Cat. No. | Product Name | Target | Signaling Pathways |
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T11543 | HDAC-IN-5 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor. | |||
T61433 | HDAC1-IN-5 | ||
HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1] | |||
T78861 |
HDAC8-IN-5
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC8-IN-5 (Compound 6a),一种HDAC8抑制剂,其半抑制浓度(IC50)为28 nM。该化合物主要适用于癌症研究领域。 | |||
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。 | |||
T63907 |
PDE5/HDAC-IN-1
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PDE5/HDAC-IN-1 是磷酸二酯酶 5 (PDE5) 和 HDAC 的有效抑制剂,他们的 IC50 值分别为 46.3 nM 和 14.5 nM。PDE5/HDAC-IN-1 能够诱导细胞凋亡(apoptosis),表现出抗癌效果。 | |||
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。 | |||
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。 | |||
T79371 |
HDAC-IN-62
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Autophagy | Autophagy |
HDAC-IN-62(Compound 5),是一款针对HDAC6/8/11的HDAC抑制剂,IC50分别为0.78、1.0、1.2μM。该化合物通过诱导自噬(Autophagy)来抑制微胶质细胞的激活,进而抑制一氧化氮产生,显示出抗炎和抗抑郁的效果。此外,HDAC-IN-62还能抑制实验小鼠大脑中的微胶质细胞活化。 | |||
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。 | |||
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。 | |||
T70779 | BPR1J-340 | ||
BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibit... | |||
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... |