
|
Animal models |
Balb/c and C57BL6 mice treated with whole-body gamma irradiation |
|
Dosage form |
2.2 mg/kg; i.p. injection |
|
Application |
In Balb/c and C57BL6 mice treated with whole-body gamma irradiation, pifithrin-¦Á completely rescued mice of both strains from 60% killing doses of gamma irradiation (8 Gy for C57BL and 6 Gy for Balb/c). pifithrin-¦Á did not protect p53-null mice from lethal irradiation, suggesting that pifithrin-¦Á acted through a p53-dependent way. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References Information [1] Abdelalim EM, Tooyama I. The p53 inhibitor, pifithrin-¦Á, suppresses self-renewal of embryonic stem cells. Biochem Biophys Res Commun. 2012 Apr 13;420(3):605-10. [2] Komarov PG, Komarova EA, Kondratov RV, Christov-Tselkov K, Coon JS, Chernov MV, Gudkov AV. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science. 1999 Sep 10;285(5434):1733-7. |
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Product Name |
Cat.No. |
Quantity |
Price($) |
Price($) |
Availability |
|
Pifithrin-¦Á (PFT¦Á) |
IC-012036 |
5mg |
$112.00 |
€93.33 |
In stock |
|
Pifithrin-¦Á (PFT¦Á) |
IC-012036 |
10mg |
$162.00 |
€135.00 |
In stock |
|
Pifithrin-¦Á (PFT¦Á) |
IC-012036 |
50mg |
$420.00 |
€350.00 |
In stock |
