Date published: 2025-11-22

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MGMT Inhibitors

MGMT inhibitors are a distinctive group within the realm of chemical compounds recognized for their ability to modulate the function of O6-methylguanine-DNA methyltransferase (MGMT). These inhibitors operate by interfering with the interactions involving MGMT, an essential enzyme responsible for repairing DNA damage caused by alkylating agents. MGMT plays a pivotal role in safeguarding genomic integrity by counteracting mutations through the removal of alkyl groups from DNA. MGMT inhibitors are strategically designed to target specific binding sites or molecular pathways associated with MGMT, thereby affecting its cellular functions and subsequent consequences. The development of MGMT inhibitors entails a comprehensive comprehension of the structural attributes characterizing MGMT and its interactions with DNA substrates and alkylating agents. Researchers in this field diligently work to engineer molecules demonstrating heightened selectivity and affinity for MGMT, enabling precise modulation of its activities. These inhibitors often incorporate innovative design strategies aimed at disrupting key molecular interactions necessary for MGMT's catalytic efficiency. By unraveling the intricate mechanisms by which MGMT participates in DNA repair and the preservation of genetic stability, researchers aim to unearth its significance in fundamental cellular processes. Ongoing advancements in the arena of molecular pharmacology and chemical synthesis continue to guide the refinement of MGMT inhibitors, with the ability to find applications across a diverse range of scientific contexts where manipulation of MGMT-mediated processes is of interest.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Diethylamine NONOate

372965-00-9sc-202575
sc-202575A
sc-202575B
sc-202575C
10 mg
50 mg
100 mg
500 mg
$37.00
$111.00
$199.00
$882.00
1
(1)

Diethylamine NONOate is a unique compound known for its ability to release nitric oxide upon hydrolysis, facilitating various signaling pathways. Its structure allows for rapid diffusion across membranes, enhancing its reactivity with biological targets. The compound exhibits distinct electron-donating properties, which can influence redox reactions. Additionally, its interactions with metal ions can modulate catalytic processes, showcasing its versatility in chemical reactivity and molecular dynamics.

Temozolomide

85622-93-1sc-203292
sc-203292A
25 mg
100 mg
$89.00
$250.00
32
(1)

Temozolomide is an alkylating agent that methylates DNA at the O6 position of guanine. MGMT repairs this DNA damage by transferring the methyl group from O6-methylguanine to its active site, thus inactivating MGMT. Temozolomide inhibits MGMT, allowing O6-methylguanine to persist and trigger DNA mismatch repair, eventually leading to cell death.

O6-Benzylguanine

19916-73-5sc-202747
sc-202747A
10 mg
50 mg
$50.00
$77.00
7
(1)

6-Benzylthioinosine is an MGMT inhibitor that has been explored for its ability to sensitize cancer cells to alkylating agents. It interferes with the repair of O6-methylguanine lesions by MGMT, leading to DNA damage accumulation and potential cell death.

Lomeguatrib

192441-08-0sc-362764
sc-362764A
10 mg
50 mg
$205.00
$865.00
(0)

Lomeguatrib is a suicide inhibitor of MGMT. It irreversibly binds to the active site of MGMT, forming a covalent complex that prevents MGMT from repairing O6-methylguanine lesions in DNA. This enhances the efficacy of alkylating agents used in cancer chemotherapy.

NU2058

161058-83-9sc-202744
sc-202744A
5 mg
25 mg
$66.00
$321.00
2
(1)

NU2058 is another pseudosubstrate for MGMT that functions similarly to O6-Benzylguanine. It irreversibly inhibits MGMT by forming a covalent complex, preventing the repair of O6-methylguanine lesions in DNA.

Semustine

13909-09-6sc-391062
100 mg
$114.00
1
(0)

Semustine is an alkylating agent that induces the formation of O6-methylguanine lesions in DNA. MGMT repairs these lesions by transferring the methyl group to its active site. Inhibition of MGMT by Methyl-CCNU can enhance the cytotoxic effects of alkylating chemotherapy.

6-Ethyl Guanine

51866-19-4sc-496096
1 g
$393.00
(0)

O6-Ethylguanine is structurally similar to O6-methylguanine and acts as a substrate for MGMT. It binds to MGMT's active site and inactivates the enzyme by transferring the alkyl group from O6-ethylguanine. This prevents repair of O6-ethylguanine lesions.