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Cat. No. | Product Name | Target | Signaling Pathways |
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T5858 |
Sertindole
Lu 23-174,舍吲哚 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Sertindole (Lu 23-174) 是一种非典型抗精神病药,可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合,Kd 值分别为 2.7、20、0.14 和 6 nM。 | |||
T8966 |
ML-298
ML298,CID53393915 |
Phospholipase | Metabolism |
ML-298 (CID53393915) 是一种磷脂酶 D2 的选择性抑制剂,其IC50=355 nM,能够抑制 U87-MG 胶质母细胞瘤细胞的侵袭性迁移。 | |||
T81184 | Sec61-IN-4 | ||
Sec61-IN-4(Compound 16b)作为Sec61抑制剂,其IC50值在U87-MG细胞中为0.04 nM。 | |||
T78804 |
PI3Kα-IN-12
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PI3K | PI3K/Akt/mTOR signaling |
PI3Kα-IN-12(化合物13),作为一种高度选择性的PI3Kα抑制剂,展现出了1.2 nM的IC50值。在HCT-116和U87-MG细胞线上的抑制作用,IC50s分别为0.83 μM和1.25 μM。通过腹腔注射(IP)给予40 mg/kg的PI3Kα-IN-12,能够有效引起接受U87-MG细胞系异种移植的小鼠模型中的肿瘤退缩。 | |||
T70890 |
ML309
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ML309 is a potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. ML309 is capable of potent and selective inhibition of mutant IDH1 and effectively lowers cell-based production of 2-HG in a U87MG mutant glioblastoma cell line. | |||
T81469 | PI3Kα-IN-14 | PI3K | PI3K/Akt/mTOR signaling |
PI3Kα-IN-14(复合物F8)是一款高度选择性的PI3Kα抑制剂,其IC50值为0.14 nM 。此化合物能显著降低线粒体膜的完整性,并在U87-MG细胞中引起G1期细胞周期的停滞以及凋亡现象。此外,PI3Kα-IN-14在不同来源的肿瘤细胞系中均展现出明显的抗增殖能力,其中PC-3的IC50为0.28 μM,HCT-116的IC50为0.57 μM,以及U87-MG的IC50为1.37 μM。 | |||
T38004 |
ML-309 (hydrochloride)
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ML-309 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It reversibly and selective inhibits IDH1R132H over wild-type IDH1 (IC50s = 96 and 36,500 nM, respectively). ML-309 reduces 2-hydroxyglutarate production in U87 MG glioblastoma cells (EC50 = 55 nM). | |||
T62060 | NF-κB-IN-5 | ||
NF-κB-IN-5 (化合物 4d) 是口服有效的靶向 NF-κB 抑制剂。NF-κB-IN-5 具有明显的抗肿瘤活性,抑制人癌细胞株,包括 HCT116、U87-MG、HepG2、BGC823、PC9,IC50分别为 5.35、2.81、2.83、2.02 和 3.90 μM。 | |||
T78773 |
Tubulin inhibitor 38
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Tubulin inhibitor 38(化合物14)是一款强效的四唑基微管蛋白抑制剂,能够显著抑制细胞增殖。以100 nM浓度作用24小时后,该抑制剂能够引起有丝分裂停滞,特别是在G2/M期细胞周期阶段,进而诱导细胞凋亡。在HeLa、MCF7和U87 MG细胞系中,Tubulin inhibitor 38展现了较高的细胞毒性及选择性。 | |||
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. | |||
T71261 | Arsthinol | ||
Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50/IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 +/- 0.08 micromol/l after 24 h) than As(2)O(3) (IC50 = 1.60 +/- 0.23 micro... | |||
T8968 |
ML299
VU0463568,ML-299 |
Phospholipase | Metabolism |
ML299 (VU0463568) 是一种有效的 DHCR7 抑制剂。 DHCR7 是胆固醇生物合成中的一种酶。 是一种磷脂酶 D1和磷脂酶 D2的选择性变构调节剂和双重抑制剂 (IC50值分别为 6 和 12 nM),能够抑制 U87-MG 胶质母细胞瘤细胞的侵袭性迁移。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T1166 |
Ellipticine
玫瑰树碱,NSC 71795,Elliptisine |
Topoisomerase | DNA Damage/DNA Repair |
Ellipticine (Elliptisine) 是一种有效的抗肿瘤剂,抑制 DNA 拓扑异构酶 II 活性,对白血病、神经母细胞瘤和胶质母细胞瘤有部分活性。 |