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CAY10603

Catalog No. T1983   CAS 1045792-66-2
Synonyms: HDAC6 Inhibitor, BML-281

CAY10603 (BML-281) is a potent and selective inhibitor of HDAC6.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
CAY10603 Chemical Structure
CAY10603, CAS 1045792-66-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 57.00
2 mg In stock $ 75.00
5 mg In stock $ 97.00
10 mg In stock $ 173.00
25 mg In stock $ 323.00
50 mg In stock $ 547.00
100 mg In stock $ 788.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 98.06%
Purity: 98%
Purity: 95.97%
Purity: 95.75%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CAY10603 (BML-281) is a potent and selective inhibitor of HDAC6.
Targets&IC50 HDAC6:2 pM
In vivo CAY10603 exhibits effective anti-proliferative activity against pancreatic cancer cell lines by inhibiting HDAC6, with an IC50 of less than 1 μM.
Kinase Assay HDAC Inhibition Assays: 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.
Cell Research 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.(Only for Reference)
Synonyms HDAC6 Inhibitor, BML-281
Molecular Weight 446.5
Formula C22H30N4O6
CAS No. 1045792-66-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 5 mg/mL (11.19 mM), warmed

DMSO: 82 mg/mL (183.7 mM)

TargetMolReferences and Literature

1. Kozikowski AP, et al. J Med Chem. 2008, 51(15), 4370-4373.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Aging Compound Library Epigenetics Compound Library Drug Repurposing Compound Library Histone Modification Compound Library Anti-Pancreatic Cancer Compound Library Chromatin Modification Compound Library

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Keywords

CAY10603 1045792-66-2 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC HDAC6 Inhibitor BML 281 inhibit Histone deacetylases CAY 10603 Inhibitor BML281 BML-281 CAY-10603 inhibitor

 

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