Home Apoptosis p53 activator PRIMA-1 For research use only.

PRIMA-1

Synonyms: 2,2-Bis(hydroxymethyl)-3-quinuclidinone

PRIMA-1 (2,2-Bis(hydroxymethyl)-3-quinuclidinone) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.

PRIMA-1 Chemical Structure

PRIMA-1 Chemical Structure

CAS: 5608-24-2

Selleck's PRIMA-1 has been cited by 7 publications

Purity & Quality Control

Batch: S772301 DMSO] 37 mg/mL] false] Water] 37 mg/mL] false] Ethanol] 37 mg/mL] false Purity: >97%
97

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Signaling Pathway

p53 Signaling Pathways

p53 Signaling Pathway

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Biological Activity

Description PRIMA-1 (2,2-Bis(hydroxymethyl)-3-quinuclidinone) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
Targets
Mutant p53 [1]
In vitro
In vitro PRIMA-1 is converted to compounds that form adducts with thiols in mutant p53. Modification of thiol groups in mutant p53 by PRIMA-1 conversion products is sufficient to restore its tumor suppressor activity.[2]. PRIMA-1 inhibits the growth of pancreatic cancer cell lines and induces cell cycle arrest and decreases DNA synthesis. It selectively induces apoptosis and cell death in mutant p53-expressing pancreatic cancer cells and also leads to activation of p53-dependent apoptotic pathways. PRIMA-1 enhances the cytotoxicity of chemotherapeutic agents active against mutant p53 pancreatic cancer cells[1]. PRIMA-1 has antileukemic properties in acute promyelocytic leukemia-derived NB4 cells. PRIMA-1-triggered apoptosis is in a dose-dependent and time-dependent manner as indicated by the MTT assay and annexin-V staining. Apoptosis induction by PRIMA-1 is associated with caspase-9, caspase-7 activation and PARP cleavage. PRIMA-1 does not show any significant apoptotic effect in normal human peripheral blood mononuclear cells[4].
Cell Research Cell lines mutant p53 expressing pancreatic cancer cell lines PANC-1 (p.R273H) and BxPC-3 (p.Y220C) and the wild type p53-expressing Capan-2 cells (wtp53)
Concentrations 25-100 μM
Incubation Time 12-48 h
Method Cells are kept at a temperature of 37 °C, a minimum relative humidity of 95 %, and an atmosphere of 5 % CO2 in air. Cell viability is measured by MTT assay after treatment with PRIMA-1. Briefly, cells are seeded in each well of 96-well plates in 100 μl culture medium and incubated overnight at 37 °C in an atmosphere of 5 % CO2. The next day, the medium is removed and cells washed with PBS and treated with vehicle control(DMSO, dimethylsulfoxide) or different concentrations of PRIMA-1 for 12 to 48 h; the medium is replaced with MTT solution diluted in medium once the treatment is completed. The plates are further incubated at 37 °C under 5 % CO2 for 4 h and then left at room temperature until completely dry. DMSO was then added and the absorbance is read at 492 nm using a microplate enzyme-linked immunoassay reader (ELISA). The relative growth activity is determined as the percentage absorbance of treated cells compared to that of vehicle treated cells (control).
In Vivo
In vivo Intravenous (i.v.) injections of PRIMA-1 in mice does not cause any obvious changes in weight or behavior compared with untreated animals. PRIMA-1 has in vivo antitumor activity in this animal tumor model. It suppresses in vivo tumor growth in a mutant p53-dependent manner[3].
Animal Research Animal Models SCID mice
Dosages 1, 10, 20 and 100 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 185.22 Formula

C9H15NO3
CAS No. 5608-24-2 SDF Download PRIMA-1 SDF
Smiles C1CN2CCC1C(=O)C2(CO)CO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 37 mg/mL ( (199.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 37 mg/mL

Ethanol : 37 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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