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Search Results for " deacetylation "

24

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6111	Selisistat EX-527,司来司他,SEN0014196	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Selisistat (EX-527) 是一种去乙酰化酶 SIRT1 的抑制剂 (IC50=38 nM)，具有有效性和特异性。Selisistat 可以用于神经系统疾病如亨廷顿舞蹈病的研究。
T9320	YK-3-237 B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	YK-3-237 (B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid) 是 SIRT1 激活剂，靶向突变体 p53。它抑制三阴性乳腺癌细胞的增殖。
T20080	Exifone NSC 680919,NSC680919,NSC-680919,依昔苯酮	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Exifone (NSC-680919) 是一种混合的、非必需的 HDAC1 激活剂，能够与游离酶和底物结合酶结合，从而提高 HDAC1 催化的去乙酰化的相对最大速率。
T4062	CAY10602	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	CAY10602 是一种SIRT1激活剂，可剂量依赖性地抑制 THP-1 细胞中脂多糖对 TNF-α 的 NF-κB 依赖性诱导。
T64529	MDL-800 MDL 800,MDL800	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT6, responsible for deacetylation of histone H3 Nε-acetyl-lysines 9 (H3K9ac) and 56 (H3K56ac), is a tumor suppressor which has frequently been found to have low expression in various cancers. MDL-800 is a selective SIRT6 activator. It increased the deacetylase activity of SIRT6 by up to 22-fold and led to a global decrease in H3K9ac and H3K56ac levels in human hepatocellular carcinoma (HCC) cells. Also, it inhibited the proliferation of HCC cells via SIRT6-driven cell-cycle arrest and was eff...
T69707	MDL-801
	MDL-801 is an activator of SIRT6 deacetylation.
T28853	SRTCX1003 SRTCX-1003,SRTCX 1003
	SRTCX1003, a SIRT1 activator, suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB activity.
T26226	SRTCX1002 SRTCX 1002,SRTCX-1002
	SRTCX1002 is a SIRT1 Activator Suppressing Inflammatory Responses through Promotion of p65 Deacetylation and NF-κB Activity inhibitor.
T36686	Ac-Arg-Gly-Lys(Ac)-AMC
	Ac-RGK(Ac)-AMC, fluorogenic substrate for assaying histone deacetylase (HDAC) activity in a two-step enzymatic reaction. The assay consists of the initial lysine deacetylation by HDAC followed by the release of the fluorescent group by trypsin.
T14936	Ivaltinostat CG-200745	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	CG-200745 is a potent inhibitor of HDAC. CG200745 induces apoptosis and also inhibits the deacetylation of histone H3 and tubulin.
T39829	BPK-25
	BPK-25 is an active acrylamide compound that enhances the degradation of proteins in the nucleosome remodeling and deacetylation (NuRD) complex through a post-translational mechanism involving covalent protein interaction. Additionally, BPK-25 acts as an inhibitor of TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
TP1836	BMf-BH3
	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.
T81831	MDL-811	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	MDL-811为SIRT6的异构激活剂，有效促进SIRT6对组蛋白H3的去乙酰化作用（H3K9Ac, H3K18Ac, 和 H3K56Ac）。该化合物在结肠癌研究中有应用价值。
T39800	S2116
	S2116 is a powerful inhibitor of lysine-specific demethylase 1 (LSD1), and it is a derivative of N-alkylated tranylcypromine (TCP). S2116 exhibits its inhibitory effects by increasing H3K9 methylation and inducing reciprocal H3K27 deacetylation at super-enhancer regions. In TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells, S2116 triggers apoptosis by repressing the transcription of NOTCH3 and TAL1 genes. Furthermore, S2116 demonstrates significant growth retardation of T-ALL cells...
T61947	SIRT5 inhibitor 3
	SIRT5 inhibitor 3 (compound 46) 是有效的、竞争性的 SIRT5抑制剂（IC50= 5.9 μM），对 SIRT5 去乙酰化具有抑制作用。SIRT5 inhibitor 3 在癌症和神经退行性疾病中具有研究价值。
T70748	Bisthianostat
	Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. Thi...
T79565	Sirt1/2-IN-4	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Sirt1/2-IN-4（compound PS3）为SIRT1/2/3抑制剂，其IC50分别为1.2 μM (SIRT1)、1.9 μM (SIRT2) 和2.0 μM (SIRT3)。该化合物能完全阻制p53脱乙酰化作用，显示出潜在的抗癌活性。
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。
T79564	Sirt1/2-IN-3	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Sirt1/2-IN-3 (compound PS9) 作为SIRT1/2的双重抑制剂，其对SIRT1和SIRT2的IC50值分别为1.4 μM 和 2.0 μM。该化合物能够有效抑制p53脱乙酰化，并提升p53与α-微管蛋白的乙酰化水平。Sirt1/2-IN-3还能诱导细胞凋亡，并展现对人白血病细胞系的抗增殖效果。
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。
T79563	Sirt1/2-IN-2	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Sirt1/2-IN-2 (compound hsa55)是一种针对SIRT1/2的双重抑制剂，具有分别针对SIRT1和SIRT2的IC50值为1.8 μM和2.4 μM。该化合物能有效阻止p53的脱乙酰化作用，并提高p53及α-微管蛋白的乙酰化水平。此外，Sirt1/2-IN-2能诱导细胞凋亡，并展示出对人白血病细胞系的抗增殖效果。
T27534	Herkinorin BF3DNCA methyl ester
	Herkinorin is an opioid analgesic and an analogue of the natural product Salvinorin A. herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A. Herkinorin is a semi-synthetic c
T71110	Nanatinostat TFA
	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...
T63074	Ivaltinostat formic
	Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂，具有异羟肟酸部分，能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累，诱导 p53 依赖性反式激活，并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡，并具有抗肿瘤效果。

化合物

Cat.No: T6111

Synonym: EX-527,司来司他,SEN0014196

Target: Sirtuin

Cat.No: T9320

Synonym: B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid

Target: Sirtuin

Cat.No: T20080

Synonym: NSC 680919,NSC680919,NSC-680919,依昔苯酮

Target: HDAC

Cat.No: T4062

Target: Sirtuin

Cat.No: T64529

Synonym: MDL 800,MDL800

Target: Sirtuin

Cat.No: T69707

Cat.No: T28853

Synonym: SRTCX-1003,SRTCX 1003

Cat.No: T26226

Synonym: SRTCX 1002,SRTCX-1002

Ac-Arg-Gly-Lys(Ac)-AMC

Cat.No: T36686

Cat.No: T14936

Synonym: CG-200745

Target: HDAC

Cat.No: T39829

Cat.No: TP1836

Cat.No: T81831

Target: Sirtuin

Cat.No: T39800

SIRT5 inhibitor 3

Cat.No: T61947

Cat.No: T70748

Cat.No: T79565

Target: Sirtuin

Cat.No: T78708

Target: JAK

Cat.No: T79564

Target: Sirtuin

Cat.No: T64187

Cat.No: T79563

Target: Sirtuin

Cat.No: T27534

Synonym: BF3DNCA methyl ester

Nanatinostat TFA

Cat.No: T71110

Ivaltinostat formic

Cat.No: T63074

Cat. No.	Product Name	Target	Signaling Pathways
T9454	4-Hydroxyestrone	Estrogen Receptor/ERR; Endogenous Metabolite	Endocrinology/Hormones; Metabolism
	4-Hydroxyestrone 是一种内源性雌激素代谢物，可强烈保护神经元细胞免受氧化损伤。
TN2063	Physalin B NSC-287088	Apoptosis; NF-κB; Akt; PI3K; Nrf2; NOD	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; PI3K/Akt/mTOR signaling
	Physalin B 是茄科植物的主要活性化合物之一，具有广泛的生物活性，可用于治疗炎症湿疹和疱疹等疾病。Physalin B 通过激活 PI3K/Akt 通路抑制 NF-κB 和 NLRP3，从而改善脂多糖诱导的急性肺损伤造成的炎症反应。Physalin B 通过激活 Nrf2 通路抑制 PDGF-BB 诱导的 VSMC 增殖、迁移和表型转化。Physalin B 通过抑制 LAP2α-HDAC1 介导的胶质瘤相关癌基因 1 的去乙酰化和肝星状细胞活化来发挥抗肿瘤活性。

天然产物

4-Hydroxyestrone

Cat.No: T9454

Target: Estrogen Receptor/ERR, Endogenous Metabolite

Cat.No: TN2063

Synonym: NSC-287088

Target: Apoptosis, NF-κB, Akt, PI3K, Nrf2, NOD

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