Pifithrin-α, p-nitro, cyclic
- CAS No.
- 60477-38-5
- Chemical Name:
- Pifithrin-α, p-nitro, cyclic
- Synonyms
- PFN-α;p-Nitro-CyclicPifithrin-α;p-Nitro-Cyclic Pifithrin-a;Cyclic pifithrin-α-p-nitro;p-nitro-Cyclic Pifithrin-α;Cyclic pifithrin-α-p-nitro;Pifithrin-α, p-nitro, cyclic;Pifithrin-alpha, p-Nitro, Cyclic;p-nitro Cyclic Pifithrin-.alpha.;Pifithrin-α, p-Nitro, Cyclic - CAS 60477-38-5 - Calbiochem
- CBNumber:
- CB43136760
- Molecular Formula:
- C15H13N3O2S
- Molecular Weight:
- 299.35
- MDL Number:
- MOL File:
- 60477-38-5.mol
Pifithrin-α, p-nitro, cyclic price More Price(9)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 506154 | Pifithrin-α, p-Nitro, Cyclic - CAS 60477-38-5 - Calbiochem A cell-permeable p53 inhibitor that exhibits 10-fold higher potency and 50% longer half-life than Pifithrin-α. |
60477-38-5 | 5mg | $172 | 2024-03-01 | Buy |
| Cayman Chemical | 17848 | p-nitro-Cyclic Pifithrin-α ≥95% | 60477-38-5 | 1mg | $37 | 2024-03-01 | Buy |
| Cayman Chemical | 17848 | p-nitro-Cyclic Pifithrin-α ≥95% | 60477-38-5 | 5mg | $108 | 2024-03-01 | Buy |
| Cayman Chemical | 17848 | p-nitro-Cyclic Pifithrin-α ≥95% | 60477-38-5 | 10mg | $195 | 2024-03-01 | Buy |
| Cayman Chemical | 17848 | p-nitro-Cyclic Pifithrin-α ≥95% | 60477-38-5 | 25mg | $397 | 2024-03-01 | Buy |
Pifithrin-α, p-nitro, cyclic Chemical Properties,Uses,Production
Uses
p-nitro-Cyclic Pifithrin-α is an inactivator of p53 that blocks p53-dependent transcriptional activation and apoptisis. Anti-cancer agent.
General Description
A cell-permeable p53 inhibitor that exhibits 10-fold higher potency (ED50 = 30 nM in protecting etoposide-induced cortical neuron death) and 50% longer half-life (t1/2 = 6h in neuron culture medium at 37°C) than Pifithrin-α (Cat. No. 506132). However, despite its in vitro efficacy, this inhibitor is not effective when adminstered in rats in vivo. For in vivo applications, please consider Pifithrin-α, p-Nitro (Cat. No. 506152).
Biological Activity
p-nitro-cyclic pifithrin-α is an inactivator of p53.the activation of the tumor suppressor gene p53 plays a key role in regulating the in-vitro death of neurons, following apoptotic stimuli molecules including glutamate and dna-damaging agents. thus, p53 inhibitors may prove effective in suppressing the degenerative processes in neurodegenerative disorders.
Biochem/physiol Actions
Cell permeable: yes
in vitro
pifithrin-α (pft-α) was identified as an inactivator of p53 blocking p53-dependent transcriptional activation and apoptosis. cyclic pft-α was a stable analog of pft-α. p-nitro-cyclic pft-α, a cell-permeable form of cyclic pft-α, was found to be one order of magnitude more active than pft-α in protecting cortical neurons exposed to etoposide. p-nitro-cyclic pft-α acted in a p53-dependently but did not block phosphorylation of p53 on ser15 in response to etoposide treatment, although it prevented p53 posttranscriptional activity [1].
in vivo
in a previou study, c57bl/6 mice were fed a high-fat (hfd) or control diet for 8 weeks; pft was administered three times per week. results showed that pft administration could suppress hfd-induced weight gain, steatosis, oxidative stress, alt elevation, and apoptosis. pft treatment also able to blunt the hfd-induced upregulation of mirna34a and increase sirt1 expression. in the livers of hfd-fed, pft-treated mice, activation of the sirt1/pgc1α/pparα axis increased the expression of malonyl-coa decarboxylase [2].
References
[1] . pietrancosta, n.,moumen, a.,dono, r., et al. imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: discovery of a highly potent in vivo inhibitor and its action mechanism. journal of medicinal chemistry 49(12), 3645-3652 (2006).
[2] derdak z, villegas ka, harb r, wu am, sousa a, wands jr. inhibition of p53 attenuates steatosis and liver injury in a mouse model of non-alcoholic fatty liver disease. j hepatol. 2013 apr;58(4):785-91.
Pifithrin-α, p-nitro, cyclic Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +undefined18621343501 | product@acmec-e.com | China | 33350 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51471 | 80 |
| Shanghai Rechem science Co., Ltd. | 21-31433387 15618786686 | sales@rechemscience.com | China | 2969 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 18892239720 | psaitong@jm-bio.com | China | 12308 | 58 |
| Angel Pharmatech, Ltd. | 17317130613 | 3358272972@qq.com | China | 3250 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |