Cat. No. | Product Name | Target | Signaling Pathways |
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T7082 |
HDAC8-IN-1
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC8-IN-1 是一种 HDAC8 抑制剂,在癌细胞系中的 IC50 为 27.2 nM,有抗增殖作用。 | |||
T62171 |
HDAC8/BRPF1-IN-1
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HDAC8/BRPF1-IN-1 (Compound 23a) 是一种双重的 HDAC8 和 BRPF1 抑制剂,能够作用于人 HDAC8 (IC50: 443 nM)、人 BRPF1 (Kd: 67 nM)。 HDAC8/BRPF1-IN-1 对 HDAC1 和 6 具有较低的体外活性。 | |||
T79082 |
HDAC8-IN-4
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC8-IN-4为HDAC8特异性抑制剂,对HDAC8及HDAC3具有抑制活性,IC50s值分别为0.15 μM与12 μM。 | |||
T61524 |
Tubulin/HDAC-IN-1
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Tubulin/HDAC-IN-1 is a compound that functions as a dual inhibitor for tubulin and HDAC-IN-1. It achieves this by interacting with tubulin through CH/π interaction and with HDAC8 through hydrogen bond interaction. This compound effectively inhibits tubulin polymerization and selectively targets HDAC8 with an IC50 of 150 nM. Additionally, Tubulin/HDAC-IN-1 demonstrates cytotoxicity against various human cancer cells, induces cell cycle arrest in the G2/M phase, and triggers cell apoptosis. This c... | |||
T61858 | HDAC8-IN-3 | ||
HDAC8-IN-3 (compound P19) is a highly potent inhibitor of HDAC8, displaying an IC50 value of 9.3 μM and producing thermal stabilization. Moreover, HDAC8-IN-3 exhibits cytotoxicity and induces apoptosis specifically in leukemic cell lines [1]. | |||
T61549 | HDAC8-IN-2 | ||
HDAC8-IN-2 (compound 5o) is a potent HDAC8 inhibitor, with IC50 values of 0.27 μM and 0.32 μM for smHDAC8 (Schistosoma mansoni histone deacetylase 8) and hHDAC8, respectively. It effectively kills schistosome larvae and greatly reduces egg laying in adult worm pairs [1]. | |||
T78861 |
HDAC8-IN-5
|
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。 | |||
T61727 |
HDAC6/8/BRPF1-IN-1
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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]. | |||
T63509 | Top/HDAC-IN-1 | ||
Top/HDAC-IN-1 是拓扑异构酶 (Top)/HDAC 双重抑制剂,能够作用于 HDAC1 (IC50: 18 nM)、HDAC2 (IC50: 230 nM)、HDAC3 (IC50: 790 nM)、HDAC6 (IC50: 87 nM) 和 HDAC8 (IC50: 5250 nM)。Top/HDAC-IN-1 对 HCT116 细胞表现出有效的抗肿瘤作用 (IC50: 180 nM),可将 HCT116 细胞的细胞周期阻滞 G2 期,有效诱导其凋亡 (apoptosis)。 | |||
T60856 |
HDAC6-IN-9
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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。 | |||
T62327 | HDAC2-IN-1 | ||
HDAC2-IN-1 (Compound 17) 是一种口服具有活力的、能够透过血脑屏障的、竞争性 HDAC2 抑制剂 (IC50: 0.5 μM)。HDAC2-IN-1 也能够抑制 HDAC1 (IC50: 1.61 μM) 和 HDAC8 (IC50: 0.98 μM)。 | |||
T63543 |
HDAC/Top-IN-1
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HDAC/Top-IN-1 是广谱的、口服具有活力的 HDAC/Top 双重抑制剂,能够作用于HDAC1 (IC50: 0.036 μM)、HDAC2 (IC50: 0.14 μM)、HDAC3 (IC50: 0.059 μM)、HDAC6 (IC50: 0.089 μM) 和 HDAC8 (IC50: 9.8 μM)。HDAC/Top-IN-1 能够将HEL 细胞的细胞阻滞在 S 期,并有效诱导细胞凋亡 (apoptosis)。 | |||
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]. | |||
T78769 |
HDAC6-IN-17
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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。 | |||
T75021 | SZUH280 | ||
SZUH280 是一种有效的、选择性的 PROTACHDAC8降解剂,在 A549 细胞中的 DC50为 0.58 μM。SZUH280 诱导癌细胞凋亡 (apoptosis)。SZUH280 在癌细胞中阻碍 DNA 损伤修复,促进细胞放射致敏。 | |||
T61451 | NMDAR/HDAC-IN-1 | ||
NMDAR/HDAC-IN-1 (Compound 9d) is a potent dual inhibitor of N-methyl-D-aspartate receptors (NMDARs) and histone deacetylases (HDACs). It exhibits a high affinity (Ki = 0.59 μM) for NMDARs, while demonstrating significant inhibitory effects on various HDAC isoforms, including HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC 50 values of 2.67 μM, 8.00 μM, 2.21 μM, 0.18 μM, and 0.62 μM, respectively. Moreover, NMDAR/HDAC-IN-1 efficiently crosses the blood-brain barrier [1]. | |||
T78880 |
Tubulin/HDAC-IN-3
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Tubulin/HDAC-IN-3(compound 12a)为一种高效的tubulin/HDAC汇合型抑制剂,能显著破坏微管蛋白聚合(IC50: 5.4 μM),并对HDAC1/8展现强效抑制作用,IC50值分别为0.155 μM和0.177 μM。该化合物通过阻断细胞周期、诱导细胞凋亡(apoptosis)及抑制集落形成以施展其生物学效用。 | |||
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。 |