Cat. No. | Product Name | Target | Signaling Pathways |
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T72012 |
HDAC-IN-6
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HDAC-IN-6 is an HDAC inhibitor, targeting HDAC2, HDAC3, HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9. | |||
T71587 |
Fluoxetine succinate ester
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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. | |||
T2294 |
BG45
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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
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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
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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
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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. | |||
T78708 |
JAK/HDAC-IN-2
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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。 | |||
T79674 |
HDAC-IN-64
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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。 | |||
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
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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... |