SS-208

Inhibitor of HDAC6

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe SS-208 is in the process of SERP review.

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Information

HDAC6

Inhibitor

up to 5 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q9UBN7

Target Class: Epigenetic

Target SubClass: HDAC

Potency: IC50

Potency Value: 12 nM

Potency Assay: HDAC inhibition assay

PDB ID for probe-target interaction (3D structure): --

Structure-activity relationship: yes

Target aliases:

Histone deacetylase 6, KIAA0901, HDAC6, HDAC6_HUMA ...

DOI Reference: 10.1021/acs.jmedchem.9b00946

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 HDAC1 1390 nM

Potency assay (off target): HDAC inhibition assay

Probe Selectivity in Vitro:

Selectivity against other HDAC isoforms (IC50, uM): HDAC4 (19.5), HDAC5 (6.91), HDAC7 (8.34), HDAC8 (1.23), HDAC9 (38.2), HDAC11 (5.12)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 19 Mar 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

SS-208 represents a well-validated, selective chemical tool for exploring the functions of HDAC6 in cells. Notably, SS-206 does not induce cytotoxicity in human or mouse cell lines at doses where significant HDAC6 inhibition is observed, however this should be evaluated with the specific cellular model being used. As genetic knockout studies have shown that HDAC6 loss is generally not lethal to cells, the cytotoxicity observed with other existing HDAC6 inhibitors is likely through significant off-target inhibition of other HDACs or unrelated factors (see Lin et al, Sci Transl. Med., 2019; DOI: 10.1126/scitranslmed.aaw8412). Further credentialing of SS-208 (and all putative HDAC6 inhibitors) should assess cytoxicity profiles in HDAC6 knockout cells).

(last updated: 4 May 2021 )