25
6
2
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,BW1370U87,1370U87,1370U 87,BW 1370U87 |
MAO | Metabolism; Neuroscience |
BW-1370U87 是一种可逆的竞争性单胺氧化酶-A抑制剂,可用于研究抑郁症和其他中枢神经系统疾病。 | |||
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
|
Others | Others |
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。 | |||
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。 | |||
T63624 |
Exatecan-amide-cyclopropanol
|
Others; ADC Cytotoxin | Antibody-drug Conjugate/ADC Related; Others |
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。 | |||
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。 | |||
T70890 |
ML309
|
Others | Others |
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. | |||
T74536 |
IDO/Tubulin-IN-2
|
Others | Others |
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。 | |||
T38004 |
ML-309 (hydrochloride)
|
Others | Others |
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). | |||
T78773 |
Tubulin inhibitor 38
|
Others | Others |
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。 | |||
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。 | |||
T62060 |
NF-κB-IN-5
|
Others | Others |
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
|
Others | Others |
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
|
Others | Others |
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. | |||
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。 | |||
T71261 |
Arsthinol
|
Others | Others |
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... | |||
T36241 |
Arecaidine propargyl ester (hydrobromide)
|
Others | Others |
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。 |
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIJ-0518 |
L-Kynurenine-d4-1
|
||
L-Kynurenine-d4-1 是 L-Kynurenine 的氘代化合物。L-Kynurenine 的 CAS 号为 2922-83-0。L-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。 | |||
TMID-0071 |
L-Kynurenine-d4
|
||
L-Kynurenine-d4 是 L-Kynurenine 的氘代化合物。L-Kynurenine 的 CAS 号为 2922-83-0。L-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。 |