Fig. 1 · Structure

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BRD-6929

HDAC1/HDAC2 inhibitor

BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50= 1 and 8 nM), extracted from patent US2018360927.

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Biological Activity

Target & Activity

Target Activity Value
HDAC1 IC50 1 nM
HDAC2 IC50 8 nM
HDAC3 IC50 458 nM
HIV-1  

Cellular Effect

Cell Line Activity Value Description Reference
Epithelial cell IC50 > 50 μM Cytotoxicity against human mammary epithelial cells by MTT assay [PMID: 17941625]
HCT-116 IC50 0.5 μM Cytotoxicity against human HCT116 cells by MTT assay [PMID: 17941625]
Jurkat CC50 12.6 μM Cytotoxicity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent cell viability assay [PMID: 29541372]
Jurkat IC50 204 nM Inhibition of FLAG-tagged HDAC1 S113A mutant (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis [PMID: 24405391]
Jurkat IC50 40 nM Inhibition of wild-type FLAG-tagged HDAC1 (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis [PMID: 24405391]
KB IC50 5.27 μM Cytotoxicity against human KB cells after 72 hrs by MTS assay [PMID: 25899338]
Sf9 IC50 0.001 μM Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate [PMID: 27377864]
Sf9 IC50 0.013 μM Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate preincubated for 3 hrs measured after 60 mins by flu [PMID: 27377864]
U-937 CC50 14 μM Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay [PMID: 29541372]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 849234-64-6
Applications HDAC1/HDAC2 inhibitor
Formula C19H17N3O2S
Molecular Weight 351.42
SMILES
O=C(NC1=CC(C2=CC=CS2)=CC=C1N)C3=CC=C(NC(C)=O)C=C3

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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