Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11419 |
O6BTG-octylglucoside
Glucose-conjugated MGMT inhibitor |
Others | Others |
O6BTG-octylglucoside is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor (IC50s: 10 nM and 32 nM in HeLa S3 cells and in vitro (cell extracts)). | |||
T0192 |
Levetiracetam
左乙拉西坦,UCB L059,SIB-S1 |
DNA Methyltransferase; Others; Calcium Channel | Chromatin/Epigenetic; Membrane transporter/Ion channel; Metabolism; Others |
Levetiracetam (SIB-S1) 是一种化学增敏剂,增强 Temozolomide 对胶质母细胞瘤干细胞增殖和凋亡的影响。它调节 HDAC 水平,最终使 MGMT 沉默从而提高 Temozolomide 的有效性。它是一种抗癫痫药,可结合突触小泡蛋白 SV2A。 | |||
T2495 |
Lomeguatrib
罗米鲁曲,PaTrin-2 |
DNA Methyltransferase; DNA Alkylation | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Lomeguatrib (PaTrin-2) 是修饰鸟嘌呤碱基,是MGMT 有效抑制剂,可抑制 DNA 修复蛋白 O(6)-烷基鸟嘌呤-DNA 烷基转移酶 (MGMT) 的活性。在非细胞体系和 MCF-7 细胞体系中,IC50值分别为 9 nM 和约 6 nM。 | |||
T7539 |
O6-Benzylguanine
O-6-苄基鸟嘌呤 |
Apoptosis; DNA Alkylation; DNA/RNA Synthesis | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
O6-Benzylguanine 是鸟嘌呤类似物,是 DNA 修复酶 O6 烷基鸟嘌呤DNA 烷基转移酶(MGMT/AGT)抑制剂,可诱导肿瘤细胞凋亡,具有抗肿瘤活性。它作为 AGT 底物,将其苄基转移到 AGT 半胱氨酸残基上,从而不可逆地灭活 AGT 并阻止 DNA 修复。 | |||
T26496 |
AA-CW236
AA-CW 236,AACW-236,AACW236,AACW 236,AA-CW-236 |
||
AA-CW236 is a covalent inhibitor of human O(6)-alkylguanine DNA methyltransferase (MGMT). | |||
T60281 | MPO-IN-4 | ||
MPO-IN-4 (compound 12) 是一种有效的选择性髓过氧化物酶 (MPO) 抑制剂,IC50为 25 nM。MPO-IN-4对甲状腺过氧化物酶(TPO)也显示抑制作用,IC50为2.2 μM。MPO-IN-4 对甲基鸟嘌呤甲基转移酶 (MGMT) 没有影响。 | |||
T36100 | K-TMZ | ||
K-TMZ is a DNA alkylating agent. It increases the concentration of O6-methylated deoxyguanosine in U87 glioblastoma multiforme (GBM) cells in a concentration-dependent manner. K-TMZ reduces cell viability of GBM cell lines lacking (IC50s = 18-44 μM) or expressing O6-methylguanine DNA methyltransferase (MGMT; IC50s = 115-240 μM). K-TMZ can cross the blood-brain barrier and increases survival in a Br23c mouse xenograft model of GBM when administered at a dose of 14.9 mg/kg. |