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。 |