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CAS:675576-98-4|Nutlin-3a
作者：德尔塔 日期：2022-03-14
产品名称 Nutlin-3a 英文名称 Nutlin-3a 规格或纯度 ≥97% 别名 (-)-Nutlin-3;2-Piperazinone, 4-[[(4S,5R)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]- 英文别名 (-)-Nutlin-3;2-Piperazinone, 4-[[(4S,5R)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]- 运输条件 超低温冰袋运输 生化机理 Nutlin-3 is MDM2 antagonist. Nutlin-3 inhibits the MDM2-p53 interaction (IC50 = 0.09 μM) and activates p53. Antiproliferative agent;chemotherapeutic agent; induces apoptosis in cancer cell
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CAS:71555-25-4|NSC 319726
作者：德尔塔 日期：2022-03-14
产品名称 NSC 319726 英文名称 NSC 319726 规格或纯度 ≥95% 别名 NSC-319726 英文别名 NSC-319726；1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide；[1-(2-Pyridinyl)ethylidene]hydrazide 1-Azetidinecarbothioic Acid 运输条件 超低温冰袋运输 生化机理 NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells, shows 10- to 100-fold selectivity over the other hotspot p53 mutants. NSC319276 induces p53(R175)-m
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CAS:548472-68-0|Nutlin-3
作者：德尔塔 日期：2022-03-14
产品名称 Nutlin-3 英文名称 Nutlin-3 应用 Disrupts MDM2-p53 interaction, inducing apoptosis. 规格或纯度 ≥98% 别名 Nutlin 3;Nutlin3;4-[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one; 英文别名 Nutlin 3;Nutlin3;4-[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one; 运输条件 超低温冰袋运输 生化机理
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CAS:675576-97-3|Nutlin-3b
作者：德尔塔 日期：2022-03-14
产品名称 Nutlin-3b 英文名称 Nutlin-3b 规格或纯度 ≥98% 别名 Nutlin 3b 英文别名 Nutlin 3b;4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one ；(+)-Nutlin-3 运输条件 超低温冰袋运输 生化机理 Nutlin-3b is a 150-fold less potent (+)-enantiomer of Nutlin-3 as p53 MDM2 antagonist or inhibitor, in comparison with more potent opposite (-)-enantiomer Nutlin-3a. It is useful as a negative control for non-Mdm2 related cellular activities.CAS编号 675576-97-3
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CAS:114899-77-3|Trabectedin
作者：德尔塔 日期：2022-03-14
产品名称 Trabectedin 英文名称 Trabectedin 生化机理 Description:IC50 Value: 0.1-3.7 nM(breast cancer cell lines) [1]Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.in vitro: Trabectedin induced cytotoxicity and apoptosis in both breast cancer cells in a time and concentration-dependent manner. The expression levels of the death receptor pathway molecules, TRAIL-R1/DR4, TRAIL-R2/DR5, FAS/TNFRSF6, TNF RI/TNFRSF1A, and FADD were significantly increased by 2.6-, 3.1-, 1.7-, 11.2- and 4.0-fold by trabectedin treatment in MCF-7 cells. However, in MDA-MB-453 cells, the mitochondrial pathway related pro-apoptotic proteins Bax, Bad, Cytochrome c, Smac/DIABLO, and Cleaved Caspase-3 expressions were induced by 4.2-, 3.6-, 4.8-, 4.5-, and 4.4-fold, and the expression levels of anti-apoptotic proteins Bcl-2 and Bcl-XL were reduced by 4.8- and 5.2-fold in MDA-MB-453 cells [2]. In vitro treatment with noncytotoxic concentrations of trabectedin selectively inhibited the production of CCL2, CXCL8, IL-6, VEGF, and PTX3 by MLS primary tumor cultures and/or cell lines [3].in vivo: A xenograft mouse model of human MLS showed marked redu
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CAS:877877-35-5|TW-37
作者：德尔塔 日期：2022-03-14
产品名称 TW-37 英文名称 TW-37 规格或纯度 ≥99% 别名 5-(2-isopropylbenzyl)-N-(4-(2-tert-butylphenylsulfonyl)phenyl)-2,3,4-trihydroxybenzamide 英文别名 5-(2-isopropylbenzyl)-N-(4-(2-tert-butylphenylsulfonyl)phenyl)-2,3,4-trihydroxybenzamide 运输条件 超低温冰袋运输 生化机理 TW-37 is Bcl-2 inhibitor (Ki values are 0.29 μM and 1.11 μM for Bcl-2 and Bcl-XL respectively). TW-37 inhibits the angiogenic potential of endothelial cells in vitro. TW-37 induces S-phase arrest and apoptosis in pancreatic cancer cell lines;
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CAS:204005-46-9|塞马西尼
作者：德尔塔 日期：2022-03-14
产品名称 塞马西尼 英文名称 SU5416 应用 It was used to study the mechanism of development of cerebral vasculature in zebrafish hindbrain，and study the pulmonary vascular remodeling in response to hypoxia in mouse model of pulmonary arterial hypertension. 规格或纯度 ≥98% (HPLC) 别名 SU-5416;SU5416 英文别名 Semaxinib;SU-5416;VEGFR2 Kinase Inhibitor III; 1,3-Dihydro-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylene]-2H-indol-2-one 运输条件 超低温冰袋运输 生化机理
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CAS:143360-00-3|SMIP004
作者：德尔塔 日期：2022-03-14
产品名称 SMIP004 英文名称 SMIP004 规格或纯度 ≥98% 生化机理 Description:IC50 Value: 1.09 uM (MTT assay in LNCaP-S14 cells) [1]SMIP004 (N-(4-butyl-2-methyl-phenyl) acetamide) is a novel inducer of cancer-cell selective apoptosis of human prostate cancer cells. Unlike SMIP001, SMIP004 was found to downregulate SKP2 and to stabilize p27, although neither SMIP is a proteasome inhibitor.in vitro: Whereas SMIP012 and 016 were moderately toxic in normal fibroblasts, SMIPs 001 and 004 showed substantial cancer cell specificity being at least five times more potent in LNCaP-S14 than in IMR90 cells , treatment with either MG132 or SMIP004 increased p27 half-life to > 6 h [1]. Both SMIP001 and 004 led to a strong increase in the recruitment of p27 to CDK2, while SMIP001 also slightly increased coprecipitation of p21 (Figure 6c). SMIP004 also reduced the amounts of cyclins E and A retrieved with CDK2. This was paralleled by a marked downregulation of cyclins E and A upon SMIP004 treatment. SMIP004 decreased the levels of positive cell cycle regulators, upregulate
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CAS:1096687-52-3|SPK-601
作者：德尔塔 日期：2022-03-14
产品名称 SPK-601 英文名称 SPK-601 规格或纯度 ≥98% 生化机理 SPK-601 is useful for viral diseases.CAS编号 1096687-52-3 溶解性 DMSO 储存温度 储存温度-20°C
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CAS:882531-87-5|R1530
作者：德尔塔 日期：2022-03-14
产品名称 R1530 英文名称 R1530 规格或纯度 ≥98.0% 别名 R 1530;R-1530;5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine 英文别名 R 1530;R-1530;5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine 运输条件 冰袋运输 生化机理 多激酶抑制剂。表现出对Chk2，KDR，FGFR，Aurora A激酶和Cdk2的抑制活性（IC50分别为24、34、50、58和88 nM）。还结合VEGFR-2，FGFR1和PDGFRβ（Kd值分别为0.015、0.061和0.088μM）。在体外显示抗增殖活性；抑制有丝分裂和血管生成。口服具有生物活性。CAS编号 88253
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CAS:939981-39-2|RG7112
作者：德尔塔 日期：2022-03-14
产品名称 RG7112 英文名称 RG7112 规格或纯度 ≥98% 运输条件 超低温冰袋运输 生化机理 Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment. RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.Potent, orally bioavailable MDM2 inhibitor that displays antineoplastic activity. Nutlin imidazoline compound. RG-7112 binds to MDM2, thereby preventing the binding of the MDM2 protein to the transcriptional activation domain of the tumor suppressor proteCAS编号 939981-39-2
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CAS:781661-94-7|YM155 (Sepantronium Bromide)
作者：德尔塔 日期：2022-03-14
产品名称 YM155 (Sepantronium Bromide) 英文名称 YM155 (Sepantronium Bromide) 应用 An inhibitor of survivin expression and apoptosis inducer. 规格或纯度 ≥98% 别名 YM-155 英文别名 YM155; Sepantronium bromide;YM 155;YM-155;1H-Naphth[2,3-d]imidazolium, 4,9-dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-, bromide;4,9-Dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-1H-naphth[2,3-d]imidazolium br 运输条件 超低温冰袋运输 生
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CAS:1431866-33-9|WEHI-539
作者：德尔塔 日期：2022-03-14
产品名称 WEHI-539 英文名称 WEHI-539 生化机理 Description:IC50 Value: 1.1 nM (BCL-XL) [1]The prosurvival BCL-2 family protein BCL-XL is often overexpressed in solid tumors and renders malignant tumor cells resistant to anticancer therapeutics. The optimized compound, WEHI-539, has high affinity (subnanomolar) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity.WEHI-539 has a high affinity for BCL-XL (IC50 = 1.1 nM). WEHI-539 interacts with residues in the P4 pocket and adopts a distinct binding mode compared to ABT-737. WEHI-539 induces apoptosis in MEFs only if they lack MCL-1 supports the notion that cell killing induced by WEHI-539 is due to direct inhibition of BCL-XL. Accordingly, restoring expression of MCL-1 in mcl-1 knockout cells renders them highly resistant to WEHI-539. WEHI-539 could only kill cells that contained BAK (Fig. 6b). This observation was confirmed in MEFs where both the amount and activity of MCL-1 were abrogated by expression of its natural and selective BH3-only ligand NOXA. Cytochrome c release and caspase-3 processing confirmed that WEHI-539 induces apoptosis in BAX-deficient MEF cells expressing BIM2A but not in their BAK-deficien
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CAS:1260251-31-7|Birinapant
作者：德尔塔 日期：2022-03-14
产品名称 Birinapant 英文名称 Birinapant 规格或纯度 98% 别名 Propanamide, N,N'-[(6,6'-difluoro[2,2'-bi-1H-indole]-3,3'-diyl)bis[methylene[(2R,4S)-4-hydroxy-2,1-pyrrolidinediyl][(1S)-1-ethyl-2-oxo-2,1-ethanediyl]]]bis[2-(methylamino)-, (2S,2'S)- 英文别名 Propanamide, N,N'-[(6,6'-difluoro[2,2'-bi-1H-indole]-3,3'-diyl)bis[methylene[(2R,4S)-4-hydroxy-2,1-pyrrolidinediyl][(1S)-1-ethyl-2-oxo-2,1-ethanediyl]]]bis[2-(methylamino)-, (2S,2'S)- 运输条件 超低温冰袋运输 生化机理 cIAP1（Kd
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CAS:331244-89-4|BAM7
作者：德尔塔 日期：2022-03-14
产品名称 BAM7 英文名称 BAM7 规格或纯度 ≥99% 别名 3-甲基-1-(4-苯基-2-噻唑基)-1H-吡唑-4,5-二酮 4-[2-(2-乙氧基苯基)腙] 英文别名 BAM 7;BAM-7；4-(2-(2-Ethoxyphenyl)hydrazono)-3-methyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one；BAX activator molecule 7 运输条件 超低温冰袋运输 生化机理 Bax激活剂（EC50 =3.3μM）; 在BH3结合位点结合。对Bax的选择性高于其他抗凋亡蛋白和促凋亡蛋白。在体外触发Bax低聚；诱导小鼠胚胎成纤维细胞中Bax介导的凋亡。CAS编号 331244-89-4
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