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14

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9880 ZINC05007751

MAPK MAPK
ZINC05007751 是 NIMA 相关激酶 NEK6 的有效抑制剂(IC50 = 3.4 μM)。 ZINC05007751 对 NEK1 和 NEK6 具有很强的特异性,对 NEK2、NEK7 和 NEK9 没有显着的活性。
TQ0059 Ilorasertib

ABT-348

VEGFR; FLT; c-RET; PDGFR; Aurora Kinase Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
Ilorasertib (ABT-348) 是一种 ATP 竞争性多靶点激酶抑制剂,可抑制 Aurora A、Aurora B 和Aurora C,IC50值为120 nM、7 nM 和1 nM。它还抑制 RET 酪氨酸激酶、PDGFRβ 和 Flt1,IC50为7 nM、3 nM 和 32 nM。
T13017 STL127705

Compound L,7-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione

DNA-PK; Others DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling
STL127705 (Compound L) 是一种有效的 Ku 70/80 异二聚体蛋白抑制剂,抑制 Ku70/80-DNA 相互作用,IC50 为 3.5 μM。 它抑制 Ku 依赖性 DNA-PKCS 激酶的激活,IC50 为 2.5 μM。
T36493 CMLD-2

Apoptosis; HuR Apoptosis; Chromatin/Epigenetic
CMLD-2是一种 HuR-ARE 相互作用的抑制剂(Ki:350 nM),能竞争性地结合 HuR 蛋白并破坏其与富含腺嘌呤元素(ARE)的 mRNA 目标的相互作用。CMLD-2诱导细胞凋亡并通过 MAD2下调表现出抗肿瘤作用。CMLD-2 (1-75 μM ; 24-72 h) 对甲状腺癌细胞的活力具有抑制作用.CMLD-2 (20-30 μM ; 24-48 h) 激活 Caspases 并诱导H1299和A549细胞凋亡.CMLD-2 (30 μM ; 24-48 h) 诱导H1299和A549细胞的G1细胞周期停止和线粒体扰动。 CMLD-2(30μM;24-48小时)减少H1299细胞中HuR 和HuR 调节的mRNAs 和蛋白质的表达.CMLD-2(35μM;72小时)降低SW1736、8505C、BCPAP 和K1细胞的定向迁移能力。CMLD-2诱导SW1736、8505C、BCPAP 和K1细胞中的MAD2 mRNA 水平强烈下降。
T7082 HDAC8-IN-1

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
HDAC8-IN-1 是一种 HDAC8 抑制剂,在癌细胞系中的 IC50 为 27.2 nM,有抗增殖作用。
T78156 MC4033

Apoptosis Apoptosis
MC4033是一种选择性的,可逆的KAT8赖氨酸乙酰转移酶抑制剂,IC50为12.1μM,具有抗癌活性,并能诱导凋亡(apoptosisautophagy)。
T19661 8-Chloroadenosine

NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷

AMPK Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
8-Chloroadenosine (NSC-354258) 是一种 5' AMP 激活的蛋白激酶激动剂,可能用于治疗慢性淋巴细胞白血病。 它的活性与 mTOR 通路的抑制有关。它是一种核苷类似物。在体内代谢为 8-氯-ATP。在转录过程中掺入 RNA 并抑制 RNA 合成。在 MM.1S、RPMI-8226 和 U266 癌细胞系中表现出细胞毒性;在 A549 和 H1299 细胞中诱导 G2/M 细胞周期停滞和有丝分裂灾难。它已被证明可消耗 ATP 并抑制血液恶性肿瘤以及肺癌和乳腺癌细胞系中的肿瘤生长。
T72525 Antitumor agent-48

Antitumor agent-48 是一种具有抗肿瘤活性的 2,3-dehydrosilybin 衍生物。Antitumor agent-48 对 MCF-7、NCI-H1299、HepG2 和 HT29 细胞具有细胞毒活性,IC50值分别为 8.06 µM、13.1 µM、16.51 µM 和 12.44 µM。
T36350 Cho-Arg (trifluoroacetate salt)

Cho-Arg is a steroid-based cationic lipid that contains a cholesterol skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratios greater than or equal to 4. Cho-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence or absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the cav...
T72524 Antitumor agent-47

Antitumor agent-47 是一种具有抗肿瘤活性的水飞蓟宾衍生物。Antitumor agent-47 对 NCI-H1299 和 HT29 细胞具有细胞毒活性,IC50值分别为 8.07 µM 和 6.27 µM。
T83011 Antitumor agent-105

Antitumor agent-105(Compound 37)是一种对A549、H1299、H460、HCT116、MDA-MB-231细胞线显示出抗肿瘤活性的化合物,其IC50值分别为6.7、8.3、4.3、4.4、6.7μM。
T36368 2H-Cho-Arg (trifluoroacetate salt)

2H-Cho-Arg is a steroid-based cationic lipid that contains a 2H-cholesterol skeleton coupled to an L-arginine head group and can be used to facilitate gene transfection. It forms a complex with plasmid DNA (pDNA) and decreases pDNA migration in an electrophoretic mobility shift assay at +/- charge ratios of 4 or higher. 2H-Cho-Arg facilitates transfection of a luciferase gene into H1299 cells, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and t...
T36359 Dios-Arg (trifluoroacetate salt)

Dios-Arg is a steroid-based cationic lipid that contains a diosgenin skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratio greater than or equal to 4. Dios-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence and absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the cav...
T35729 Nemadipine-A

Nemadipine A is an L-type calcium channel blocker that induces morphological and growth defects in wild-type C. elegans and those with hypoexpression of egl-19, which encodes the only L-type calcium channel α1-subunit in the C. elegans genome. It also inhibits L-type calcium channels in chick ciliary neurons. Nemadipine A increases TRAIL-induced cytotoxicity and synergistically enhances caspase-8 and caspase-3 activation in a concentration-dependent manner in H1299 lung adenocarcinoma cells. It ...

化合物

ZINC05007751
Cat.No: T9880
Synonym:
Target: MAPK
Ilorasertib
Cat.No: TQ0059
Synonym: ABT-348
Target: VEGFR, FLT, c-RET, PDGFR, Aurora Kinase
STL127705
Cat.No: T13017
Synonym: Compound L,7-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione
Target: DNA-PK, Others
CMLD-2
Cat.No: T36493
Synonym:
Target: Apoptosis, HuR
HDAC8-IN-1
Cat.No: T7082
Synonym:
Target: HDAC
MC4033
Cat.No: T78156
Synonym:
Target: Apoptosis
8-Chloroadenosine
Cat.No: T19661
Synonym: NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷
Target: AMPK
Antitumor agent-48
Cat.No: T72525
Synonym:
Target:
Cho-Arg (trifluoroacetate salt)
Cat.No: T36350
Synonym:
Target:
Antitumor agent-47
Cat.No: T72524
Synonym:
Target:
Antitumor agent-105
Cat.No: T83011
Synonym:
Target:
2H-Cho-Arg (trifluoroacetate salt)
Cat.No: T36368
Synonym:
Target:
Dios-Arg (trifluoroacetate salt)
Cat.No: T36359
Synonym:
Target:
Nemadipine-A
Cat.No: T35729
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1393 (-)-Anonaine

番荔枝碱

Apoptosis; Antioxidant; Parasite; Antifungal Apoptosis; Microbiology/Virology; oxidation-reduction
(-)-Anonaine 可从木兰科和安妮科的几个物种中提取出来,具有抗疟、抗菌、抗真菌、抗氧化、抗癌、抗抑郁和血管舒张的活性。(-)-Anonaine 通过 Bax 和 caspase 依赖性途径诱导人类宫颈癌(HeLa)细胞的凋亡,诱导 DNA 损伤并抑制人类肺癌 h1299细胞的生长和迁移。
T82429 Euphoheliosnoid A

Euphoheliosnoid A (Compound 24) 为二萜类化合物,以 2.5 μM 浓度显著提升 NK 细胞针对 H1299-luci 及 A549-luci 细胞的杀伤效率。
TN5440 Catechin-7-O-xyloside

Catechin 7-O-β-D-xylopyranoside

Others Others
Catechin-7-O-xyloside(C7Ox)具有抗癌活性,它通过内质网应激和线粒体功能障碍诱导人非小细胞肺癌H1299细胞凋亡。
T82427 Euphoscopin C

Euphoscopin C, 一种自Euphorbia helioscopia分离得到的二萜类化合物,可显著增强NK细胞对H1299-luci细胞和A549-luci细胞的杀伤活性。

天然产物

(-)-Anonaine
Cat.No: TN1393
Synonym: 番荔枝碱
Target: Apoptosis, Antioxidant, Parasite, Antifungal
Euphoheliosnoid A
Cat.No: T82429
Synonym:
Target:
Catechin-7-O-xyloside
Cat.No: TN5440
Synonym: Catechin 7-O-β-D-xylopyranoside
Target: Others
Euphoscopin C
Cat.No: T82427
Synonym:
Target:
TargetMol Loading
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