Art. -Nr.: HY-18613

CAY10603

(Synonyms: BML-281)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

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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Reinheit: 99.76%
CAS. Nr.: 1045792-66-2
Formel: C₂₂H₃₀N₄O₆
Molecular Weight:446.50

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CAY10603 Chemical Structure

CAS. Nr.: 1045792-66-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC6

0.002 nM (IC₅₀)

HDAC3

0.42 nM (IC₅₀)

HDAC10

90.7 nM (IC₅₀)

HDAC2

252 nM (IC₅₀)

HDAC1

271 nM (IC₅₀)

HDAC8

6851 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10 μM Compound: CAY10603	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 35043615]
B16-F10	IC₅₀	9.41 μM Compound: CAY10603	Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 35043615]
BXPC-3	IC₅₀	1 μM Compound: 7	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 18642892]
HCT-116	IC₅₀	1.47 μM Compound: CAY10603	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 35043615]
HL-60	IC₅₀	594 nM Compound: CAY10603	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 33360560]
HMEC	IC₅₀	<1 μM Compound: 7	Cytotoxicity against HMEC after 72 hrs by MTT assay Cytotoxicity against HMEC after 72 hrs by MTT assay	[PMID: 18642892]
HuP-T3	IC₅₀	0.3 μM Compound: 7	Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay	[PMID: 18642892]
Jurkat	IC₅₀	0.61 μM Compound: CAY10603	Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35043615]
MCF7	IC₅₀	2.82 μM Compound: CAY10603	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 35043615]
MIA PaCa-2	IC₅₀	0.1 μM Compound: 7	Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay	[PMID: 18642892]
Sf9	IC₅₀	13.8 nM Compound: 1b	Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s	[PMID: 31414801]
Sf9	IC₅₀	3.2 nM Compound: 1b	Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi	[PMID: 31414801]
SU.86.86	IC₅₀	0.6 μM Compound: 7	Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay	[PMID: 18642892]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1045792-66-2
Appearance Solid
Molecular Weight 446.50
Formel C₂₂H₃₀N₄O₆
Color White to light yellow
SMILES

O=C(OC(C)(C)C)NC1=CC=C(C2=CC(C(NCCCCCCC(NO)=O)=O)=NO2)C=C1
Synonyms

BML-281
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (7)

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Journal Impact Factor

J Transl Med

Construction of an ER stress-related prognostic signature for predicting prognosis and screening the effective anti-tumor drug in osteosarcoma. [Abstract]

2024 Jan 16;22(1):66. PMID: 38229155
Clin Transl Med

A methyltransferase-like 14/miR-99a-5p/tribble 2 positive feedback circuit promotes cancer stem cell persistence and radioresistance via histone deacetylase 2-mediated epigenetic modulation in esophageal squamous cell carcinoma. [Abstract]

2021 Sep;11(9):e545. PMID: 34586732
Cancer Cell Int

Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]

2021 Jun 5;21(1):291. PMID: 34090418
Commun Biol

Selective inhibition of HDAC class IIA as therapeutic intervention for KMT2A-rearranged acute lymphoblastic leukemia. [Abstract]

2024 Oct 4;7(1):1257. PMID: 39362994
Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.
Arch Biochem Biophys

Inhibition of HDAC6 with CAY10603 alleviates acute and chronic kidney injury by suppressing the ATF6 branch of UPR. [Abstract]

2024 Jun:756:110009. PMID: 38642631
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (111.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2396 mL

11.1982 mL

22.3964 mL

5 mM

0.4479 mL

2.2396 mL

4.4793 mL

10 mM

0.2240 mL

1.1198 mL

2.2396 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (11.20 mM); Suspended solution; Need ultrasonic and warming and heat to 42°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kozikowski AP, et al. Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. J Med Chem. 2008 Aug 14;51(15):4370-3. [Content Brief]

[2]. Wang Z, et al. HDAC6 promotes cell proliferation and confers resistance to gefitinib in lung adenocarcinoma. Oncol Rep. 2016 Jul;36(1):589-97. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2396 mL	11.1982 mL	22.3964 mL	55.9910 mL
	5 mM	0.4479 mL	2.2396 mL	4.4793 mL	11.1982 mL
	10 mM	0.2240 mL	1.1198 mL	2.2396 mL	5.5991 mL
	15 mM	0.1493 mL	0.7465 mL	1.4931 mL	3.7327 mL
	20 mM	0.1120 mL	0.5599 mL	1.1198 mL	2.7996 mL
	25 mM	0.0896 mL	0.4479 mL	0.8959 mL	2.2396 mL
	30 mM	0.0747 mL	0.3733 mL	0.7465 mL	1.8664 mL
	40 mM	0.0560 mL	0.2800 mL	0.5599 mL	1.3998 mL
	50 mM	0.0448 mL	0.2240 mL	0.4479 mL	1.1198 mL
	60 mM	0.0373 mL	0.1866 mL	0.3733 mL	0.9332 mL
	80 mM	0.0280 mL	0.1400 mL	0.2800 mL	0.6999 mL
	100 mM	0.0224 mL	0.1120 mL	0.2240 mL	0.5599 mL

Keywords

CAY10603

7 Cited Publications

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CAY10603

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Osteogenesis Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) CAY10603

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CAY10603

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Osteogenesis Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) CAY10603

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CAY10603 Related Classifications

HY-18613 Related Classifications