Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7008 |
Vacquinol-1
Vacquinol 1 |
JNK | MAPK |
Vacquinol-1 能够激活 MAPK 通路,是MKK4特异性激活剂。它可以诱导肝细胞癌细胞凋亡,在多形性胶质母细胞瘤小鼠模型中特异性诱导人胶质母细胞瘤细胞死亡、减缓肿瘤进展并延长生存期。 | |||
T16754 |
RIPGBM
|
Apoptosis | Apoptosis |
RIPGBM 是一种选择性诱导多形性胶质母细胞瘤癌症的细胞凋亡诱导剂 ,EC50≤500 nM。 | |||
T77706 |
4-Borono-L-phenylalanine
(s)-2-amino-3-(4-boronophenyl)propanoic acid,L-p-Boronophenylalanine |
Others | Others |
4-Borono-L-phenylalanine 具有抗肿瘤活性,可用于硼中子俘获疗法治疗黑色素瘤和多形性胶质母细胞瘤的临床试验。 | |||
T2116 |
AEE788
NVP-AEE 788 |
Apoptosis; EGFR; c-Fms; FLT; Bcr-Abl | Angiogenesis; Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
AEE788 (NVP-AEE 788)是EGFR 和ErbB2的抑制剂,IC50值分别为2和6 nM。它已用于研究癌症、多形性胶质母细胞瘤以及脑和中枢神经系统肿瘤治疗的试验。 | |||
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。 | |||
T11118 |
Duocarmycin SA
|
Others | Others |
Duocarmycin SA is an extremely potent cytotoxic agent and antitumor antibiotic that induces sequence-selective alkylation of duplex DNA, with an IC50 of 10 pM. It demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells when combined with proton radiation in vitro. | |||
T78771 |
Tubulin inhibitor 36
|
||
Tubulin inhibitor 36 (Compound 10) 是新型高效微管蛋白抑制剂,可阻止微管蛋白聚合并诱发细胞凋亡,IC50值为1.5±0.1 μM。该化合物在抗有丝分裂中表现出显著活性,并对胶质母细胞瘤(GBM)细胞线有效,适用于胶质母细胞瘤(GBM)的抗肿瘤研究。 | |||
TP1589L |
EGFRvIII peptide PEPvIII acetate
|
Others | Others |
EGFRvIII peptide PEPvIII acetate 是一种肿瘤特异性突变,在多形性胶质母细胞瘤 (GBM) 和其他肿瘤中广泛表达并增强致瘤性。 | |||
T35542 |
LLP-3
|
||
Survivin (also known as baculoviral IAP repeat-containing protein 5 (BIRC5)) is a member of the inhibitor of apoptosis (IAP) family that interacts with and inhibits the apoptotic function of several proteins. LLP-3 is a cell-permeable ligand of Survivin that blocks its interaction with Ran, resulting in the induction of apoptosis (IAP) in glioma stem cells (IC50 = 31 μM). It abolishes the growth of glioblastoma multiforme cell in spheres and in tumor slice cultures. | |||
T68663 |
GPI-15427
|
||
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... | |||
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. | |||
T63797 | PDZ1i | ||
PDZ1i 是有效的、能够透过血脑屏障的 MDA-9/Syntenin 特异性抑制剂。PDZ1i 能够抑制关键的 GBM (多形性成胶质细胞瘤)信号,包括 FAK 及 EGFRvIII,并能够减少 MMP 分泌。PDZ1i 可以提高患脑瘤小鼠的生存率并减少肿瘤的侵袭。 | |||
T76911 | Asunercept | ||
Asunercept (APG101; CAN008) 是一种靶向CD95L 的可溶性CD95-Fc 融合蛋白。Asunercept 通过选择性地与CD95L 结合,来破坏CD95/CD95L 的信号传导。Asunercept 可用于多形性胶质母细胞瘤 (GBM)、骨髓增生异常综合征 (MDS) 以及移植物抗宿主病 (GvHD) 的研究。 | |||
T72832 |
MDM2-p53-IN-16
|
||
MDM2-p53-IN-16 是MDM2-p53复合体抑制剂,其IC50值针对人MDM2-p532复合体为4.3 nM。该化合物能够重新激活p53,进而诱导多形性成胶质细胞瘤(GBM)细胞的凋亡和细胞周期阻滞,适用于癌症研究。 | |||
T60348 |
N1,N11-Diethylnorspermine
|
||
N1,N11-Diethylnorspermine (DENSPM) 是一种有效的抗癌剂。N1,N11-Diethylnorspermine 是一种精胺类似物,可激活多胺分解代谢。N1,N11-Diethylnorspermine 诱导细胞色素 c 从线粒体中释放,导致 caspase 3的激活。N1,N11-Diethylnorspermine 通过诱导亚精胺/精胺 N1- 乙酰转移酶 (SSAT) 结合产生过氧化氢杀灭多形胶质母细胞瘤 (GBM) 细胞。 | |||
T72658 | cRIPGBM chloride | ||
cRIPGBM chloride是一种口服有效的促凋亡衍生物,针对多形性胶质母细胞瘤(GBM)中的癌症干细胞(CSC)。该化合物通过靶向受体相互作用蛋白激酶2(RIPK2),诱导caspase 1依赖的细胞凋亡,抑制RIPK2/TAK1的活性,增加RIPK2/caspase 1复合物的形成,表现出强大的体内抗肿瘤效果。 | |||
T83716 |
KSL-128114 TFA
Ac-rRrGrKkRrSHWX1X2DI-OH (X1=tert-Leucine; X2=Cyclohexylglycine) |
||
KSL-128114是一种对膜调节剂syntenin的肽抑制剂(Ki = 300 nM)。它能够依赖浓度降低A2058黑色素瘤和患者来源的多形性胶质母细胞瘤(GBM)细胞的存活率。在使用患者来源的GBM细胞并在颅内植入前用KSL-128114培养的患者衍生异种移植(PDX)小鼠模型中,KSL-128114(50 µM)提高了动物的存活时间。 | |||
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。 |