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25

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T2430 HPOB

Apoptosis; HDAC Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
HPOB 是一种高选择性HDAC6抑制剂,IC50为 56 nM,其选择性是其他 HDAC 的 30 倍以上。它提高 DNA 损伤抗癌药物在转化细胞中的有效性。
T5622 BAY-218

AHR antagonist 1

AhR; Aryl Hydrocarbon Receptor Immunology/Inflammation; Metabolism
BAY-218 (AHR antagonist 1) 是一种芳基烃受体(AHR)拮抗剂,在人细胞系中的IC50值为 39.9 nM。
T6920 ON123300

FGFR; c-RET; JAK; CDK; PDGFR; Src; AMPK Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
ON123300 是一种可透过血脑屏障的多激酶抑制剂,作用于 CDK4、CDK6、Ark5、PDGFRβ、FGFR1、RET 和 Fyn,IC50值为3.9、9.82、5、26、26、9.2和11 nM。它在脑肿瘤中抑制 Akt 磷酸化及激活 Erk。
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。
T26930 BW-1370U87

1370U 87,1370U-87,1370U87,BW 1370U87

BW-1370U87 is a monoamine oxidase A (MAO-A) inhibitor. BW-1370U87 elevates neurotransmitter amines in the brain over the same dose range at which it exhibits positive activities in animal models of depressive illness. BW-1370U87's mechanism of action foll
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。
T3213 Hematoporphyrin dihydrochloride

血卟啉二盐酸盐,Hematoporphyrin IX dihydrochloride

Apoptosis; Others; Endogenous Metabolite Apoptosis; Metabolism; Others
Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride) 是一种光敏剂,是血红素结合蛋白亲和色谱底物。它暴露在红光下时,可诱导 U87 胶质瘤细胞凋亡,并降低体内肿瘤的生长。
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.
T63624 Exatecan-amide-cyclopropanol

Exatecan-amide-cyclopropanol 是一种抗癌剂,能够抑制 SK-BR-3 细胞 (IC50: 0.12 nM) 和 U87 细胞 (IC50: 0.23 nM)的增殖。
T79530 SA-PA

PROTACs PROTAC
SA-PA是一种细胞内自组装PROTAC,以叠氮化物和炔烃为基础。它在U87细胞中可选择性降解VEGFR-2、PDGFR-β和EphB4蛋白,并可利用肿瘤组织中的内源性铜通过点击化学反应转化为PROTAC。
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).
T78862 EGFR-IN-86

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
EGFR-IN-86(化合物4i)是一种高效的EGFR抑制剂,IC50为1.5 nM,对胶质母细胞瘤表现出强抗癌活性。该化合物能够诱导细胞凋亡并使U87细胞周期在G2/M期发生阻滞。
T74536 IDO/Tubulin-IN-2

IDO/Tubulin-IN-2 (HT2) 是一种对TDO和微管蛋白 (tubulin)展现出高效抑制作用的化合物。该抑制剂对多种癌细胞系(包括U87、HepG2、A549、HCT-116和LO2)均表现出强抗肿瘤活性,其半抑制浓度(IC50)分别为0.43、0.036、0.041、0.095和1.04 μM,有效提升了抗肿瘤效果。
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。
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。
T79531 SA-VA

PROTACs PROTAC
SA-VA是一种细胞内自组装PROTAC,采用叠氮化物和炔烃基团。它能选择性地在U87细胞中降解VEGFR-2与EphB4蛋白,并可利用肿瘤组织的内源性铜促成点击反应生成PROTAC。此外,SA-VA能够促进(apoptosis)并干预S期细胞周期。
T69438 MT477

MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays.
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...
T83709 LIH383 TFA

Phe-Gly-Gly-Phe-Met-Arg-Arg-Lys-NH2

LIH383是一种趋化因子(C-X-C motif) 受体7 (CXCR7)的多肽激动剂,属于趋化因子和阿片肽清除受体。它专一性激活CXCR7 (EC50 = 0.61 nM),在3 µM浓度时,相比μ-、δ-、κ-阿片受体以及诺氨酸阿片肽(NOP)受体的β-arrestin招募实验中表现出高选择性。LIH383(3 µM)通过阻止U87-ACKR3细胞中,由非选择性阿片受体激动剂dynorphin A诱导的CXCR7对阿片肽的摄取,发挥作用。
T36241 Arecaidine propargyl ester (hydrobromide)

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecai...
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

HPOB
Cat.No: T2430
Synonym:
Target: Apoptosis, HDAC
BAY-218
Cat.No: T5622
Synonym: AHR antagonist 1
Target: AhR, Aryl Hydrocarbon Receptor
ON123300
Cat.No: T6920
Synonym:
Target: FGFR, c-RET, JAK, CDK, PDGFR, Src, AMPK
Sertindole
Cat.No: T5858
Synonym: Lu 23-174,舍吲哚
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy
BW-1370U87
Cat.No: T26930
Synonym: 1370U 87,1370U-87,1370U87,BW 1370U87
Target:
ML-298
Cat.No: T8966
Synonym: ML298,CID53393915
Target: Phospholipase
Hematoporphyrin dihydrochloride
Cat.No: T3213
Synonym: 血卟啉二盐酸盐,Hematoporphyrin IX dihydrochloride
Target: Apoptosis, Others, Endogenous Metabolite
Sec61-IN-4
Cat.No: T81184
Synonym:
Target:
PI3Kα-IN-12
Cat.No: T78804
Synonym:
Target: PI3K
ML309
Cat.No: T70890
Synonym:
Target:
Exatecan-amide-cyclopropanol
Cat.No: T63624
Synonym:
Target:
SA-PA
Cat.No: T79530
Synonym:
Target: PROTACs
PI3Kα-IN-14
Cat.No: T81469
Synonym:
Target: PI3K
ML-309 (hydrochloride)
Cat.No: T38004
Synonym:
Target:
EGFR-IN-86
Cat.No: T78862
Synonym:
Target: EGFR
IDO/Tubulin-IN-2
Cat.No: T74536
Synonym:
Target:
Tubulin inhibitor 38
Cat.No: T78773
Synonym:
Target:
NF-κB-IN-5
Cat.No: T62060
Synonym:
Target:
SA-VA
Cat.No: T79531
Synonym:
Target: PROTACs
MT477
Cat.No: T69438
Synonym:
Target:
K-TMZ
Cat.No: T36100
Synonym:
Target:
Arsthinol
Cat.No: T71261
Synonym:
Target:
LIH383 TFA
Cat.No: T83709
Synonym: Phe-Gly-Gly-Phe-Met-Arg-Arg-Lys-NH2
Target:
Arecaidine propargyl ester (hydrobromide)
Cat.No: T36241
Synonym:
Target:
ML299
Cat.No: T8968
Synonym: VU0463568,ML-299
Target: Phospholipase
Cat. No. Product Name Target Signaling Pathways
T5784 Topotecan

NSC 609669,拓扑替康,SKF 104864A

Topoisomerase; Autophagy Autophagy; DNA Damage/DNA Repair
Topotecan (NSC-609669) 是一种拓扑异构酶 I 抑制剂,通过抑制 DNA 拓扑异构酶起抗肿瘤作用,可用于治疗卵巢癌。
T5429 Theaflavin 3,3'-digallate

茶黄素-3,3'-双没食子酸,8-Gingerol,TFDG

Virus Protease; Antioxidant; HIV Protease; HSV Microbiology/Virology; oxidation-reduction; Proteases/Proteasome
Theaflavin 3,3'-digallate (8-Gingerol) 是一种寨卡病毒蛋白酶抑制剂,IC50为 2.3 μM。它直接与 ZIKVpro 结合并抑制 ZIKV 复制,可抑制 gp41 和 NS2B-3 蛋白酶的活性,并具有抗 HSV 和 HIV-1病毒活性。它是红茶中的主要多酚,有抗肿瘤作用。
T4928 L-Kynurenine

L-犬尿氨酸,(S)-Kynurenine

AhR; Aryl Hydrocarbon Receptor; Endogenous Metabolite Immunology/Inflammation; Metabolism
L-Kynurenine ((S)-Kynurenine) 是L-色氨酸的代谢物,是芳香烃受体激动剂,可抑制同种异体 T 细胞增殖并增加恶性 U87 神经胶质瘤细胞侵入胶原基质。
T8190 5-Hydroxyflavone

Others Others
5-Hydroxyflavone 是类黄酮配体,对 FaDU,MCF-7,U87,MDA-MB-435S,RPE-1 和 HEK293 细胞没有细胞毒性。
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。
T83446 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide

15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2), 一种从冬凌草提取的ent-kaurene diterpenoid,显示了对多个细胞系的细胞毒性作用。具体而言,其对EC-1、U87、A549、MCF-7 和 Hela 细胞系的IC50值分别为37.69 μM、79.362 μM、80.07 μM、197.35 μM、462.13 μM 和180.09 μM。

天然产物

Topotecan
Cat.No: T5784
Synonym: NSC 609669,拓扑替康,SKF 104864A
Target: Topoisomerase, Autophagy
Theaflavin 3,3'-digallate
Cat.No: T5429
Synonym: 茶黄素-3,3'-双没食子酸,8-Gingerol,TFDG
Target: Virus Protease, Antioxidant, HIV Protease, HSV
L-Kynurenine
Cat.No: T4928
Synonym: L-犬尿氨酸,(S)-Kynurenine
Target: AhR, Aryl Hydrocarbon Receptor, Endogenous Metabolite
5-Hydroxyflavone
Cat.No: T8190
Synonym:
Target: Others
Ellipticine
Cat.No: T1166
Synonym: 玫瑰树碱,NSC 71795,Elliptisine
Target: Topoisomerase
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide
Cat.No: T83446
Synonym:
Target:
TargetMol Loading
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