Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T60870 | BRG1-IN-1 | ||
BRG1-IN-1 (Compound 11d) 是BRG1的有效抑制剂。在体外使 GBM 细胞对 Temozolomide 的抗增殖和细胞死亡诱导增敏时,其疗效优于 PFI-3 。BRG1-IN-1增强 Temozolomide 对皮下 GBM 肿瘤生长的抑制作用。 | |||
T78202 | IV-255 | Epigenetic Reader Domain | Chromatin/Epigenetic |
IV-255为BRG1溴域的选择性小分子抑制剂,能增强Temozolomide及Bleomycin诱导的DNA损伤。此外,IV-255抑制GBM细胞侵袭,并强化Temozolomide诱导的细胞死亡与细胞凋亡活性。 | |||
T61694 |
PARP1-IN-10
|
||
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]. | |||
T79642 |
IV-275
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
IV-275为BRG1与BRM溴域的抑制剂,能够增强Temozolomide和Bleomycin所诱导的DNA损害。此外,IV-275可抑制GBM(Glioblastoma multiforme)细胞的侵袭性,并增强Temozolomide所诱导的细胞凋亡。 | |||
T71908 |
NU1085
|
||
NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h. | |||
T41151 |
K34c
|
||
K34c is a potent and selective α5β1 integrin inhibitor (IC50 = 3.1 nM). K34c inhibits cell survival and migration, inhibits p53-dependent senescence induced by Temozolomide or Ellipticine and promotes apoptosis in U87MG cells. K34c also prevents TGFβ-induced infiltrationin vivoand reduces cell adhesion on fibronectin. | |||
T69596 |
SK-575
|
||
SK-575 is a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations and induces potent and specific degradation of PARP1 in various human cancer cells even at low picomolar concentrations. SK-575 achieves durable tumor growth inhibition in mice when used as a single agent or in combination with cytotoxic agents, such as temozolomide and cisplatin. | |||
T79487 | MAO A/HSP90-IN-2 | Monoamine Oxidase | Neuroscience |
MAO A/HSP90-IN-2(compound 4-C)是一种针对HSP90和MAO A的双重抑制剂,显示出分别对这两种酶有0.016 μM和4.58 μM的IC50值。该化合物能够上调HSP70,降低HER2和磷酸化AKT的表达,同时能减少GL26细胞中由IFN-γ诱导的PD-L1表达增加。此外,MAO A/HSP90-IN-2能够抑制对Temozolomide敏感或耐药的胶质母细胞瘤(GBM)、结肠癌、白血病和非小细胞肺癌细胞的生长,并可能有助于阻止肿瘤逃避免疫监控。 | |||
T83912 |
HR68
PP21 |
||
HR68是一种抗癌化合物,是过氧化物酶体增殖物激活受体(PPAR)激动剂非诺贝酯的衍生物。它能降低LN-229胶质母细胞瘤细胞的存活率(IC50 = 1.17 µM)。HR68能够穿越血脑屏障,在对替莫唑胺耐药的原位患者衍生的异种移植(PDX)小鼠胶质母细胞瘤模型中发挥作用。 |