Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T36100 |
K-TMZ
|
Others | Others |
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. | |||
T1178 |
Temozolomide
NSC 362856,替莫唑胺,TZM,CCRG 81045,TMZ |
Apoptosis; DNA Alkylator/Crosslinker; DNA/RNA Synthesis; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
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。 | |||
T4517 |
L189
|
DNA; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
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。 | |||
T21463 |
Temozolomide Acid
TMZA,3,4-二氢-3-甲基-4-氧代咪唑并[5,1-D]-1,2,3,5-四嗪-8-甲酰胺酸 |
Others | Others |
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。 | |||
T35688 |
MTIC
NSC 407347 |
Drug Metabolite | Metabolism |
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。 | |||
T61694 |
PARP1-IN-10
|
Others | Others |
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]. | |||
T68663 |
GPI-15427
|
Others | Others |
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... |