上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
CAY10603 (Synonyms: BML-281) 纯度: 99.62%
CAY10603 (BML-281) 是一种有效的,选择性的 HDAC6 抑制剂,IC50 值为 2 pM;CAY10603 (BML-281) 同时可抑制 HDAC1,HDAC2,HDAC3,HDAC8 和 HDAC10 的活性,IC50 值分别为 271,252,0.42,6851,90.7 nM。
CAY10603 Chemical Structure
CAS No. : 1045792-66-2
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥1081 | In-stock | |
5 mg | ¥1100 | In-stock | |
10 mg | ¥1800 | In-stock | |
25 mg | ¥3500 | In-stock | |
50 mg | ¥5500 | In-stock | |
100 mg | ¥8000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
CAY10603 相关产品
•相关化合物库:
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- Oxygen Sensing Compound Library
- Anti-Breast Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
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生物活性 |
CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
CAY10603 (Compound 7) shows potent inhibitory activities against pancreatic cancer cell lines, with IC50s of 1, 0.3, 0.1, 0.1, 0.6, <1, 0.5 μM for BxPC-3, HupT3, Mia Paca-2, Panc 04.03, SU.86.86, HMEC, HPDE6c7, respectively. CAY10603 (100 nM, 200-300 nM) is active against both the Mia Paca-2 and Panc04.03 cell lines[1]. CAY10603 inhibits HDAC6 deacetylase activity, and supresses the proliferation of lung adenocarcinoma cells. CAY10603 also induces apoptosis of lung adenocarcinoma cells. Furthermore, CAY10603 synergizes with gefitinib to induce apoptosis in lung adenocarcinoma cell lines, partly through the destabilization of EGFR and inactivation of the EGFR pathway[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
446.50 |
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Formula |
C22H30N4O6 |
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CAS 号 |
1045792-66-2 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 50 mg/mL (111.98 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Kinase Assay [1] |
Purified HDACs are incubated with 1 mm carboxyfluorescein (FAM)-labeled acetylated peptide substrate and test compound for 17 h at 25°C in HDAC assay buffer containing 100 mm HEPES (pH 7.5), 25 mm KCl, 0.1% BSA, and 0.01% Triton X-100. Reactions are terminated by the addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05%. Substrate and product are separated electrophoretically using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2). The fluorescence intensity in the substrate and product peaks is determined using the Well Analyzer software on the Caliper system. The reactions are performed in duplicate for each sample. IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the XLFit 4-Parameter Logistic Model (sigmoidal dose-response model): ((A+ ((B_A)/1+((C/x)D)))), in which x is compound concentration, A and B are respectively the estimated minimum and maximum of percent inhibition, C is the inflection point, and D is the Hill slope of the sigmoidal curve. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Cell Assay [1] |
The pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 are obtained from ATCC and are grown in medium (DMEM or RPMI) containing 10% fetal calf serum and l-glutamine. Pancreatic cancer cells are plated out in duplicate into 6 wells of a 96-well microtiter plate at 2.5-4P103 cells per well. Four hours post plating, individual wells are treated with diluent (DMSO) or varying concentrations of SAHA or the indicated HDACIs from a concentration of 1 nm to 50 mm. Cytotoxicity is measured at time “0”, and 72 h post treatment using the colorimetric MTT assay. The IC50 values are calculated using XLfit. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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