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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
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

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

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)

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

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。

化合物

Sertindole
Cat.No: T5858
Synonym: Lu 23-174,舍吲哚
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy
ML-298
Cat.No: T8966
Synonym: ML298,CID53393915
Target: Phospholipase
Sec61-IN-4
Cat.No: T81184
Synonym:
Target:
PI3Kα-IN-12
Cat.No: T78804
Synonym:
Target: PI3K
ML309
Cat.No: T70890
Synonym:
Target:
PI3Kα-IN-14
Cat.No: T81469
Synonym:
Target: PI3K
ML-309 (hydrochloride)
Cat.No: T38004
Synonym:
Target:
NF-κB-IN-5
Cat.No: T62060
Synonym:
Target:
Tubulin inhibitor 38
Cat.No: T78773
Synonym:
Target:
K-TMZ
Cat.No: T36100
Synonym:
Target:
Arsthinol
Cat.No: T71261
Synonym:
Target:
ML299
Cat.No: T8968
Synonym: VU0463568,ML-299
Target: Phospholipase
Cat. No. Product Name Target Signaling Pathways
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。

天然产物

Ellipticine
Cat.No: T1166
Synonym: 玫瑰树碱,NSC 71795,Elliptisine
Target: Topoisomerase
TargetMol Loading
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