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DKFZ-748 | DKFZ-748 : Inhibitor of HDAC10
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
HDAC10
  • IC50:5 nM
  • IC50:22 nM
  • Kd apparent:160 nM
  • EC50:>50 uM
  • EC50:~0.1 uM
  • Activity:~5 uM
Inhibitor
1 to 5 µM
1 µM up to 10 uM

Selectivity

In Vitro Selectivity Assessment
HDAC1

Gene ID: Q13547

Organism: Homo sapiens

Family: histone deacetylase family

Potency: IC50 - 13 uM

Potency Assay Off-Target:
HDAC enzymatic assay (HDAC-glo assay)
Selectivity Assessment Description:
2500-fold selectivity factor
In Vitro Selectivity Assessment
HDAC2

Gene ID: Q92769

Organism: Homo sapiens

Family: histone deacetylase family

Potency: IC50 - 51 uM

Potency Assay Off-Target:
HDAC enzymatic assay (HDAC-glo assay)
Selectivity Assessment Description:
10000-fold selectivity factor
In Vitro Selectivity Assessment
HDAC3

Gene ID: O15379

Organism: Homo sapiens

Family: histone deacetylase family

Potency: IC50 - <100 uM

Potency Assay Off-Target:
HDAC enzymatic assay (HDAC-glo assay)
Selectivity Assessment Description:
>10000-fold selectivity factor
In Vitro Selectivity Assessment
HDAC6

Gene ID: Q9UBN7

Organism: Homo sapiens

Family: histone deacetylase family

Potency: IC50 - 3 uM

Potency Assay Off-Target:
HDAC enzymatic assay (HDAC-glo assay)
Selectivity Assessment Description:
630-fold selectivity factor
In Vitro Selectivity Assessment
HDAC8

Gene ID: Q9BY41

Organism: Homo sapiens

Family: histone deacetylase family

Potency: IC50 - 1.3 uM

Potency Assay Off-Target:
HDAC enzymatic assay (HDAC-glo assay)
Selectivity Assessment Description:
263-fold selectivity
In Cell Selectivity Assessment
HDAC1

Gene ID: Q13547

Organism: Homo sapiens

Family: histone deacetylase family

Potency: Kd apparent - <100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
HDAC2

Gene ID: Q92769

Organism: Homo sapiens

Family: histone deacetylase family

Potency: Kd apparent - <100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
HDAC5

Gene ID: Q9UQL6

Organism: Homo sapiens

Family: histone deacetylase family

Potency: Kd apparent - >100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
HDAC6

Gene ID: Q9UBN7

Organism: Homo sapiens

Family: histone deacetylase family

Potency: Kd apparent - >100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
HDAC8

Gene ID: Q9BY41

Organism: Homo sapiens

Family: histone deacetylase family

Potency: Kd apparent - >100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
ISOC1

Gene ID: Q96CN7

Organism: Homo sapiens

Family: isochorismatase family

Potency: Kd apparent - 40 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
250-fold selectivity
In Cell Selectivity Assessment
ISOC2

Gene ID: Q96AB3

Organism: Homo sapiens

Family: isochorismatase family

Potency: Kd apparent - 11 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
79-fold selectivity
In Cell Selectivity Assessment
ALDH1B1

Gene ID: P30837

Organism: Homo sapiens

Family: aldehyde dehydrogenase family

Potency: Kd apparent - >100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
ALDH2

Gene ID: P05091

Organism: Homo sapiens

Family: aldehyde dehydrogenase family

Potency: Kd apparent - >100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
GATD3

Gene ID: P0DPI2

Organism: Homo sapiens

Family: GATD3 family

Potency: Kd apparent - >100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity
In Cell Selectivity Assessment
MBLAC2

Gene ID: Q68D91

Organism: Homo sapiens

Family: Glyoxalase II family

Potency: Kd apparent - >100 uM

Potency Assay Off-Target:
Proteomic profiling
Selectivity Assessment Description:
>630-fold selectivity

Potency
Cellular
In Vitro

HDAC10

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jacs.2c05030

Negative Control Compounds

DKFZ-829
SMILES: O=C(C1=C2C=CC=CC2=CC=C1)NCCN(C)CCCC(OC)=O

Chemical Information

Molecular Formula C18H23N3O3
SMILEs CN(CCCC(=O)NO)CCNC(=O)c1cccc2ccccc12
InChI InChI=1S/C18H23N3O3/c1-21(12-5-10-17(22)20-24)13-11-19-18(23)16-9-4-7-14-6-2-3-8-15(14)16/h2-4,6-9,24H,5,10-13H2,1H3,(H,19,23)(H,20,22)
Molecular weight 329.17 Da
AlogP 0.0
HBond acceptors 6
HBond donors 3
Atoms 47

Expert Reviews

by SERP
(on 14 Apr 2024 )
Cellular Use Rating
This is an welcome advance in HDAC-specific probes. The original report provides significant SAR data to establish the potency and selectivity of this probe. In general, I would recommend starting off...
by SERP
(on 30 May 2024 )
Cellular Use Rating
This probe shows superb potency for HDAC10 as well as excellent selectivity for other members of the HDAC family and non-HDAC metalloproteases. This selectivity extends to cellular assays making this an...
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