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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

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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

DFZ-821
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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