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Santacruzamate A (CAY10683) HDAC inhibitor

Name: Santacruzamate A (CAY10683)
Brand: Selleck Chemicals
SKU: S7595
Availability: InStock
Rating: 5 (26 reviews)

Cat.No.S7595

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

Chemical Structure

Molecular Weight: 278.35

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.62%

99.62

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
HCT116 cell	Cytotoxicity assay	96 h	Cytotoxicity against human HCT116 cells after 96 hrs by MTS-PMS assay, GI50=29.4 μM
HUT78 cell	Cytotoxicity assay	72 h	Cytotoxicity against human HUT78 cells after 72 hrs by MTS-PMS assay, GI50=1.4 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	278.35	Formula	C₁₅H₂₂N₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1477949-42-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCOC(=O)NCCCC(=O)NCCC1=CC=CC=C1

Solubility

In vitro
Batch:

DMSO : 56 mg/mL ( (201.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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 30%PEG300 2 5%Tween80 3 60%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (35.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (17.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (8.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (17.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	HDAC2 ^[1] 119 pM
In vitro	Santacruzamate A (CAY10683) 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, it shows hypotoxicity to human dermal fibroblast cells (GI₅₀ >100 μM). ^[1]
Kinase Assay	HDAC Enzyme Assay
Kinase Assay	Santacruzamate A (CAY10683) was evaluated using commercially available human recombinant enzyme and fluorogenic HDAC assay kits to measure percent inhibition and IC₅₀ values of three HDAC isozymes (HDAC2, HDAC4, HDAC6). Briefly, the inhibitor was added sequentially to a black, flat-bottom 96-well microtiter plate, and the reaction mixture was incubated for 30 min at 37°C. The potent HDAC inhibitor trichostatin A (included in the assay kit) was 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 was further incubated at room temperature for 15 min. Fluorescence was measured on a Spectra Max Gemini XPS using an excitation wavelength of 360 nm and a detection wavelength of 460 nm.
In vivo	CAY10683 (Santacruzamate A) is a potent and selective HDAC2 inhibitor that suppressed metastasis in mice liver metastasis model.
References	https://pubmed.ncbi.nlm.nih.gov/24164245/ https://pubmed.ncbi.nlm.nih.gov/35884488/

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