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Cat. No. Product Name Target Signaling Pathways
T17204 UNC0321

Histone Methyltransferase Chromatin/Epigenetic
UNC0321 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,在 ECSD 和 CLOT 测定中,Ki 为 63 pM,IC50 分别为 9 nM 和 6 nM。 UNC0321 抑制 GLP,在 ECSD 和 CLOT 试验中 IC50 分别为 15 nM 和 23 nM。
T7378 BRD9539

Histone Methyltransferase Chromatin/Epigenetic
BRD9539 是一种组蛋白甲基转移酶G9a 抑制剂,IC50为 6.3 μM,还抑制PRC2活性。
T17203 UNC0224

Histone Methyltransferase Chromatin/Epigenetic
UNC0224 是 G9a 的特异性抑制剂,Ki 为 2.6 nM,IC50 为 15 nM。 UNC0224 还有效抑制 GLP,IC50 值为 20-58 nM。
T1923 BRD4770

Histone Methyltransferase Chromatin/Epigenetic
BRD4770 是组蛋白甲基转移酶G9a 抑制剂,可激活共济失调毛细血管扩张突变途径并诱导细胞衰老。它可抑制H3K9的二甲基和三甲基化,EC50为 5 µM。
T14991 CMS-121

CMS121

Acetyl-CoA Carboxylase Metabolism
CMS-121 是喹诺酮衍生物,对乙酰辅酶 A 羧化酶 1 具有抑制作用,具有口服活性。CMS-121具有保护 HT22 细胞免受缺血和氧化损伤的活性,EC50分别为7 nM 和200 nM。CMS-121具有强大的抗炎,抗氧化,神经保护和肾保护作用。
T6593 ML324

Histone Demethylase; Others; HSV Chromatin/Epigenetic; Microbiology/Virology; Others
ML324 是 jumonji 组蛋白去甲基化酶的特异性抑制剂,IC50值为920 nM。
T4328 OSS_128167

SIRT6-IN-1

HBV; Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology
OSS_128167 (SIRT6-IN-1) 是一种选择性沉默调节蛋白 6 (SIRT6) 抑制剂,对 SIRT6,SIRT1 和 SIRT2 的 IC50分别为 89 μM,1578 μM 和 751 μM。它具有抗 HBV、抗癌、抗炎和抗病毒活性,可抑制 HBV 的转录和复制。
T77697 BML-278

BML278,BML 278

Sirtuin; Histone Methyltransferase Chromatin/Epigenetic; DNA Damage/DNA Repair
BML-278 是一种 SIRT1 激活剂 ,EC150 值为 1 μM。BML-278 增加父本和母本原核中的 H3K9 甲基化并抑制 H3K9 乙酰化,可用于改善早期胚胎发育。BML-278 促使原代人间充质细胞的细胞周期停止在 G1/S 期,可用于延缓衰老。BML-278 减少 U937 细胞中的微管蛋白乙酰化,增加小鼠 C2C12 成肌细胞的线粒体密度。
T24793 SIRT6-IN-5

SIRT6 inhibitor5,SIRT6 IN 5,SIRT6 inhibitor-5,SIRT6 inhibitor 5

Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair
SIRT6-IN-5(SIRT6 inhibitor 5) 是一种具有有效性和选择性的 SIRT6 抑制剂 ,IC50 值为 34 μM。SIRT6-IN-5 具有免疫抑制和化疗增敏作用,可增加 H3K9 的乙酰化并增加培养细胞中的葡萄糖摄取,减少 T 细胞增殖。
T21715 BRD6688

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
BRD6688 为 HDAC2 的选择性抑制剂。本品可使原代小鼠神经元细胞中的 H4K12 和 H3K9 组蛋白的乙酰化作用增强。在 CK-p25 小鼠模型中,它可透过血脑屏障,并改善由p25 引起的神经退行性病变相关的记忆缺陷。
T69937 INCB059872 tosylate

INCB059872, also known as INCB59872, is a potent, selective, and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively, through amine oxidation. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. In addition, LSD...
T38774 E67-2

E67-2

E67-2, a derivative of E67, is a low-toxicity, selective inhibitor of the KIAA1718 Jumonji domain. It has an IC 50 value of 3.4 μM. E67-2 specifically inhibits the Jumonji demethylase for histone H3 lysine 9 (H3K9) and histone H3 lysine 4 (H3K4) demethylase.
T39799 S2157

S2157

S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted...
T79713 JMJD3/HDAC-IN-1

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
JMJD3/HDAC-IN-1 (compound A5b) 是靶向 JMJD3 和 HDAC1(IC50=16 nM)的双重抑制剂。它能够促进 H3K27 高甲基化和 H3K9 高乙酰化,并通过裂解 caspase-7 和 PARP 导致细胞凋亡。此外,JMJD3/HDAC-IN-1 对抑制癌细胞克隆形成、迁移和侵袭也表现出有效性。
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。
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...
T79714 HDAC3-IN-2

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
HDAC3-IN-2 (compound 4i) 是一种具有纳摩尔级效力的吡嗪酰肼基HDAC3抑制剂,IC50值为14 nM,针对三阴性乳腺癌细胞表现出高效抑制作用。该化合物在细胞内毒性测定中显示,对4T1细胞株的IC50为0.55 μM,对MDA-MB-231细胞株的IC50为0.74 μM。HDAC3-IN-2通过增加乙酰化水平(如H3K9、H3K27和H4K12),促进细胞凋亡(涉及caspase-3、caspase-7和细胞色素c的水平提升),并抑制细胞增殖相关蛋白(如Bcl-2、CD44、EGFR和Ki-67)的表达,从而在荷瘤小鼠模型中表现出显著的体内抗肿瘤作用。
T63935 Bomedemstat hydrochloride

Bomedemstat (IMG-7289) hydrochloride 是一种口服具有活力的、不可逆的 lysine-specific demethylase 1(LSD1) 抑制剂。Bomedemstat hydrochloride 能够增加 H3K4 和 H3K9 的甲基化,并改变基因表达。Bomedemstat hydrochloride 能够抑制癌细胞增殖并诱导细胞凋亡,表现出抗癌效果。

化合物

UNC0321
Cat.No: T17204
Synonym:
Target: Histone Methyltransferase
BRD9539
Cat.No: T7378
Synonym:
Target: Histone Methyltransferase
UNC0224
Cat.No: T17203
Synonym:
Target: Histone Methyltransferase
BRD4770
Cat.No: T1923
Synonym:
Target: Histone Methyltransferase
CMS-121
Cat.No: T14991
Synonym: CMS121
Target: Acetyl-CoA Carboxylase
ML324
Cat.No: T6593
Synonym:
Target: Histone Demethylase, Others, HSV
OSS_128167
Cat.No: T4328
Synonym: SIRT6-IN-1
Target: HBV, Sirtuin
BML-278
Cat.No: T77697
Synonym: BML278,BML 278
Target: Sirtuin, Histone Methyltransferase
SIRT6-IN-5
Cat.No: T24793
Synonym: SIRT6 inhibitor5,SIRT6 IN 5,SIRT6 inhibitor-5,SIRT6 inhibitor 5
Target: Sirtuin
BRD6688
Cat.No: T21715
Synonym:
Target: HDAC
INCB059872 tosylate
Cat.No: T69937
Synonym:
Target:
E67-2
Cat.No: T38774
Synonym: E67-2
Target:
S2157
Cat.No: T39799
Synonym: S2157
Target:
JMJD3/HDAC-IN-1
Cat.No: T79713
Synonym:
Target: HDAC
HDAC1/6-IN-1
Cat.No: T64187
Synonym:
Target:
S2116
Cat.No: T39800
Synonym:
Target:
HDAC3-IN-2
Cat.No: T79714
Synonym:
Target: HDAC
Bomedemstat hydrochloride
Cat.No: T63935
Synonym:
Target:
TargetMol Loading
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