15
1
Cat. No. | Product Name | Target | Signaling Pathways |
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T36758 |
CAIX Inhibitor S4
S4 |
Carbonic Anhydrase | Metabolism |
CAIX Inhibitor S4 (S4) 是一种有效的碳酸酐酶 IX/XII 抑制剂,Ki 分别为 7 nM 和 2 nM。 CA II 和 CA I 的 Ki 分别为 546 和 5600 nM。 | |||
T21294 |
Polmacoxib
CG-100649,帕马考昔,CG100649,CG 100649 |
COX; Carbonic Anhydrase | Immunology/Inflammation; Metabolism; Neuroscience |
Polmacoxib (CG 100649) 是一流的 NSAID 候选药物,是碳酸酐酶 (CA) 和 COX-2 的双重抑制剂。它在小鼠模型中抑制大肠腺瘤和肿瘤生长。 | |||
T24997 |
ABT-510 acetate
ABT 510 acetate |
Apoptosis | Apoptosis |
ABT-510 acetate 是一种内源性抗血管生成的 TSP 肽抑制剂,是一种凝血酶原类似物,具有抗炎抗癌和抗血管生成活性,能诱导肿瘤细胞凋亡并抑制上皮性卵巢癌正位、同种异体模型中的卵巢肿瘤生长。ABT-510 acetate 可减少小鼠炎症性肠病模型的血管生成和炎症反应,可用于癌症 (尤其是上皮性卵巢癌) 以及炎症性肠病 (IBD) 的研究。 | |||
T60202 |
MMRi62
7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol |
Ferroptosis | Apoptosis |
MMRi62 (7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol) 是一种铁死亡 (ferroptosis) 诱导剂,靶向 MDM2-MDM4 (抑癌基因 p53 负调控因子)。MMRi62 对胰腺导管腺癌 (PDAC) 细胞显示出 p53 独立的促凋亡 (apoptosis) 活性,并诱导其自噬 (autophagy)。MMRi62 诱导铁死亡,伴随着活性氧增加和铁蛋白重链 (FTH1) 溶酶体降解。MMRi62 还可导致突变型 p53 的蛋白酶体降解,并对具有 KRAS 和 TP53 高频突变特征的原位异种移植 PDAC 小鼠模型具有体内药效。 | |||
T24598 |
BrBzGCp2
p BrBzGSH(Cp)2,BBGC,pBrBzGSH(Cp)2,p-BrBzGSH(Cp)2,BBGD |
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p-BrBzGSH(Cp)2 is a glyoxylase 1 inhibitor. In orthotopic mouse models, it acts by increasing DNA-AGEs, stimulating RAGE expression, and inhibiting brain tumor growth. | |||
T79408 |
KGP591
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KGP591为微管蛋白聚合抑制剂(IC50 0.57µM),能显著诱导MDA-MB-231细胞G2/M停滞,同时抑制细胞迁移,破坏微管结构及细胞形态。在RENCA原位肾癌模型中,KGP591展现了抗肿瘤活性。 | |||
T81574 | PAA4 | ||
PAA4为含中心甲基化物碳的多核Au(I)簇,具有抗增殖活性。PAA4能时间依赖性地提升pH2AX表达,并在原位膀胱癌小鼠模型中展现抗肿瘤效果。 | |||
T70345 | JAS239 | ||
JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly. JAS239 attenuated choline phosphorylation and viability in a panel of human breast cancer cell lines. Antibody blockade prevented cellular retention of JAS239 indicating direct interaction with ChoKα independent of the choline transporters and catabolic choline pathways. In mice bearing orthotopic MCF7 breast xenografts, optical imaging with JAS239 distinguished tumors overexpressing C... | |||
T83912 |
HR68
PP21 |
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HR68是一种抗癌化合物,是过氧化物酶体增殖物激活受体(PPAR)激动剂非诺贝酯的衍生物。它能降低LN-229胶质母细胞瘤细胞的存活率(IC50 = 1.17 µM)。HR68能够穿越血脑屏障,在对替莫唑胺耐药的原位患者衍生的异种移植(PDX)小鼠胶质母细胞瘤模型中发挥作用。 | |||
T69898 | NG25 trihydrochloride | ||
NG25 trihydrochloride is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration... | |||
T75941 |
Foxy-5 TFA
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Foxy-5 TFA 是WNT5A 激动剂,是 WNT5A 的一个模拟肽,是Wnt 家族的非经典成员。Foxy-5 TFA 可在不影响β-catenin 激活的情况下触发胞浆游离钙信号传导,并可抑制上皮癌细胞的迁移和侵袭。Foxy-5 TFA 在原位小鼠模型中能有效降低 WNT5A 低表达的前列腺癌细胞的转移扩散。 | |||
T36195 |
CAY10744
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CAY10744 is a topoisomerase II-α poison.1 It inhibits topoisomerase II-α by 78.9% when used at a concentration of 20 μM. CAY10744 is selective for topoisomerase II-α over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 μM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 μM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 μM. CAY1074... | |||
T36779 |
NG 25 (hydrochloride hydrate)
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NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv... | |||
T83777 |
LAU-0901
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LAU-0901是一种血小板活化因子(PAF)受体拮抗剂。在体内,LAU-0901(30、60及90 mg/kg)通过减少梗塞体积和改善大鼠由中脑动脉阻塞(MCAO)引起的脑缺血模型中的神经功能来发挥作用。它还能减少同一模型中的小胶质细胞浸润,并增加星形胶质细胞和神经元的存活率。单独使用LAU-0901(30 mg/kg)或与阿托伐他汀联合使用,能减少U87MG胶质母细胞瘤小鼠原位肿瘤模型中的肿瘤生长。 | |||
T83911 |
CYY292
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CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T16332 |
NKH477
Colforsin dapropate hydrochloride |
NMDAR | Neuroscience |
NKH477 is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 shows an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute |