HDAC6 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S7596 CAY10603

CAY10603是一种强效的选择性HDAC6抑制剂,IC50为2 pM,选择性比其它HDACs高200多倍。

Selective HDAC6, IC50: 2 pM
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.

Selective HDAC6, IC50: 0.4 nM
S8648 ACY-738

ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.

Selective HDAC6, IC50: 1.7 nM
S8464 Citarinostat (ACY-241)

Citarinostat (ACY-241)是一种具有口服活性的、选择性HDAC6抑制剂,对HDAC6和HDAC3的IC50分别为2.6 nM和46 nM。对HDAC6的选择性是对HDAC1-3的选择性的13-18倍。

Selective HDAC6, IC50: 2.6 nM
S2239 Tubacin

Tubacin是一种高度有效的选择性的,可逆的,细胞渗透性HDAC6抑制剂,无细胞试验中IC50为4 nM,比作用于HDAC1的选择性高350倍。

Selective HDAC6, IC50: 4 nM
S8001 Ricolinostat (ACY-1215)

Ricolinostat (ACY-1215)是一种选择性HDAC6抑制剂,无细胞试验中IC50为5 nM,作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上,对HDAC8具有微弱的作用活性,对HDAC4/5/7/9/11, Sirtuin1和Sirtuin2具有最小的作用活性。Phase 2。

Selective HDAC6, IC50: 4.7 nM
S7473 Nexturastat A

Nexturastat A 是一种强效的选择性的HDAC抑制剂,IC50为5 nM,其选择性高于其他的HDACs190倍。

Selective HDAC6, IC50: 5 nM
S0864 ACY-775

ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5  nM.

Selective HDAC6, IC50: 7.5 nM
S0709 Tubastatin A TFA

Tubastatin A is a potent inhibitor of HDAC6 with IC50 of 15 nM.

Selective HDAC6, IC50: 15 nM
S2627 Tubastatin A HCl

Tubastatin A HCl是一种有效的,选择性HDAC6抑制剂,无细胞试验中IC50为15 nM。选择性作用于所有其他同工酶(1000倍以上),除了HDAC8(57倍以上)。

Selective HDAC6, IC50: 15 nM
S8049 Tubastatin A

Tubastatin A是一种有效的,选择性HDAC6抑制剂,无细胞试验中IC50为15 nM,选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。

Selective HDAC6, IC50: 15 nM
S7278 HPOB

HPOB是一种有效的,选择性 HDAC6抑制剂,IC50为56 nM,选择性比对其它HDACs高30多倍。

Selective HDAC6, IC50: 56 nM
S8743 SKLB-23bb

SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.

Selective HDAC6, IC50: <100 nM
S1194 CUDC-101

CUDC-101是一种有效的,多靶点抑制剂,作用于HDACEGFR和HER2,IC50分别为4.4 nM, 2.4 nM,和15.7 nM,且抑制I/II型HDACs,但是对III型, Sir-type HDACs没有抑制作用。Phase 1。

Pan HDAC6, IC50: 5.1 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 HDAC6, IC50: 6 nM
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 HDAC6, IC50: 9.1 nM
S1090 Abexinostat (PCI-24781)

Abexinostat (PCI-24781)是一种新型的pan-HDAC抑制剂,靶向作用于HDAC1Ki为7 nM,对HDACs 2, 3, 6,和10有适中的抑制性,但比作用于HDAC8选择性强40倍。Phase 1/2。

Pan HDAC6, Ki: 17 nM
S2759 Fimepinostat (CUDC-907)

CUDC-907是一种PI3K和HDAC双重抑制剂,作用于PI3KαHDAC1/2/3/10IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。Phase 1。

Pan HDAC6, IC50: 27 nM
S7726 BRD73954

BRD73954是一种有效的选择性 HDAC 抑制剂,对HDAC6 和 HDAC8的 IC50 分别为 36 nM 和 120 nM。

Pan HDAC6, IC50: 36 nM
S2693 Resminostat

Resminostat剂量依赖性的选择性的抑制HDAC1/3/6IC50为42.5 nM/50.1 nM/71.8 nM,作用于HDAC8效果弱,IC50为877 nM。

Pan HDAC6, IC50: 71.8 nM
S1515 Pracinostat (SB939)

Pracinostat (SB939)是一种有效的pan-HDAC抑制剂,IC50为40-140 nM,除了HDAC6例外,对III型同工酶SIRT I没有抑制活性。Phase 2。

Pan HDAC6, IC50: 1.008 μM
S1422 Droxinostat

Droxinostat是一种选择性的HDAC抑制剂,最有效作用于HDACs 6和8,IC50为2.47μM和1.46 μM,比作用于HDAC3选择性高8倍,对HDAC1, 2, 4, 5, 7, 9,和10没有抑制作用。

Pan HDAC6, IC50: 2.47 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 HDAC6, IC50: 3.7 μM
S8773 TH34

TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM).

Pan HDAC6, IC50: 4.6 μM
S9275 Isoguanosine

Isoguanosine (Crotonoside) inhibits FLT3 and HDAC3/6 for the treatment of AML.Isoguanosine is a naturally occurring active isomer of guanosine that is found in the seeds of Croton tiglium.

Pan