Description
Key facts
CAS number:63208-82-2,
Purity:>95%,
Form:SolidSee storage information,
Molecular weight:367.3 Da,
Molecular formula:C16H19BrN2OS,
PubChem:9929138,
Nature:Synthetic,
Solubility:Soluble in DMSO to 100 mM,
Biochemical name:Pifithrin-alpha,
Biological description:p53 Inhibitor. Specifically blocks tumor supressor p53 transcriptional activity and can supress heat shock and glucocorticoid signalling pathways. Additionally offers protection to cells from p53 mediated apoptosis. Active in vivo; protects mice from chemotherapy side effects associated with p53 induction. Also aryl hydrocarbon receptor (AHR) agonist.,
Canonical smiles:CC1=CC=C(C=C1)C(=O)CN2C3=C(CCCC3)SC2=N.Br,
InChi:InChI=1S/C16H18N2OS.BrH/c1-11-6-8-12(9-7-11)14(19)10-18-13-4-2-3-5-15(13)20-16(18)17;/h6-9,17H,2-5,10H2,1H3;1H,
InChiKey:HAGVCKULCLQGRF-UHFFFAOYSA-N,
IUPAC Name:2-(2-imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-methylphenyl)ethanone;hydrobromide
Product details:
Pifithrin-α-HBr is light senstive and it is recommended that the compound is protected from light.
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
CYP1A1 and CYP1B1 are members of the cytochrome P450 family of enzymes alternatively known as AHH and aryl hydrocarbon hydroxylase. CYP1A1 has a mass of approximately 58 kDa while CYP1B1 weighs around 60 kDa. These enzymes are expressed in various tissues including the lungs liver and the gastrointestinal tract. Their mechanical role involves the oxidation of organic substances which is important for the metabolism of xenobiotics and endogenous compounds like steroids.
Biological function summary
These cytochrome P450 enzymes play a critical role in detoxifying numerous harmful compounds. They help metabolize polycyclic aromatic hydrocarbons and estrogens. CYP1A1 and CYP1B1 do not form a known multimeric complex but they do function in association with electron transfer partners like NADPH-cytochrome P450 reductase. This association aids in facilitating the enzymatic reactions important for metabolic processes.
Pathways
CYP1A1 and CYP1B1 participate prominently in the metabolic activation of procarcinogens and in estrogen metabolism pathways. These enzymes convert procarcinogens to their active carcinogenic forms influencing the risk of carcinogen-induced DNA damage. They also play a role in estrogen metabolism by hydroxylation of estrogens contributing to hormonal regulation. The pathways involve various proteins including NADPH-cytochrome P450 reductase and other members of the cytochrome P450 family.
CYP1A1 and CYP1B1 have a strong connection to cancer and glaucoma. Overexpression and polymorphisms in these enzymes are linked to an increased risk of lung cancer due to enhanced activation of carcinogens. In glaucoma mutations in CYP1B1 lead to structural changes that impair normal eye development. These connections to diseases highlight their interaction with regulatory proteins like p53 which plays a role in controlling cell proliferation and apoptosis. Understanding these relationships is important for developing targeted therapeutic strategies.
