Santacruzamate A (CAY10683)

Catalog No.S7595

For research use only.

Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.

Santacruzamate A (CAY10683) Chemical Structure

CAS No. 1477949-42-0

Selleck's Santacruzamate A (CAY10683) has been cited by 10 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.
Targets
HDAC2 [1]
()
119 pM
In vitro

Santacruzamate A inhibits the growth of HCT116 colon carcinoma cells and HuT-78 cutaneous T-cell lymphoma cells, with GI50 values of 29.4 μM and 1.4 μM, respectively. However, Santacruzamate A shows hypotoxicity to human dermal fibroblast cells (GI50 >100 μM). [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cell NFPBW4JEgXSxdH;4bYNqfHliYYPzZZk> NF3FXW06PiCq M{DBU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSVLWDNV{Bie3OjeTygS2k2OD1{OT60JO69VQ>? MnzJNlQyPjR{NEW=
HUT78 cell MnjSR5l1d3SxeHnjbZR6KGG|c3H5 Ml;tO|IhcA>? MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWXQ4QCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUNVCPUzDhd5NigSxiR1m1NF0yNjRizszN MnXWNlQyPjR{NEW=

Protocol (from reference)

Kinase Assay:

[1]

  • HDAC Enzyme Assay:

    The commercially availablae human recombinant enzyme and fluorogenic HDAC assay kits have used to measure percent inhibition and IC50 values of three HDAC isozymes (HDAC2, HDAC4, HDAC6). Briefly, the inhibitor is added sequentially to a black, flat-bottom 96-well microtiter plate, and the reaction mixture is incubated for 30 min at 37°C. The potent HDAC inhibitor trichostatin A (included in the assay kit) is added to the bifunctional HDAC assay developer at a final reaction concentration of 1 μM to stop deacetylation and initiate the release of the fluorophore. The reaction mixture is further incubated at room temperature for 15 min. Fluorescence is measured on a Spectra Max Gemini XPS using an excitation wavelength of 360 nm and a detection wavelength of 460 nm.

Cell Research:

[1]

  • Cell lines: HuT-78 cells, and HCT-116 cells
  • Concentrations: ~100 μM
  • Incubation Time: 72 or 96 hours
  • Method:

    HuT-78 cells incubated in Iscove’s modified Dulbecco’s medium supplemented with 20% FBS, 1% penicillin/streptomycin, and 1% L-glutamine. HCT-116 cells cultivated using McCoy’s 5A medium supplemented with 10% FBS, 1% penicillin/streptomycin, and 1% nonessential amino acids. Cells were seeded in a 96-well plate at 5000cells per well. Before treatment, the plates were incubated at 37°C, 5% CO2 for 24 h. Treatment with inhibitors were incubated in wells for 72 or 96 h using SAHA as a positive control. Antiproliferative activity was determined using a standard MTS-PMS assay.

Solubility (25°C)

In vitro

DMSO 55 mg/mL
(197.59 mM)
Ethanol 55 mg/mL
(197.59 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+30%PEG300+5%TW80+H2O
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 278.35
Formula

C15H22N2O3

CAS No. 1477949-42-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)NCCCC(=O)NCCC1=CC=CC=C1

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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