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Cat. No. | Product Name | Target | Signaling Pathways |
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T3661 |
Citarinostat
ACY241,HDAC-IN-2 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Citarinostat (ACY241) 是一种强效、选择性和口服组蛋白脱乙酰酶 (HDAC) 抑制剂,具有抗肿瘤活性,对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50分别为 35、45、46、2.6 和 137 nM。 | |||
T39567 |
HDAC1/2-IN-3
HDAC1/2-IN-3 |
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HDAC1/2-IN-3 is an inhibitor of both HDAC1 and HDAC2, demonstrating IC50 values of 0-5 nM and 5-10 nM, respectively. | |||
T63664 |
CDK/HDAC-IN-2
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CDK/HDAC-IN-2 是有效的 HDAC/CDK 双重抑制剂,能够作用于 HDAC1 (IC50: 6.4 nM)、HDAC2 (IC50: 0.25 nM)、HDAC3 (IC50: 45 nM)、HDAC6,8 (IC50>1000 nM)、CDK1 (IC50: 8.63 nM)、CDK2 (IC50: 0.30 nM)、CDK4,6,7 (IC50>1000 nM)。CDK/HDAC-IN-2 能够将细胞周期停滞在 G2/M 期,并诱导细胞凋亡 (apoptosis)。CDK/HDAC-IN-2 具有优异的抗增殖效果,显示出显著的抗肿瘤作用。 | |||
T64025 | Top/HDAC-IN-2 | ||
Top/HDAC-IN-2 (45b) 是 Top 和 HDAC 的双重抑制剂,能够诱导细胞凋亡,表现出显著的抗肿瘤作用。 | |||
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。 | |||
T79452 |
Tubulin/HDAC-IN-2
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Tubulin/HDAC-IN-2 (Compound II-19k) 为Tubulin和HDAC的双重抑制剂,IC50分别对HDAC1、HDAC2、HDAC3和HDAC6为0.403 μM、0.591μM、3.552μM和0.459μM。该化合物能够导致细胞周期在G2期的阻滞及诱导细胞凋亡。Tubulin/HDAC-IN-2 有效抑制血肿和实体瘤细胞增殖,降低肿瘤转移,并在肝肿瘤同种异体移植的小鼠模型中抑制肿瘤生长。 | |||
T62717 |
A2AAR/HDAC-IN-2
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A2AAR/HDAC-IN-2 是一种有效的 A2AAR/HDAC 双重抑制剂。A2AAR/HDAC-IN-2 对 A2AAR 表现出良好的亲和力 (Ki:10.3 nM), 能够良好的抑制 HDAC1 (IC50:18.5 nM). A2AAR/HDAC-IN-2 能够用于研究抗肿瘤。 | |||
T62912 |
PI3K/HDAC-IN-2
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PI3K/HDAC-IN-2 是一种有效的 PI3K/HDAC 双重抑制剂,能够作用于 PI3Kα (IC50: 226 nM)、PI3Kβ (IC50: 279 nM)、PI3Kγ (IC50: 467 nM)、PI3Kδ (IC50: 29 nM)、HDAC1 (IC50: 1.3 nM)、HDAC2 (IC50: 3.4 nM)、HDC4 (IC50: 973 nM)、HDAC6 (IC50: 17 nM)、HDAC8 (IC50: 12 nM)。PI3K/HDAC-IN-2 具有 PI3Kδ 和 I 类和 IIb 类 HDAC 选择性,并表现出显着的抗癌作用。 | |||
T72759 | c-Met/HDAC-IN-2 | ||
c-Met/HDAC-IN-2 是一种高效的c-Met 和HDAC 双重抑制剂,对HDAC1与c-Met 的IC50分别为 18.49 nM 和 5.40 nM。c-Met/HDAC-IN-2 对几种癌细胞具有抗增殖活性。c-Met/HDAC-IN-2 能将 HCT-116 细胞周期阻滞在 G2/M 期,诱导细胞凋亡 (apoptosis)。c-Met/HDAC-IN-2 可用于抗癌耐药研究。 | |||
T2025 |
HDAC-IN-7
HBI-8000,西达本胺杂质,CS055,Chidamide impurity |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-7 (HBI-8000) 是 Chidamide 的一种杂质。Chidamide 是一种可口服的 HDAC 酶 I 类 HDAC1/2/3 和 IIb 类 HDAC10 抑制剂。 | |||
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。 | |||
T5631 |
SIS17
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
SIS17 是一种有效的选择性 HDAC 11 抑制剂,IC50 值为 0.83 μM。它可抑制 HDAC11 底物丝氨酸羟甲基转移酶 2 的去肉豆蔻酰化。 | |||
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。 | |||
T61916 | HDAC-IN-35 | ||
HDAC-IN-35 (Compound 14) 是有效的、选择性的VEGFR-2和HDAC 抑制剂,对VEGFR-2和HDAC6的IC50值分别为13.2和0.166 μM。 | |||
T62072 | HDAC-IN-47 | ||
HDAC-IN-47 是一种口服具有活力的组蛋白去乙酰化酶 (HDAC) 的抑制剂,对 HDAC1、HDAC2、HDAC3、HDAC6、HDAC8 的 IC50 值分别为 19.75 nM、57.8 nM、40.27 nM、5.63 nM、302.73 nM。HDAC-IN-47 可以将细胞周期阻滞在 G2/M 期,抑制细胞自噬,能够利用 Bax/Bcl-2 和 caspase-3 通路诱导凋亡,在体内具有抗癌活性。 | |||
T63142 | AChE/HDAC-IN-1 | ||
COX-2-IN-23 (compound A10) 是一种有效的 AChE (IC50: 0.12 nM) 和 HDAC (IC50: 0.23 nM) 抑制剂。COX-2-IN-23 表现出抗氧化作用和金属螯合特性。COX-2-IN-23 能够用于研究阿尔兹海默病。 | |||
T80873 | VEGFR2/HDAC1-IN-1 | VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR2/HDAC1-IN-1(compound 13)是一款有效的VEGFR-2和HDAC双重抑制剂,其IC50值分别为57.83 nM 和9.82 nM 。该化合物能够阻滞细胞周期于S期及G2期,并能诱导HeLa细胞发生凋亡,同时具有抗血管生成的特性。 | |||
T71110 |
Nanatinostat TFA
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Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor... | |||
T81974 |
KPZ560
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
KPZ560作为HDAC1和HDAC2的有效抑制剂,在IC50数值上分别达到12 nM 和68 nM 。此化合物能提升小鼠颗粒神经元树突的棘密度,同时也能抑制MCF乳腺癌细胞系的生长。 | |||
TP1836 |
BMf-BH3
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BMf-BH3 belongs to the Bcl-2 apoptosis mediator family. This peptide belongs to the Bcl-2 apoptosis mediator family. Bmf is a key player in histone deacetylase (HDAC) inhibition, which alters the balance between deacetylation and acetylation. | |||
T74456 | JPS036 | ||
JPS036 是一种基于苯甲酰胺的Von Hippel-Lindau (VHL)E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。JPS036 降解 I 类组蛋白脱乙酰酶 (HDAC)。JPS036 是一种有效的 HDAC1/2 降解剂,与 HCT116 细胞中更大的总差异表达基因和增强的细胞凋亡 (apoptosis) 相关。 | |||
T74454 | JPS016 | ||
JPS016 是一种基于苯甲酰胺的Von Hippel-Lindau (VHL)E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。JPS016 降解 I 类组蛋白脱乙酰酶 (HDAC)。JPS016 是一种有效的 HDAC1/2 降解剂,与 HCT116 细胞中更大的总差异表达基因和增强的细胞凋亡 (apoptosis) 相关。 | |||
T77938 |
JPS016 TFA
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
JPS016 TFA是一种苯甲酰胺基Von Hippel-Lindau (VHL) E3连接酶蛋白水解靶向嵌合体(PROTAC)。该化合物能够降解I类组蛋白脱乙酰酶(HDAC),特别是有效地降解HDAC1/2。在HCT116细胞中,JPS016 TFA与大量差异基因表达增加及细胞凋亡(apoptosis)激活相关。 | |||
T74453 | JPS014 | ||
JPS014, 基于苯甲酰胺的Von Hippel-Lindau (VHL) E3-连接酶蛋白水解靶向嵌合体 (PROTAC),有效降解I 类组蛋白脱乙酰酶 (HDAC)。它作为HDAC1/2的强效降解剂,与HCT116细胞中的总差异表达基因更大和增强的细胞凋亡 (apoptosis) 密切相关。 | |||
T36110 |
L-Pyrohomoglutamic Acid
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L-Pyrohomoglutamic acid is an amino acid building block.1,2It has been used in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. 1.Pomplun, S., Wang, Y., Kirschner, A., et al.Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)Angew. Chem. Int. Ed.54(1)345-348(2015) 2.Taddei, M., Cini, E., Giannotti, L., et al.Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors... | |||
T38711 |
YF-2 hydrochloride
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YF-2 hydrochloride is a potent histone acetyltransferase activator that exhibits high selectivity and can pass through the blood-brain barrier. It specifically acetylates H3 in the hippocampus, with EC50 values of 2.75 μM, 29.04 μM, and 49.31 μM for CBP, PCAF, and GCN5, respectively. Notably, it does not affect HDAC activity. Moreover, YF-2 hydrochloride demonstrates promising anti-cancer and anti-Alzheimer's disease properties. | |||
T36102 |
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline
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4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline is a building block and synthetic intermediate.1,2,3,4,5It has been used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer compounds.1,2,3It is also a synthetic intermediate in the synthesis of EGFR inhibitors, including erlotinib , with antiproliferative activity.4,5 | |||
T77937 |
JPS014 TFA
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
JPS014 TFA是一种VHL E3连接酶蛋白水解靶向嵌合体(PROTAC),以苯甲酰胺为基础,专门降解I类组蛋白脱乙酰酶(HDAC)。作为一种高效的HDAC1/2降解剂,JPS014 TFA与HCT116细胞中广泛的基因表达差异及促进细胞凋亡(apoptosis)密切相关。 | |||
T79683 |
HDAC/CD13-IN-1
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Others | Others |
HDAC/CD13-IN-1 (Compound 12) 作为HDAC/CD13抑制剂, 对hCD13的IC50为0.34 μM, 猪CD13为0.53 μM, 对HDAC1/2/3的IC50分别为0.03、0.06、0.02 μM。此化合物有效抑制MV4-11、K562、Jeko-1 和 HL60细胞增殖, IC50范围为0.25-2.04 μM,并诱导癌细胞凋亡。同时表现出抗转移和抗侵袭的特性。 | |||
T21898 |
MI-192
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MI-192 是一种选择性 HDAC2和 HDAC3抑制剂,IC50分别为 30 nM 和 16 nM。MI-192 比其他 HDAC 异构体对 HDAC2/3 具有更高选择性。MI-192 诱导髓系白血病细胞凋亡 (apoptosis)。抗癌和神经保护活性。 | |||
T74455 |
JPS035
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JPS035 是一种基于苯甲酰胺的Von Hippel-Lindau (VHL)E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。JPS035 降解 I 类组蛋白脱乙酰酶 (HDAC)。JPS035 是一种有效的 HDAC1/2 降解剂,与 HCT116 细胞中更大的总差异表达基因和增强的细胞凋亡 (apoptosis) 相关。 | |||
T21719 |
CBHA
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m-Carboxycinnamic acid bishydroxamide 是一种有效的HDAC 抑制剂,在体外对 HDAC1 和 HDAC3 的ID50值分别为 10 nM 和 70 nM。m-Carboxycinnamic acid bishydroxamide 也可诱导细胞凋亡并且抑制肿瘤生长。 | |||
T70962 | MHY219 | ||
MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. M... | |||
T64152 | Purinostat mesylate | ||
Purinostat mesylate 是一种选择性的 HDAC 抑制剂。Purinostat mesylate 能够抑制 I 型和 IIb 型 HDACs (IC50: 0.81-11.5 nM)。Purinostat mesylate 能够影响LAMA84 和 188 BL-2 细胞的细胞周期,并诱导其凋亡,在体内显示出较强的抗白血病效果。Purinostat mesylate 能够用于研究淋巴细胞白血病。 | |||
T36421 | Immuno-Oncology Screening Library | ||
The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list ... | |||
T61753 |
MPT0G211 mesylate
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MPT0G211 mesylate is a powerful and selective HDAC6 inhibitor (IC50 = 0.291 nM), with high oral bioavailability. It exhibits remarkable selectivity for HDAC6 over other HDAC isoforms (>1000-fold selectivity). Additionally, MPT0G211 mesylate can effectively cross the blood-brain barrier. In preclinical studies using an Alzheimer's disease model, MPT0G211 mesylate has shown promising results in reducing tau phosphorylation and cognitive deficits. Furthermore, this compound exhibits anti-metastatic... | |||
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... | |||
T36103 |
TW9
TW9 |
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TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistica... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T7064 |
Valproic Acid
Sodium valproate,2-Propylpentanoic Acid,丙戊酸,VPA,Depakine,2-Propylvaleric Acid |
Mitophagy; Gamma-secretase; HIV Protease; GABA Receptor; Sodium Channel; HDAC; Autophagy | Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells |
Valproic Acid (2-Propylpentanoic Acid) 是一种 HDAC 抑制剂,可抑制 HDAC1 活性,诱导 HDAC2 降解,具有口服活性。Valproic Acid 可以用于癫痫和躁郁症的研究。 | |||
T36797 | 1-Alaninechlamydocin | ||
1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp. and an inhibitor of histone deacetylases (HDACs). It reduces total HDAC activity in HeLa cell lysates in a concentration-dependent manner. 1-Alaninechlamydocin reduces proliferation of MIA PaCa-2, PANC-1, and hTERT-HPNE cells (GI50s = 5.3, 14, and 2.0 nM, respectively). |