tmz

Temozolomide (TMZ) 是一种 DNA 烷基化剂，具有血脑屏障渗透性和口服活性。Temozolomide 具有抗肿瘤活性和抗血管生成活性，还可以诱导细胞凋亡和自噬。 Temozolomide 在酸性条件下稳定，在中性或微碱性条件下会发生水解。

L189 是一种人类 DNA 连接酶抑制剂，抑制 hLigI III IV，IC50值分别为5、9 和 5 μM。

MMC(TMZ)-TOC TFA 对生长抑素受体亚型 2 (SSTR2) 展现出卓越的结合亲和力及选择性，具有靶向将 TMZ 递送至 SSTR2 阳性肿瘤细胞的能力。该化合物适用于癌症研究。

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.

Temozolomide Acid (TMZA) 是 temozolomide (TMZ) 的代谢物。TMZ 在体外具有抗癌活性。TMZ 是一种口服烷化剂，用于治疗多形性胶质母细胞瘤 (GBM) 和星形细胞瘤。

GNF362 是一种可口服且具有选择性和高效性的肌醇三磷酸3'激酶 B (ITPKB) 抑制剂，抑制 Itpka 和 Itpkc，可克服 TMZ 化疗耐药性，选择性地删除了供体同种异体反应性T细胞。GNF362 可逆转 ITPKA 过表达对迁移的刺激作用。

MTIC 是 Temozolomide (TMZ) 的活性代谢物，具有抗癌抗肿瘤活性，可用于研究黑色素瘤。

PARP1-IN-10 (compound 12c) is a highly potent and non-cytotoxic PARP1 inhibitor, displaying an in vitro IC50 value of 50.62 nM. This compound effectively induces cell cycle arrest at the G2 M phase and apoptosis, while also significantly augmenting the cytotoxic effects of temozolomide (TMZ) [1].

GPI-15427 is a potent PARP-1 inhibitor capable of crossing the blood-brain barrier, which can significantly increased the antitumor activity of the methylating agent TMZ against malignant melanoma, glioblastoma multiforme, or lymphoma growing at the CNS site. GPI-15427 acts as a potent inhibitor of the enzyme, being capable of inhibiting the activity of purified PARP-1 at nanomolar concentrations. GPI-15427 induced significant sensitization to radiotherapy, representing a promising new treatment in the management of HNSCC.

PP5-IN-2 是一种具有口服活性的蛋白磷酸酶 5 (PP5) 选择性抑制剂，IC50 值达 0.9 μM。在 U87 MG 细胞系中，该化合物能够激活 p53，并降低细胞周期蛋白 D1 与 MGMT 的表达，显示出其在引起细胞周期停滞和克服 Temozolomide (TMZ) 耐药性方面的潜力。此外，PP5-IN-2 在异种移植的小鼠模型中有效地抑制了肿瘤的生长。