Art. -Nr.: HY-149208

HDAC-IN-53

1 Cited Publications

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HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC₅₀ values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC₅₀>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer.

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Reinheit: 95.73%
CAS. Nr.: 2921948-27-6
Formel: C₂₃H₂₀ClN₇O₂
Molecular Weight:461.90

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

HDAC-IN-53 Chemical Structure

CAS. Nr.: 2921948-27-6

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC1

47 nM (IC₅₀)

HDAC2

125 nM (IC₅₀)

HDAC3

450 nM (IC₅₀)

HDAC4

>10 μM (IC₅₀)

HDAC5

>10 μM (IC₅₀)

HDAC6

>10 μM (IC₅₀)

HDAC7

>10 μM (IC₅₀)

HDAC8

>10 μM (IC₅₀)

HDAC9

>10 μM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1425 nM Compound: 19h	Antiproliferative activity against human A549 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
CAKI-1	IC₅₀	252 nM Compound: 19h	Antiproliferative activity against human CAKI-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human CAKI-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
DOHH-2	IC₅₀	65 nM Compound: 19h	Antiproliferative activity against human DOHH-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human DOHH-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
ES-2	IC₅₀	15 nM Compound: 19h	Antiproliferative activity against human ES2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ES2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HCT-116	IC₅₀	0.56 μM Compound: 19h	Antiproliferative activity against human HCT-116 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HEK293	IC₅₀	1256 nM Compound: 19h	Antiproliferative activity against human HEK293 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HEK293 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HeLa	IC₅₀	644 nM Compound: 19h	Antiproliferative activity against human HeLa cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
Jurkat	IC₅₀	126 nM Compound: 19h	Antiproliferative activity against human Jurkat cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Jurkat cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
K562	IC₅₀	345 nM Compound: 19h	Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MC-38	IC₅₀	0.66 μM Compound: 19h	Antiproliferative activity against mouse MC38 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse MC38 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MDA-MB-231	IC₅₀	425 nM Compound: 19h	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MIA PaCa-2	IC₅₀	297 nM Compound: 19h	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
NCI-N87	IC₅₀	607 nM Compound: 19h	Antiproliferative activity against human NCI-N87 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-N87 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
PC-3	IC₅₀	1657 nM Compound: 19h	Antiproliferative activity against human PC-3 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-3 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
PC-9	IC₅₀	249 nM Compound: 19h	Antiproliferative activity against human PC-9 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
ZR-75-1	IC₅₀	1125 nM Compound: 19h	Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]

In Vitro

HDAC-IN-53 (compound 19h) has good antiproliferative activity against a panel of cancer cell lines, for example MC38 (IC₅₀=0.66 μM), HCT116 cell (IC₅₀=0.56 μM) ^[1].
HDAC-IN-53 (0.1-1 μM; 24 h) causes G0/G1 cell cycle arrest in MC38 cells and induces G2/M cell cycle arrest in HCT116 cells^[1].
HDAC-IN-53 (0.1-1 μM; 24 h) upregulates the expressions of cleaved caspase-3 and cleaved PARP in a dose-dependent manner^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

MC38 and HCT116 cells
Concentration:

0.1, 0.3, 1 μM
Incubation Time:

24 h
Result:

Caused G0/G1 cell cycle arrest in MC38 cells and induced G2/M cell cycle arrest in HCT116 cells.
Significantly decreased the proportion of S phase cells in MC38 cells.

Western Blot Analysis^[1]

Cell Line:

MC38 and HCT116 cells
Concentration:

0.1, 0.3, 1 μM
Incubation Time:

24 h
Result:

Upregulated the expressions of cleaved caspase-3 and cleaved PARP in a dose-dependent manner.

In Vivo

HDAC-IN-53 (60 or 120 mg/kg; PO; daily for 15 days) exerts antitumor activities by both direct tumor growth inhibition and indirect immune cell-mediated antitumor effect^[1].
Pharmacokinetic Parameters of HDAC-IN-53 in Mice^[1].

	IV (5 mg/kg)	PO (20 mg/kg)
T_max (h)		0.42
C_max (ng/mL)	8129	9558
AUC_0-t (ng/mL∗h)	5864	15278
t_1/2 (h)	0.85	2.49
F (%)		65.1%

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

Animal Model:

C57BL/6 Mice or athymic nude mice (female, 6-8 weeks old) with MC38 cells^[1]
Dosage:

60 or 120 mg/kg
Administration:

PO; daily for 15 days
Result:

Yielded TGI values of 60.3 and 87.6%, respectively.
Increased the percentage of CD4+ T cells.

Chemical Information

CAS. Nr. 2921948-27-6
Appearance Solid
Molecular Weight 461.90
Formel C₂₃H₂₀ClN₇O₂
Color White to off-white
SMILES

NC1=NN(C2=CC=CC=C2Cl)N=C1C(NCC3=CC=C(C=C3)C(NC4=CC=CC=C4N)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (216.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.1650 mL

10.8249 mL

21.6497 mL

5 mM

0.4330 mL

2.1650 mL

4.3299 mL

10 mM

0.2165 mL

1.0825 mL

2.1650 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Nan Sun, et al. Design and Synthesis of Triazole-Containing HDAC Inhibitors That Induce Antitumor Effects and Immune Response. J Med Chem. 2023 Apr 13;66(7):4802-4826. [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	2.1650 mL	10.8249 mL	21.6497 mL	54.1243 mL
	5 mM	0.4330 mL	2.1650 mL	4.3299 mL	10.8249 mL
	10 mM	0.2165 mL	1.0825 mL	2.1650 mL	5.4124 mL
	15 mM	0.1443 mL	0.7217 mL	1.4433 mL	3.6083 mL
	20 mM	0.1082 mL	0.5412 mL	1.0825 mL	2.7062 mL
	25 mM	0.0866 mL	0.4330 mL	0.8660 mL	2.1650 mL
	30 mM	0.0722 mL	0.3608 mL	0.7217 mL	1.8041 mL
	40 mM	0.0541 mL	0.2706 mL	0.5412 mL	1.3531 mL
	50 mM	0.0433 mL	0.2165 mL	0.4330 mL	1.0825 mL
	60 mM	0.0361 mL	0.1804 mL	0.3608 mL	0.9021 mL
	80 mM	0.0271 mL	0.1353 mL	0.2706 mL	0.6766 mL
	100 mM	0.0216 mL	0.1082 mL	0.2165 mL	0.5412 mL

Keywords

HDAC-IN-53

1 Cited Publications

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HDAC-IN-53

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) HDAC-IN-53

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HDAC-IN-53

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) HDAC-IN-53

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HDAC-IN-53 Related Classifications

HY-149208 Related Classifications