hdac6

HDAC6 degrader 9c is a small molecule histone deacetylase 6 (HDAC6) degrader that can be used to study cancer or other diseases.

BChE/HDAC6-IN-2 is a selective and potent dual inhibitor of BChE and HDAC6 with neuroprotective and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is a metal ion co-agonist that inhibits tau phosphorylation and can be used in the study of immune and neurological diseases.

TCS HDAC6 20b (HDAC6-IN-7) is a selective HDAC6 inhibitor that blocks the growth of breast cancer cells and may be used in the study of cancer and neurodegenerative diseases.

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.

LSD1/HDAC6-IN-1 is an orally active dual inhibitor targeting lysine specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6), demonstrating promising anti-tumor activity, particularly valuable for multiple myeloma (MM) research [1].

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1/2/3/6/7/11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

MPI_5a is a small molecule inhibitor and a highly selective HDAC6 inhibitor (IC50=36 nM). The IC50 value for MPI_5a inhibition of intracellular acetylated tubulin accumulation is 210 nM, used for HDAC6 function research.

ACY-1083 is a small molecule inhibitor, a highly selective HDAC6 inhibitor (IC50=3 nM), with 260-fold higher selectivity over other classes of HDAC isoforms. It is brain-penetrant and used for research on chemotherapy-induced peripheral neuropathy.

SS-208 is a selective inhibitor of HDAC6 (IC50 = 12 nM) with anti-tumor activity. SS-208 shows selectivity over other HDAC subtypes.

BRD 9757 (N-Hydroxy-1-cyclopentene-1-carboxamide) is a selective inhibitor of HDAC6 (IC50 = 30 nM).

MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.

Imofinostat (MPT0E028) is a selective, orally available pan-HDAC inhibitor with IC₅₀ values of 53.0/106.2/29.5 nM against HDAC1/HDAC2/HDAC6 in HCT116 cells. In B-cell lymphoma, Imofinostat induces cell cycle arrest and apoptosis whilst inhibiting Akt phosphorylation, demonstrating anticancer activity across multiple tumour types.

BG45 is an HDAC I type inhibitor with IC50 of 289 nM, 2.0 μM, 2.2 μM and >20 μM for HDAC3/1/2/6 in cell-free assays, respectively.

Droxinostat (NS 41080) is a selective HDAC inhibitor, primarily targeting HDACs 6 and 8 with IC50 values of 2.47 μM and 1.46 μM, respectively. It is over 8-fold more selective against HDAC3 and shows no inhibition for HDAC1, 2, 4, 5, 7, 9, and 10.

PCI-24781 (Abexinostat (PCI24781)) is a new pan-HDAC inhibitor mainly targeting HDAC1 (Ki: 7 nM), also have moderate inhibitory for HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.

AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6, HDAC11 (IC50s: 654, 190, and 636 nM) with anti-tumor activity.

CG347B is a selective inhibitor of HDAC6.

CRA-026440 is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.

HDAC-IN-4, a selective HDAC6 and HDAC10 inhibitor (pIC50s: 7.2 and 6.8 in the BRET assay), exhibits antitumoral activity.

HDACs/mTOR Inhibitor 1 is a dual HDAC and mammalian target of Rapamycin (mTOR) inhibitor for treating hematologic malignancies, with IC50 values of 0.19 nM, 1.8 nM, 1.2 nM, and >500 nM for HDAC1, HDAC6, mTOR, and PI3Kα, respectively.

J22352, a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM, enhances anticancer effects in glioblastoma by promoting HDAC6 degradation. It does so by inhibiting autophagy and stimulating the antitumor immune response, further restoring host antitumor activity through the reduction of PD-L1's immunosuppressive activity.

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K and HDAC, with IC50 values of 8.1 nM and 1.4 nM, respectively.

1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM, demonstrating greater selectivity for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). It does not increase global histone H4 acetylation or reduce total intracellular HDAC activity but can induce tubulin acetylation[1][2].

RTS-V5 is a dual inhibitor of HDAC/proteasome (IC50s: 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively).