CAY10603

製品コードS7596 バッチS759601

印刷

化学情報

Synonyms

BML-281

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₃₀N₄O₆

分子量

446.5

CAS No.

1045792-66-2

Solubility (25°C)*

体外

DMSO

89 mg/mL (199.32 mM)

Ethanol (warmed with 50ºC water bath)

5 mg/mL (11.19 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 50%PEG300 2 45%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	9.000mg/ml (20.16mM)	Taking the 1 mL working solution as an example, add 50 μL of 180 mg/ml clarified DMSO stock solution to 500 μL of PEG 300, mix evenly to clarify it; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
in vitro	CAY10603, via inhibition of HDAC6, shows potent antiproliferative activity against pancreatic cancer cell lines with IC50 of <1 μM, which can be used as a new molecular probe in exploring HDAC biology. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	HDAC Inhibition Assays
キナーゼアッセイ	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: ((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. The standard errors of the IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the formula xf4_FitResultStdError.
細胞アッセイ	細胞株	BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 cells
	濃度	~50 μM
	反応時間	72 hours
	実験の流れ	The pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 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. 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 according to the manufacturer’s suggestions. The IC50 values are calculated using XLfit.

参考

https://pubmed.ncbi.nlm.nih.gov/18642892/

カスタマーフィードバック

: Data from [Data independently produced by , , Cancer Lett, 2016, 379(1):134-42]

: Data from [Data independently produced by , , Oncotarget, 2016, 7(34):54714-54722]

: Data from [Data independently produced by , , Oncol Rep, 2016, 36(1):589-97]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HDAC6 inhibitor-loaded brain-targeted nanocarrier-mediated neuroprotection in methamphetamine-driven Parkinson's disease [ Redox Biol, 2025, 79:103457]	PubMed: 39700694
Deacetylation of TALDO1 by HDAC6 promotes glycolysis and nasopharyngeal carcinoma progression through a moonlighting function [ Cell Death Dis, 2025, 16(1):743]	PubMed: 41120289
Targeting histone deacetylase 6 (HDAC6) to enhance radiation therapy in meningiomas in a 2D and 3D in vitro study [ EBioMedicine, 2024, 105:105211]	PubMed: 38917510
Global isonicotinylome analysis identified SMAD3 isonicotinylation promotes liver cancer cell epithelial-mesenchymal transition and invasion [ iScience, 2024, 27(9):110775]	PubMed: 39286495
HDAC6-selective inhibitor CAY10603 ameliorates cigarette smoke-induced small airway remodeling by regulating epithelial barrier dysfunction and reversing [ Respir Res, 2024, 25(1):66]	PubMed: 38317159
Histone deacetylase 6 inhibition restores leptin sensitivity and reduces obesity [ Nat Metab, 2022, 4(1):44-59]	PubMed: 35039672
MicroRNA-22 represses glioma development via activation of macrophage-mediated innate and adaptive immune responses [ Oncogene, 2022, 10.1038/s41388-022-02236-7]	PubMed: 35279703
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer [ Clin Epigenetics, 2022, 14(1):147]	PubMed: 36371227
Hypoxia Selectively Increases a SMAD3 Signaling Axis to Promote Cancer Cell Invasion [ Cancers (Basel), 2022, 14(11)2751]	PubMed: 35681731
Optimal therapeutic targeting by HDAC inhibition in biopsy-derived treatment-naïve diffuse midline glioma models [ Neuro Oncol, 2021, 23(3):376-386]	PubMed: 33130903

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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