Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6327 |
Tubacin
|
Virus Protease; HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology |
Tubacin 是一种高效、选择性、可逆、可渗透细胞的 HDAC6 抑制剂,IC50 为 4 nM,选择性是 HDAC1 的约 350 倍。 | |||
T71587 |
Fluoxetine succinate ester
|
||
Fluoxetine succinate ester is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder, bulimia nervosa, panic disorder, and premenstrual dysphoric disorder. | |||
T69753 |
HDAC6 degrader 9c
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6 degrader 9c 是一种小分子组蛋白脱乙酰酶 6 (HDAC6) 降解剂,可用于研究癌症或其他疾病。 | |||
T72012 |
HDAC-IN-6
|
||
HDAC-IN-6 is an HDAC inhibitor, targeting HDAC2, HDAC3, HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9. | |||
T60954 | HDAC6-IN-6 | ||
HDAC6-IN-6 (化合物 6a) 是 HDAC6的有效抑制剂,可以穿透血脑屏障,IC50值为0.025 μM。HDAC6-IN-6 对 AChE 和 Aβ1-42自聚集具有有效的抑制活性,IC50值分别为 0.72 和 3.0 μM。HDAC6-IN-6 可促进神经突起生长而没有显著的神经毒性。 | |||
T79769 |
HDAC6-IN-23
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-23(化合物9)是一种口服活性HDAC6抑制剂。 | |||
T60856 |
HDAC6-IN-9
|
||
HDAC6-IN-9 (compound 12c) 是 HDAC6的强效选择性抑制剂,具有抗增殖活性。HDAC6-IN-9 对 HDAC6、HDAC1、HDAC3、HDAC8 和 HDAC10 的 IC50值分别为 4.2, 11.8, 15.2, 139.6, 21.3 nM。 | |||
T73043 |
HDAC6-IN-15
|
||
HDAC6-IN-15 是一种选择性组蛋白脱乙酰酶 6(HDAC6)抑制剂。HDAC6-IN-15 对 HDAC6具有有效的抑制活性,IC50值为 38.2 nM。HDAC6-IN-15 可用于癌症和神经退行性疾病的研究。 | |||
T82226 |
HDAC6-IN-21
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-21(化合物13)为一种靶向组蛋白去乙酰化酶6(histone deacetylase 6(HDAC6))的不可逆抑制剂。 | |||
T63247 | HDAC6-IN-12 | ||
HDAC6-IN-12 是 HDAC6 的有效抑制剂,能够结合 DNA 链中,导致 DNA 损伤,表现出抗癌作用,能够用于研究癌症。 | |||
T63472 |
HDAC6-IN-4
|
||
HDAC6-IN-4 (C10) 是一种口服具有活力的、高度选择性的、有效的、无明显毒性的 HDAC6 抑制剂 (IC50: 23 nM)。HDAC6-IN-4 能够诱导肿瘤细胞凋亡 (apoptosis),表现出高效的抗肿瘤效果。 | |||
T82225 |
HDAC6-IN-24
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-24(化合物N1)是一种HDAC6抑制剂。 | |||
T36625 |
LSD1/HDAC6-IN-1
LSD1/HDAC6-IN-1 |
||
LSD1/HDAC6-IN-1 is an orally active compound that functions as a dual inhibitor, targeting lysine specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6). This compound demonstrates promising anti-tumor activity and is particularly valuable for research focused on multiple myeloma (MM) [1]. | |||
T74617 | HDAC6-IN-8 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Compound 12c has been synthesized with modifications to the Cap group and exhibits broad-spectrum enzyme inhibitory activity as evidenced by enzyme inhibition assays. Compounds 9m and 9q show a preference for inhibiting HDAC6, demonstrating selective inhibitory activity among representative subtypes. | |||
T78768 |
HDAC6-IN-16
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-16(compound 5c)是基于Quinazolin-4(3H)-One的一种HDAC6抑制剂,具备抑制肿瘤细胞集落形成的抗癌活性。该化合物能够引发G2期细胞周期阻滞并诱导细胞凋亡(apoptosis)。 | |||
T79771 |
HDAC6-IN-22
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-22(化合物30)是一种针对HDAC6的抑制剂,其IC50值为4.63 nM。该化合物在体外及体内均展现出对多发性骨髓瘤细胞的抗增殖能力。HDAC6-IN-22 可诱导G2期的细胞周期阻滞,并通过线粒体路径促进细胞凋亡。 | |||
T61139 | HDAC6-IN-3 | ||
HDAC6-IN-3 (Compound 14) is a potent anti-prostate cancer agent that acts as an orally active inhibitor of HDAC6. It has IC50 values ranging from 0.02-1.54 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10. Additionally, HDAC6-IN-3 also demonstrates effective inhibition of MAO-A (IC50 = 0.79 μM) and LSD1 [1]. | |||
T61792 | HDAC6-IN-10 | ||
HDAC6-IN-10 is a potent and specific HDAC6 inhibitor, exhibiting an IC50 value of 0.73 nM. It demonstrates remarkable selectivity towards HDAC6, with a selectivity range of 144 to 10,941-fold over other HDAC isoforms. Furthermore, HDAC6-IN-10 exhibits notable anti-proliferative effects on multiple myeloma cells [1]. | |||
T79523 |
HDAC6-IN-18
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-18(化合物4)是首个针对HDAC6亚型的不可逆选择性抑制剂,显示出有效的抗多发性骨髓瘤活性。该抑制剂在RPMI8266、U266以及MM.1S细胞系中表现出对HDAC6的抑制效力,其IC50值分别为0.17、0.7和0.42 μM[1]。 | |||
T61044 |
HDAC6-IN-11
|
||
HDAC6-IN-11 (Compound 9) 对癌细胞具有抗增殖活性。HDAC6-IN-11 是 HDAC6 的选择性抑制剂,IC50值为 20.7 nM。HDAC6-IN-11 的选择性是其他 HDAC 异构体的 300 多倍。 | |||
T73031 |
HDAC6-IN-14
|
||
HDAC6-IN-14 是一种高选择性 HDAC6(HDAC) 抑制剂,IC50为 42 nM。HDAC6-IN-14 的选择性是 HDAC1/HDAC2/HDAC3/HDAC4 的 100 倍以上。 | |||
T61474 | HDAC6-IN-13 | ||
HDAC6-IN-13 (Compound 35m) is a potent and highly selective orally active inhibitor of HDAC6, with an IC50 of 0.019 μM. It also demonstrates inhibitory activity against HDAC1, HDAC2, and HDAC3, with IC50 values of 1.53 μM, 2.06 μM, and 1.03 μM, respectively. HDAC6-IN-13 exhibits substantial blood-brain barrier permeability and displays anti-inflammatory properties [1]. | |||
T78769 |
HDAC6-IN-17
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-17(化合物5b)是一种选择性HDAC6抑制剂,其IC50值针对HDAC6为150 nM,相比于HDAC8(1400 nM)和HDAC4(2300 nM)显示出较高的抑制活性。此化合物对人类癌细胞系展现出显著的细胞毒性,常用于癌症的研究领域。 | |||
T78839 |
HDAC6-IN-19
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-19(Compound 14g)是一种选择性HDAC6抑制剂,具有2.68 nM的IC50值。同时,该化合物对HDAC1、HDAC2和HDAC3也表现出一定的抑制作用,其IC50值分别为61.6 nM、98.7 nM和103 nM。此外,HDAC6-IN-19在抑制包括白血病、结肠癌、黑色素瘤和乳腺癌等多种癌细胞系的增殖方面显示出有效性。 | |||
T82224 |
HDAC6-IN-25
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6-IN-25(化合物8)作为高选择性HDAC6抑制剂,其IC50值达0.6 nM。 | |||
T62046 |
HDAC6-IN-5
|
||
HDAC6-IN-5 (化合物 11b) 是有效的、血脑屏障通透性的 HDAC6抑制剂(IC50= 0.025 μM)。HDAC6-IN-5 抑制 AChE 活性和 Aβ1-42自聚集和,IC50分别为 0.88 和 1.1 μM。HDAC6-IN-5 能够促进神经突起生长,且无明显神经毒性。 | |||
T61888 | mTOR/HDAC6-IN-1 | ||
mTOR/HDAC6-IN-1 是一种有效的组蛋白去乙酰酶 (HDAC6)和哺乳动物雷帕霉素 (mTOR) 的双重抑制剂,对于HDAC6 和 mTOR 的IC50值分别为56 nM 和133.7 nM。mTOR/HDAC6-IN-1 对细胞自噬 (autophagy)、细胞凋亡 (apoptosis)具有明显的诱导作用,对迁移具有抑制作用。mTOR/HDAC6-IN-1 在三阴性乳腺癌 (TNBC) 的研究中具有潜力 | |||
T78799 | BChE/HDAC6-IN-1 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
BChE/HDAC6-IN-1为高效的BChE及HDAC6选择性双重抑制剂,具有分别为4 nM与8.9 nM的IC50值。在aβ1-42诱导的小鼠模型中,BChE/HDAC6-IN-1能够改善认知功能障碍,显示出在阿尔茨海默病(AD)研究中的应用潜力。 | |||
T77922 |
HDAC6 degrader-1
|
PROTACs | PROTAC |
HDAC6Degrader-1是一种PROTAC,融合了作为HDAC6结合剂的Nexturastat A(Nex A)选择性抑制剂,连接肽及E3泛素连接酶配体。该化合物显著促进HDAC6降解,具备对其他HDAC亚型的高选择性,并有效抑制细胞增殖。 | |||
T64187 |
HDAC1/6-IN-1
|
||
HDAC1/6-IN-1 是一种有效的 GLP (IC50: 1.3 nM)、HDAC6 (IC50: 13 nM) 和 HDAC1 (IC50: 89 nM)的多靶点抑制剂。HDAC1/6-IN-1 能在蛋白水平上抑制 H3K9 的甲基化和去乙酰化。HDAC1/6-IN-1 能够将癌细胞的细胞周期阻滞在 G0/G1 期,能够诱导癌细胞凋亡,可阻止癌细胞迁移和入侵。 | |||
T74003 |
HDAC3/6-IN-2
|
||
HDAC3/6-IN-2 (化合物 15) 是一种高效的HDAC6和HDAC3抑制剂,IC50值分别为0.368 μM和0.635 μM。此化合物不仅具备抗肿瘤活性,能够诱导癌细胞凋亡,同时通过降低HDAC6和HDAC3水平,与H3乙酰化和α-微管蛋白的上调有关。 | |||
T75017 | PROTAC HDAC6 degrader 1 | ||
PROTACHDAC6 degrader (Compound A6) 为有效且选择性的PROTACHDAC6降解剂,具有3.5 nM的DC50。在髓系白血病细胞系中,通过诱导凋亡(apoptosis)表现出抗增殖活性。 | |||
T75018 |
HDAC6 degrader-3
|
PROTACs | PROTAC |
HDAC6degrader-3 是一种有效的选择性 HDAC6降解剂,通过三元复合物形成和泛素-蛋白酶体途径,IC50值为 19.4 nM。HDAC6degrader-3 对 HDAC6和 HDAC1的 IC50值分别为 4.54 nM 和 0.647 μM。HDAC6degrader-3 引起 α-微管蛋白的强烈高度乙酰化。 | |||
T61315 | HDAC6/HSP90-IN-2 | ||
HDAC6/HSP90-IN-2 (compound 6e) 是HDAC6和Hsp90的双抑制剂其IC50s 分别为106 nM 和61 nM。HDAC6/HSP90-IN-2 (compound 6e) 可用于癌症的研究。 | |||
T63531 |
HDAC6/HSP90-IN-1
|
||
HDAC6/HSP90-IN-1 是有效的、选择性的 HDAC6 (IC50: 4.3 nM) 和 HSP90 (IC50: 46.8 nM) 的双重抑制剂。HDAC6/HSP90-IN-1 能够下调 INF-γ 处理的 H1975 肺癌细胞中 PD-L1 的表达。HDAC6/HSP90-IN-1 在 H1975 异种移植小鼠中表现出肿瘤生长的抑制作用。 | |||
T79710 |
PI3Kα/HDAC6-IN-1
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
PI3Kα/HDAC6-IN-1(化合物21j)是一种针对PI3Kα/HDAC6的双重抑制剂,其IC50值分别为2.9 nM和26 nM。该化合物还能抑制AKT(Ser473)的磷酸化,诱导α-微管蛋白的积累,并促进其乙酰化,但对乙酰化组蛋白H3和H4无显著影响。在L-363细胞系中,PI3Kα/HDAC6-IN-1显示了高效的抑制活性(IC50=0.17 μM),表现出良好的抗癌潜力。 | |||
T61727 |
HDAC6/8/BRPF1-IN-1
|
||
HDAC6/8/BRPF1-IN-1 is a dual inhibitor that targets HDAC6, HDAC8, and the bromodomain and PHD finger containing protein 1 (BRPF1). It exhibits inhibitory activity against HDAC1, HDAC6, and HDAC8 with IC50 values of 797 nM, 344 nM, and 908 nM, respectively. In addition, it inhibits BRPF1 with a Kd value of 175.2 nM. This compound is utilized in cancer research [1]. | |||
T2294 |
BG45
|
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
BG45是一个 HDAC I 型抑制剂,选择性抑制 HDAC3,IC50为289 nM。它抑制 HDAC1/2/6的效力大大降低,IC50分别为2、2.2和>20μM。 | |||
T77664 |
KH16
|
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
KH16 是一种高效的 HDAC 抑制剂,特异性靶向I类HDACs(HDAC1, HDAC2及HDAC3),IC50值介于6至34 nM之间。KH16 能够激发细胞凋亡,并能够抑制多种肿瘤细胞中的基因表达模式。 | |||
T6865 |
Quisinostat dihydrochloride
Quisinostat 2HCl,Quisinostat (JNJ-26481585) 2HCl,JNJ26854165(Quisinostat) 2HCl,JNJ-26481585 2HCl |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) 是一种有口服活性,高效的 pan-HDAC 抑制剂,具有广泛的抗肿瘤活性。它对 HDAC1、HDAC2、HDAC4、HDAC10和HDAC11 的IC50值分别为 0.11 nM、0.33 nM、0.64 nM、0.46 nM 和 0.37 nM。 | |||
T62545 |
HDAC-IN-43
|
||
HDAC-IN-43 是一种强效的 HDAC 1/3/6 抑制剂,对 HDAC 1、HDAC 3 和 HDAC 6 的 IC50 值分别为 82 nM、45 nM 和 24 nM。HDAC-IN-43 是一种弱的 PI3K/mTOR 抑制剂,对 PI3K 和 mTOR 的 IC50 值分别为 3.6 μM 和 3.7 μM。HDAC-IN-43 具有广谱的抗增殖效果。 | |||
T62920 |
HDAC-IN-38
|
||
HDAC-IN-38 是一种 HDAC 的有效抑制剂。HDAC-IN-38 对 HDAC1、2、3、5、6 和 8 具有类似的微摩尔抑制作用,也可以提高组蛋白乙酰化水平 (H3K14 或 H4K5)。HDAC-IN-38 能够提高脑血流量 (CBF),减轻认知障碍,改善海马萎缩。 | |||
T61510 | PIM-1/HDAC-IN-1 | ||
PIM-1/HDAC-IN-1 (compound 4d) is a potent inhibitor of PIM-1, with an IC 50 of 343.87 nM. It also exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC 50 values of 63.65 and 62.39 nM, respectively. Furthermore, PIM-1/HDAC-IN-1 demonstrates apoptosis-inducing potential in MCF-7 cell lines, specifically inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase [1]. | |||
T61583 | CDK/HDAC-IN-1 | ||
CDK/HDAC-IN-1 exhibits potent inhibitory activity towards CDK2/4/6 and HDAC6, with IC50 values of 60.9 ± 2.9 nM, 276 ± 22.3 nM, 27.2 ± 4.2 nM, and 128.6 ± 0.4 nM, respectively. | |||
T79674 |
HDAC-IN-64
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-64 (Compound 13) 为HDAC抑制剂,对HDAC4/6的IC50值为24 nM及85 nM。其对前列腺癌(PCA)细胞表现出抗增殖与抗迁移效果,并能抑制LNCaP和RWPE-1细胞的生长,GI50值分别达到0.32 μM与1.1 μM。 | |||
T78708 |
JAK/HDAC-IN-2
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK/HDAC-IN-2 是一款高效的 JAK/HDAC 双靶点抑制剂,能在纳摩尔浓度范围内有效抑制 HDAC3/6 与 JAK1/2。此化合物不仅促进细胞凋亡,还能抑制组蛋白去乙酰化和 STAT3 磷酸化,对血液肿瘤和实体肿瘤细胞展现出了显著的抗增殖效果。 | |||
T74783 | HDAC-IN-53 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-53是一种口服活性的选择性HDAC1-3抑制剂,其IC50分别为47 nM、125 nM和450 nM。该化合物不针对II类HDAC(HDAC4、5、6、7、9;IC50>10 μM)展现抑制作用。HDAC-IN-53能够诱导caspase依赖的细胞凋亡并在裸鼠中显著抑制人肿瘤异种移植物生长,同时抑制携带MC38结肠癌的免疫活性小鼠的肿瘤发展。 | |||
T83947 |
HDAC4 CHDI Degrader 11
|
||
HDAC4 CHDI Degrader 11是一种高效且选择性的HDAC4降解剂(PROTAC),其在Jurkat E6-1细胞和Jurkat细胞中的DC50值分别为4 nM和6 nM。该化合物由类IIa HDAC抑制剂三氟甲基噁二唑通过连接体与Von Hippel-Lindau (VHL) 蛋白的配体连接而成。在亨廷顿病小鼠细胞模型中,HDAC4 CHDI Degrader 11能强效地降解HDAC4(DC50= 1nM)。在神经母细胞瘤细胞系中,可与P-糖蛋白抑制剂Elacridar联用以实现更有效的降解。 | |||
T36629 | Givinostat | ||
Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1... |