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14

抑制剂 & 化合物

4

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Cat. No. Product Name Target Signaling Pathways
T8922 SRS11-92

AA9

Ferroptosis Apoptosis
SRS11-92 (AA9) 是一种铁死亡抑制剂和 Ferrostatin-1 的衍生物。它抑制 Erastin 诱导的 HT-1080 人纤维肉瘤细胞铁致细胞死亡,EC50为6 nM。
T8317 5'-Fluoroindirubinoxime

5'-FIO

FLT Angiogenesis; Tyrosine Kinase/Adaptors
5'-Fluoroindirubinoxime (5'-FIO) 是一种 Indirubin 的衍生物,是一种 FLT3 的抑制剂(IC50:15 nM)。
T6500 Ferrostatin-1

Ferrostatin 1,Ferrostatin-1 (Fer-1)

Ferroptosis; Antifungal Apoptosis; Microbiology/Virology
Ferrostatin-1 (Fer-1) 是一种铁死亡抑制剂,具有强效性和选择性。Ferrostatin-1 有效抑制 Erastin 诱导的 HT-1080 细胞铁死亡 (EC50=60 nM)。Ferrostatin-1 还具抗氧化和抗真菌活性。
T4309 CIL56

CA3

Ferroptosis; ROS Apoptosis; Immunology/Inflammation
CIL56 (CA3) 是一种选择性铁死亡诱导剂,可通过产生铁依赖性活性氧来诱导细胞铁死亡。
T6334 Ridaforolimus

AP23573,Deforolimus,MK-8669

mTOR; Autophagy Autophagy; PI3K/Akt/mTOR signaling
Ridaforolimus (AP23573) 是亲脂性大环内酯类抗生素雷帕霉素的小分子非前药类似物,具有潜在的抗肿瘤活性。它是一种有效和选择性的 mTOR 抑制剂,在 HT-1080 细胞中抑制 S6 磷酸化的 IC50值为 0.2 nM。
T36404 PRLX-93936

PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM...
T70527 DAT-230

DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated ...
T36398 Paclitaxel octadecanedioate

Paclitaxel octadecanedioate is a prodrug form of paclitaxel that is comprised of paclitaxel conjugated to 1,18-octadecanedioic acid.1 Unlike paclitaxel, it does not promote tubulin polymerization in vitro when used at a concentration of 10 μM. A 5:1 mixture of paclitaxel octadecanedioate:human serum albumin (HSA) is cytotoxic to HT-1080, PANC-1, and HT-29 cells (IC50s = 12, 2.48, and 8.62 nM, respectively). This mixture reduces tumor growth and increases survival in an HT-1080 mouse xenograft mo...
T32009 GSK321

GSK 321,GSK-321

GSK321 is an effective and selective IDH1 mutation inhibitor, which can effectively inhibit the production of 2-HG in HT-1080 cells, and induce IDH1 mutant cells to differentiate into bone marrow at the level of leukemia blasts and more stem cells.
T35994 Erastin2

Erastin2

Erastin2 is a ferroptosis inducer and an inhibitor of the system xc- cystine/glutamate transporter.[1] [2] It inhibits glutamate release in CCF-STTG1 cells (IC50 = 0.0035 &#181M).[2] It induces cell death in HAP1 cells when used at a concentration of 5 &#181M, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 or deferoxamine . [1] Erastin2 also induces ferroptotic cell death in HT-1080 cells (EC50 = 0.15 &#181M), an effect that can be blocked by the reducing agent β-merc...
T82408 Ferroptosis-IN-3

Ferroptosis Apoptosis
Ferroptosis-IN-3(Compound 25)是一款抑制RSL3引起的铁死亡(HT-1080细胞中EC50为8.6nM)的铁死亡抑制剂。此外,Ferroptosis-IN-3能有效清除DPPH和ABTS自由基(EC50分别为3.94μM与6.3μM),并且能降低脂质过氧化水平。
T82767 CC-3060

CC-3060为Cereblon调节剂,专门促进ZBTB16蛋白的降解。在HT-1080细胞中,CC-3060的ZBTB16降解半数有效浓度(DC50)为0.47 nM。其主要机制是通过针对ZBTB16上的不同锌指结构域的异构结构实现靶向降解。
T83780 GPX4 24

Phospholipid Hydroperoxide Glutathione Peroxidase 24,PHGPx 24,Glutathione Peroxidase 4 24

GPX4 24是(1S,3R)-RSL3的衍生物,具有抑制谷胱甘肽过氧化物酶4(GPX4)的作用。它能够在浓度依赖的方式中与4T1小鼠乳腺癌细胞中的GPX4形成共价结合。在GPX4依赖的HT-1080成纤维细胞中,GPX4 24诱导铁死亡(EC50 = 0.16 µM)。当以200 mg/kg剂量给予小鼠时,它能够增加小鼠肾脏和血浆中丙二醛(MDA)的水平。
T83886 icFSP1 TFA

icFSP1是一种抑制剂,针对的是铁死亡抑制蛋白1(FSP1)。在2.5 µM的浓度下使用时,能够引发FSP1在细胞中的凝聚和相分离,但在无细胞测试中并不抑制FSP1的酶活性(IC50 = > 30 µM)。icFSP1以浓度依赖的方式诱导HT-1080纤维肉瘤细胞的铁死亡。在体内,icFSP1(50 mg/kg)通过使用人类过表达FSP1,Gpx4-/-Fsp1-/-的B16/F10细胞,在B16/F10鼠黑色素瘤模型中减少肿瘤体积和重量。

化合物

SRS11-92
Cat.No: T8922
Synonym: AA9
Target: Ferroptosis
5'-Fluoroindirubinoxime
Cat.No: T8317
Synonym: 5'-FIO
Target: FLT
Ferrostatin-1
Cat.No: T6500
Synonym: Ferrostatin 1,Ferrostatin-1 (Fer-1)
Target: Ferroptosis, Antifungal
CIL56
Cat.No: T4309
Synonym: CA3
Target: Ferroptosis, ROS
Ridaforolimus
Cat.No: T6334
Synonym: AP23573,Deforolimus,MK-8669
Target: mTOR, Autophagy
PRLX-93936
Cat.No: T36404
Synonym:
Target:
DAT-230
Cat.No: T70527
Synonym:
Target:
Paclitaxel octadecanedioate
Cat.No: T36398
Synonym:
Target:
GSK321
Cat.No: T32009
Synonym: GSK 321,GSK-321
Target:
Erastin2
Cat.No: T35994
Synonym: Erastin2
Target:
Ferroptosis-IN-3
Cat.No: T82408
Synonym:
Target: Ferroptosis
CC-3060
Cat.No: T82767
Synonym:
Target:
GPX4 24
Cat.No: T83780
Synonym: Phospholipid Hydroperoxide Glutathione Peroxidase 24,PHGPx 24,Glutathione Peroxidase 4 24
Target:
icFSP1 TFA
Cat.No: T83886
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T64343 3-Methylcarbazole

NSC 10154

Others Others
3-Methylcarbazole (NSC-10154) 是具有抗癌作用的咔唑生物碱化合物。3-Methylcarbazole 对人纤维肉瘤 HT-1080 细胞具有生长抑制活性 (IC50 为 25 μg/mL)。
TN3854 Dihydroniloticin

Others Others
Dihydroniloticin shows cytotoxic activity against a HT-1080 human fibrosarcoma cell line( IC50 = 8.2 microM).
TN3307 9,10-Dimethoxycanthin-6-one

Others Others
9,10-Dimethoxycanthin-6-one shows cytotoxic activity against a HT-1080 human fibrosarcoma cell line( IC50 = 5.0 microM).
TN3571 Calyxin B

Others Others
Calyxin B exhibits potent activity against human HT-1080 fibrosarcoma cells with an ED50 value of 0.69 microM. A methylated product of calyxin A and an epimeric mixture of Calyxin B, showed greatly reduced activity suggesting that phenolic hydroxyl groups

天然产物

3-Methylcarbazole
Cat.No: T64343
Synonym: NSC 10154
Target: Others
Dihydroniloticin
Cat.No: TN3854
Synonym:
Target: Others
9,10-Dimethoxycanthin-6-one
Cat.No: TN3307
Synonym:
Target: Others
Calyxin B
Cat.No: TN3571
Synonym:
Target: Others
TargetMol Loading
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