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Pifithrin-α, p-nitro, cyclic

Pifithrin-α, p-nitro, cyclic Structure
Pifithrin-α, p-nitro, cyclic structure
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;Pifithrin-α, p-nitro, cyclic;Pifithrin-alpha, p-Nitro, Cyclic;p-nitro Cyclic Pifithrin-.alpha.;Pifithrin-α, p-Nitro, Cyclic;Pifithrin-α, p-Nitro, Cyclic, 10 mM in DMSO
CBNumber:
CB43136760
Molecular Formula:
C15H13N3O2S
Molecular Weight:
299.35
MDL Number:
MOL File:
60477-38-5.mol
Last updated:2025-01-27 09:38:02
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Pifithrin-α, p-nitro, cyclic Properties

Melting point 233-234 °C(Solv: N,N-dimethylformamide (68-12-2); water (7732-18-5))
Density 1.53±0.1 g/cm3(Predicted)
storage temp. -20C
solubility ≤1mg/ml in dimethyl formamide
form Yellow solid
pka 6.14±0.20(Predicted)
color Light yellow to yellow
UNSPSC Code 12352200
NACRES NA.77

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
Product number Packaging Price Buy
506154 5mg $172 Buy
17848 1mg $37 Buy
17848 5mg $108 Buy
17848 10mg $195 Buy
17848 25mg $397 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

Pifithrin-α, p-nitro, cyclic Suppliers

Global( 47)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 33024 60
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32159 58
TargetMol Chemicals Inc. 		support@targetmol.com United States 38630 58
LEAPCHEM CO., LTD. 		+86-852-30606658 market18@leapchem.com China 43340 58
Shanghai Acmec Biochemical Technology Co., Ltd. 		+86-18621343501; +undefined18621343501 product@acmec-e.com China 33338 58
Aladdin Scientific 		tp@aladdinsci.com United States 52924 58
SHANGHAI KEAN TECHNOLOGY CO., LTD. 		+8613817748580 cooperation@kean-chem.com China 40066 58
SHANGHAI FORTUNE CHEMICAL TECHNOLOGY CO., LTD 13816107857 sales@fortunechem-sh.com China 825 58
Sigma-Aldrich 021-61415566 800-8193336 orderCN@merckgroup.com China 51456 80
Shanghai YuanYe Biotechnology Co., Ltd. 021-61312847; 18021002903 3008007409@qq.com China 71829 60
Supplier Advantage
ATK CHEMICAL COMPANY LIMITED 		60
TargetMol Chemicals Inc. 		58
TargetMol Chemicals Inc. 		58
LEAPCHEM CO., LTD. 		58
Shanghai Acmec Biochemical Technology Co., Ltd. 		58
Aladdin Scientific 		58
SHANGHAI KEAN TECHNOLOGY CO., LTD. 		58
SHANGHAI FORTUNE CHEMICAL TECHNOLOGY CO., LTD 58
Sigma-Aldrich 80
Shanghai YuanYe Biotechnology Co., Ltd. 60

View Lastest Price from Pifithrin-α, p-nitro, cyclic manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Pifithrin-α, p-Nitro, Cyclic pictures 2024-11-18 Pifithrin-α, p-Nitro, Cyclic
60477-38-5
 US $34.00-80.00 / mg 99.43% 10g TargetMol Chemicals Inc.
Pifithrin-α, p-Nitro, Cyclic pictures 2024-11-18 Pifithrin-α, p-Nitro, Cyclic
60477-38-5
 US $34.00-80.00 / mg 99.43% 10g TargetMol Chemicals Inc.

Pifithrin-α, p-nitro, cyclic Spectrum

Pifithrin-α, p-nitro, cyclic(60477-38-5)1HNMR
Pifithrin-α, p-nitro, cyclic p-nitro-Cyclic Pifithrin-α Pifithrin-alpha, p-Nitro, Cyclic 2-(4-Nitro-phenyl)-5,6,7,8-tetrahydro-benzo[d]imidazo[2,1-b]thiazole p-nitro Cyclic Pifithrin-.alpha. Cyclic pifithrin-α-p-nitro Pifithrin-α, p-Nitro, Cyclic - CAS 60477-38-5 - Calbiochem p-Nitro-Cyclic Pifithrin-a Imidazo[2,1-b]benzothiazole, 5,6,7,8-tetrahydro-2-(4-nitrophenyl)- p-Nitro-CyclicPifithrin-α PFN-α MDM-2/p53,Inhibitor,expression,p21,neurons,cortical,WAF1,Pifithrinα, pNitro, Cyclic,inhibit,death,p53-triggered,posttranscriptional,cell,Pifithrin α, p Nitro, Cyclic Cyclic pifithrin-alpha-p-nitro, transcriptional p53 inhibitor Pifithrin-α, p-Nitro, Cyclic, 10 mM in DMSO Pifithrin-α, p-Nitro, Cyclic 60477-38-5