HDAC2 Selective Inhibitors

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S7595	Santacruzamate A (CAY10683)	Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.	Selective	HDAC2, IC50: 119 pM
S5810	UF010	UF010 is a class I HDAC-selective inhibitor with IC50 values of 0.5 nM, 0.1 nM, 0.06 nM, 1.5 nM, 9.1 nM and 15.3 nM for HDAC1, HDAC2, HDAC3, HDAC8, HDAC6 and HDAC10, respectively.	Pan	HDAC2, IC50: 0.1 nM
S1096	Quisinostat (JNJ-26481585) 2HCl	Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.	Pan	HDAC2, IC50: 0.33 nM
S2759	Fimepinostat (CUDC-907)	CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.	Pan	HDAC2, IC50: 5.0 nM
S8769	Tinostamustine(EDO-S101)	Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs).	Pan	HDAC2, IC50: 9 nM
S1194	CUDC-101	CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.	Pan	HDAC2, IC50: 12.6 nM
S8495	WT161	WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis.	Pan	HDAC2, IC50: 15.4 nM
S1090	Abexinostat (PCI-24781)	Abexinostat (PCI-24781, CRA-024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with K_i of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.	Pan	HDAC2, Ki: 19 nM
S8464	Citarinostat (ACY-241)	Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.	Pan	HDAC2, IC50: 45 nM
S3020	Romidepsin	Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.	Pan	HDAC2, IC50: 47 nM
S8001	Ricolinostat (ACY-1215)	Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2.	Pan	HDAC2, IC50: 48 nM
S1515	Pracinostat (SB939)	Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2.	Pan	HDAC2, IC50: 96 nM
S6738	TC-H 106	TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively.	Pan	HDAC2, Ki: ~102 nM
S8567	Tucidinostat (Chidamide)	Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.	Pan	HDAC2, IC50: 160 nM
S1122	Mocetinostat (MGCD0103)	Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.	Pan	HDAC2, IC50: 0.29 μM
S2132	SR-4370	SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth.	Pan	HDAC2, IC50: 0.58 μM
S2818	Tacedinaline (CI994)	Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.	Pan	HDAC2, IC50: 0.9 μM
S7555	Domatinostat (4SC-202)	Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.	Pan	HDAC2, IC50: 1.12 μM
S8962	BRD3308	BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release.	Pan	HDAC2, IC50: 1.34 μM
S7689	BG45	BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively.	Pan	HDAC2, IC50: 2.2 μM
S7278	HPOB	HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.	Pan	HDAC2, IC50: 4.4 μM