Description
Key facts
CAS number:192441-08-0,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:326.17 Da,
Molecular formula:C10H8BrN5OS,
PubChem:3025944,
Nature:Synthetic,
Solubility:Soluble in DMSO to 100 mM,
Biochemical name:Lomeguatrib,
Biological description:Potent O6-methylguanine-DNA methyltransferase (MGMT) inhibitor (IC50 = 9 nM). Inhibits recombinant human ATase (IC50 = 5 nM). Shows antitumor effects in vivo. Enhances antitumor effects of temozolomide (ab141055).,
Canonical smiles:C1=C(SC=C1Br)COC2=NC(=NC3=C2NC=N3)N,
InChi:InChI=1S/C10H8BrN5OS/c11-5-1-6(18-3-5)2-17-9-7-8(14-4-13-7)15-10(12)16-9/h1,3-4H,2H2,(H3,12,13,14,15,16),
InChiKey:JUJPKFNFCWJBCX-UHFFFAOYSA-N,
IUPAC Name:6-[(4-bromothiophen-2-yl)methoxy]-7H-purin-2-amine
Product details:
Sold under license from CRT.
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
MGMT also known as O-6-methylguanine-DNA methyltransferase is an enzyme with a significant role in DNA repair. MGMT protein has a molecular weight of about 22 kDa. This protein is typically expressed in various tissues including the liver kidney and brain where it functions to protect cells from mutagenic and cytotoxic alterations. MGMT works by transferring alkyl groups from the O6 position of guanine to a cysteine residue within its active site. This mechanism directly reverses DNA damage maintaining genomic stability.
Biological function summary
MGMT prevents mutations by reversing alkylation damage playing a significant role in preserving DNA integrity. It acts independently and does not form part of any larger protein complexes. This enzyme-mediated repair is central to cellular defense against mutagenic threats such as alkylating agents. By curbing DNA damage MGMT can thwart the onset of harmful genetic mutations that might lead to issues like cancer development.
Pathways
MGMT is intimately involved in DNA damage response and repair pathways. Notably it interacts with base excision repair and direct reversal repair pathways. MGMT's function is distinct but complementary to the activities of other DNA repair proteins like XRCC1 and APE1 which are involved in the base excision repair pathway. The presence of MGMT bolsters cellular resilience by ensuring that DNA lesions caused by alkylating agents are addressed promptly and effectively.
MGMT has a profound association with several types of cancer such as glioblastoma and colorectal cancer. Reduced MGMT expression or activity can lead to enhanced susceptibility to the carcinogenic effects of alkylating agents making cancer development more likely. Additionally MGMT inhibitors such as lomeguatrib are used therapeutically to enhance the effectiveness of alkylating chemotherapy. Within this context MGMT interacts with proteins involved in tumor suppression and cell cycle regulation including p53 influencing both cancer progression and treatment outcomes.
