1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. HDAC3-IN-T247

HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells.

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HDAC3-IN-T247

HDAC3-IN-T247 Estructura química

No. CAS : 1451042-18-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Descripciòn

HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC50 of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells[1].

IC50 & Target

HDAC3

0.24 μM (IC50)

HDAC1

19 μM (IC50)

HDAC4

>100 μM (IC50)

HDAC6

>100 μM (IC50)

HDAC8

>100 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
19 3
Compound: 22; T247
Inhibition of human recombinant full-length C-terminal GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells by fluorescence assay
Inhibition of human recombinant full-length C-terminal GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells by fluorescence assay
[PMID: 30735902]
Sf9 IC50
19 3
Compound: 73
Inhibition of recombinant human full length C-terminal GST-tagged HDAC1 expressed in baculovirus Sf9 insect cells using HDAC Glo I/II substrate by Kinase Glo luminescence assay
Inhibition of recombinant human full length C-terminal GST-tagged HDAC1 expressed in baculovirus Sf9 insect cells using HDAC Glo I/II substrate by Kinase Glo luminescence assay
[PMID: 31050421]
Sf9 IC50
> 100 3
Compound: 73
Inhibition of recombinant human full length C-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus Sf9 insect cells using HDAC class 2a substrate incubated for 30 mins by fluorescence assay
Inhibition of recombinant human full length C-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus Sf9 insect cells using HDAC class 2a substrate incubated for 30 mins by fluorescence assay
[PMID: 31050421]
Sf9 IC50
19 3
Compound: 73
Inhibition of recombinant human full length C-terminal GST-tagged HDAC1 expressed in baculovirus Sf9 insect cells using HDAC Glo I/II substrate by Kinase Glo luminescence assay
Inhibition of recombinant human full length C-terminal GST-tagged HDAC1 expressed in baculovirus Sf9 insect cells using HDAC Glo I/II substrate by Kinase Glo luminescence assay
[PMID: 31050421]
Sf9 IC50
19000 1
Compound: 22; T247
Inhibition of human recombinant full-length C-terminal GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells by fluorescence assay
Inhibition of human recombinant full-length C-terminal GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells by fluorescence assay
[PMID: 30735902]
Sf9 IC50
19 3
Compound: 73
Inhibition of recombinant human full length C-terminal GST-tagged HDAC1 expressed in baculovirus Sf9 insect cells using HDAC Glo I/II substrate by Kinase Glo luminescence assay
Inhibition of recombinant human full length C-terminal GST-tagged HDAC1 expressed in baculovirus Sf9 insect cells using HDAC Glo I/II substrate by Kinase Glo luminescence assay
[PMID: 31050421]
Sf9 IC50
>100 3
Compound: 73
Inhibition of recombinant human full length C-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus Sf9 insect cells using HDAC class 2a substrate incubated for 30 mins by fluorescence assay
Inhibition of recombinant human full length C-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus Sf9 insect cells using HDAC class 2a substrate incubated for 30 mins by fluorescence assay
[PMID: 31050421]
Sf9 IC50
19000 1
Compound: 22; T247
Inhibition of human recombinant full-length C-terminal GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells by fluorescence assay
Inhibition of human recombinant full-length C-terminal GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells by fluorescence assay
[PMID: 30735902]
Sf9 IC50
> 100 3
Compound: 73
Inhibition of recombinant human full length C-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus Sf9 insect cells using HDAC class 2a substrate incubated for 30 mins by fluorescence assay
Inhibition of recombinant human full length C-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus Sf9 insect cells using HDAC class 2a substrate incubated for 30 mins by fluorescence assay
[PMID: 31050421]
U-937 CC50
0.83 3
Compound: T247
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 29541372]
U-937 CC50
0.83 3
Compound: T247
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 29541372]
U-937 CC50
0.83 3
Compound: T247
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 29541372]
Peso molecular

389.47

Fòrmula

C21H19N5OS

No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(C2=CN(CCC3=CSC=C3)N=N2)C=C1)NC4=C(N)C=CC=C4

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 25 mg/mL (64.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5676 mL 12.8380 mL 25.6759 mL
5 mM 0.5135 mL 2.5676 mL 5.1352 mL
View the Complete Stock Solution Preparation Table

* 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.

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In Vivo Dissolution Calculator
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Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5676 mL 12.8380 mL 25.6759 mL 64.1898 mL
5 mM 0.5135 mL 2.5676 mL 5.1352 mL 12.8380 mL
10 mM 0.2568 mL 1.2838 mL 2.5676 mL 6.4190 mL
15 mM 0.1712 mL 0.8559 mL 1.7117 mL 4.2793 mL
20 mM 0.1284 mL 0.6419 mL 1.2838 mL 3.2095 mL
25 mM 0.1027 mL 0.5135 mL 1.0270 mL 2.5676 mL
30 mM 0.0856 mL 0.4279 mL 0.8559 mL 2.1397 mL
40 mM 0.0642 mL 0.3209 mL 0.6419 mL 1.6047 mL
50 mM 0.0514 mL 0.2568 mL 0.5135 mL 1.2838 mL
60 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
HDAC3-IN-T247
Cat. No.:
HY-123295
Cantidad:
MCE Japan Authorized Agent: