65
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T80947 | tri-GalNAc-COOH (acetylation) | LYTACs | PROTAC |
Tri-GalNAc-COOH acetylation 是一种对 tri-GalNAc-COOH 进行乙酰化和修饰的过程,该过程可用于LYTAC的合成。 | |||
T6421 |
BRD73954
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
BRD73954 是一种有效且特异性的 HDAC 抑制剂,对 HDAC6 和 HDAC8 的 IC50 分别为 36 nM 和 120 nM。 | |||
T11563 |
Histone Acetyltransferase Inhibitor II
|
Epigenetic Reader Domain; Histone Acetyltransferase | Chromatin/Epigenetic |
Histone Acetyltransferase Inhibitor II 是一种选择性的细胞渗透性 p300 组蛋白乙酰转移酶抑制剂,IC50值为 5 µM。它在哺乳动物细胞中具有抗乙酰化酶活性,可用于癌症研究。 | |||
T1818 |
Tenovin-6
Tenovin 6 |
Dehydrogenase; Sirtuin; Autophagy | Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism |
Tenovin-6 是 Tenovin-1 的类似物,能抑制二氢乳清酸脱氢酶。它也抑制纯化人 SIRT1、SIRT2 和 SIRT3 蛋白脱乙酰酶活性,IC50分别为 21 μM、10 μM 和 67 μM。它是一种 p53转录活性的激活剂。 | |||
T11807 |
L002
|
Others; Histone Acetyltransferase; STAT | Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells |
L002 是一种细胞可渗透的,可逆特定性乙酰转移酶 p300(KAT3B)抑制剂,IC50为 1.98 μM。 它结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域,阻断组蛋白乙酰化和 p53 乙酰化,且抑制 STAT3 激活,有用于高血压引起的心脏肥大和纤维化的研究潜力。 | |||
T1919 |
Tenovin-1
Tenovin 1 |
Mdm2; Dehydrogenase; Sirtuin; p53; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism |
Tenovin-1 抑制 SirT1 和 SirT2 的蛋白质去乙酰化活性,并防止 MDM2 介导的 p53 降解,这涉及泛素化。它具有癌症的研究潜力。 | |||
T13996 |
1-Naphthohydroxamic acid
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
1-Naphthohydroxamic acid 是一种选择性 HDAC8抑制剂,IC50为 14 μM。它对 HDAC8的选择性高于 I 类 HDAC1 和 II 类 HDAC6,IC50大于100 μM,可诱导微管蛋白乙酰化。 | |||
T5347 |
CXD101
CXD-101 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
CXD101 是一种选择性和具有口服活性的 I 类HDAC 抑制剂,有抗肿瘤活性,对HDAC1、HDAC2和HDAC3的IC50分别为 63、570 和 550 nM。 | |||
T23820 |
BRD32048
BRD-32048,BRD 32048 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
BRD32048 可以与与 ETV1直接结合,KD 为 17.1 μM。BRD32048调节 ETV1 介导的转录活性和 ETV1 驱动的癌细胞侵袭。 BRD32048可以抑制 ETV1 乙酰化并促进其降解。 | |||
T8480 |
Tenovin-6 Hydrochloride
|
Dehydrogenase; Sirtuin; HDAC; p53; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism |
Tenovin-6 Hydrochloride 是 Tenovin-1 的类似物,能抑制二氢乳清酸脱氢酶。它是一种 p53转录活性的激活剂,抑制纯化人 SIRT1、SIRT2 和 SIRT3 蛋白脱乙酰酶活性,IC50分别为 21 μM、10 μM 和 67 μM。 | |||
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。 | |||
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。 | |||
T60065 |
WAY-118959-A
|
Microtubule Associated | Cytoskeletal Signaling |
WAY-118959-A 是一种潜在的微管乙酰化抑制剂。 | |||
T19717 |
Cyclo-L-Trp-L-Trp
|
Antifungal | Microbiology/Virology |
Cyclo-L-Trp-L-Trp 是一种广谱抗真菌剂。它还诱导组蛋白的高度乙酰化。 | |||
T0538 |
3-Methylindolin-2-one
3-Methyloxindole,3-Methyl-2-oxindole,3-甲基羟基吲哚 |
Others; Endogenous Metabolite | Metabolism; Others |
3-Methylindolin-2-one (3-Methyloxindole) 是内源性代谢产物的一种。 | |||
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。 | |||
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。 | |||
T28543 |
RK-9123016
RK9123016,RK 9123016 |
Sirtuin | Chromatin/Epigenetic; DNA Damage/DNA Repair |
RK-9123016是一种SIRT2抑制剂。RK-9123016增加真核翻译起始因子5A(eIF5A)(SIRT2的生理底物)的乙酰化水平,降低人乳腺癌细胞的细胞活力,同时降低c-Myc 表达。 | |||
T4353 |
SR-18292
SR 18292 |
Autophagy | Autophagy; Metabolism |
SR-18292 是一种 PPARγ 共激活因子-1α (PGC-1α) 抑制剂,可增加 PGC-1α 乙酰化,抑制糖异生基因表达并减少肝细胞中的葡萄糖生成。 | |||
T16409 |
OSMI-1
|
Others; Acyltransferase | Metabolism; Others |
OSMI-1 是一种 O-GlcNAc 转移酶 (OGT) 抑制剂 (IC50=2.7 μM),具有口服活性和细胞渗透性。OSMI-1 可以抑制蛋白质 O-GlcNA 酰化,而不会定性地改变细胞表面 N- 或 O- 连接的聚糖。 | |||
T23095 |
NU 9056
NU9056 |
Histone Acetyltransferase | Chromatin/Epigenetic |
NU 9056 是一种有效且选择性的 KAT5 组蛋白乙酰转移酶抑制剂,IC50 为 2 µM。 NU 9056 阻断 DNA 损伤反应并抑制前列腺癌细胞系中的蛋白质乙酰化。 | |||
T27083 |
Crebinostat
|
Epigenetic Reader Domain; Histone Acetyltransferase; HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂,对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用, IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性,增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化,并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。 | |||
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。 | |||
T24131 |
HDAC3-IN-T247
HDAC3 inhibitor T247,HDAC3 inhibitor-T247,HDAC3 IN T247,T247 |
Histone Demethylase; Antiviral | Chromatin/Epigenetic; Immunology/Inflammation |
HDAC3-IN-T247 (HDAC3 inhibitor T247) 是一种具有选择性和有效性的组蛋白去乙酰化酶 3(HDAC3) 抑制剂,具有抗癌和抗病毒活性。HDAC3-IN-T247 以剂量依赖的方式诱导人结肠癌 HCT116 细胞中 NF-κB 乙酰化。HDAC3-IN-T247 抑制癌细胞增殖。 | |||
T21792 |
CGP 3466B maleate
马来酸CGP3466B,Omigapil (Maleate),Omigapil maleate |
Apoptosis | Apoptosis |
CGP 3466B maleate (Omigapil maleate) 是一种口服有效的 GAPDH 亚硝基化抑制剂,可消除 Aβ1-42 诱导的小鼠 tau 乙酰化,记忆障碍和运动功能障碍,Omigapil maleate 具有研究阿尔茨海默症的潜力。Omigapil maleate (CGP3446B maleate) 是一种有效的凋亡 (apoptosis) 抑制剂。Omigapil maleate 可用于研究先天性肌营养不良 (CMD)。 | |||
T30292 | BAMF | ||
BAMF is a chemical reagent used in the chemical modification of proteins, mainly in the acetylation process. | |||
T25176 |
BRD2577
BRD-2577,BRD 2577 |
||
BRD2577 is an HDAC inhibitor, by suppressing multiple HDAC enzymes and modulating acetylation levels in cells. | |||
T69879 |
Bavarostat
|
||
Bavarostata is a highly brain penetrant HDAC6 inhibitor (IC50=60nM). Bavarostat exhibits excellent HDAC6 selectivity (>80-fold over all other Zn-containing HDAC paralogues), modulates tubulin acetylation selectively over histone acetylation, and has excellent brain penetrance. | |||
T24132 |
HDAC3-IN-T326
HDAC3 inhibitor-T326,T326,HDAC3 IN T326,HDAC3 inhibitor T326,HDAC3INT326 |
||
HDAC3-IN-T326 is a potent and selective HDAC3 inhibitor that acts by increasing NF-κB acetylation and activating HIV gene expression in latent HIV-infected cells. | |||
T23917 |
CRT-0105950
CRT 0105950 |
||
CRT-0105950 is an effective LIMK inhibitor that acts by suppressing cofilin phosphorylation and increasing αTubulin acetylation in cells. | |||
T24998 |
AC-93253 iodide
AC93253 iodide |
||
AC-93253 iodide is a selective inhibitor of SIRT2. It significantly enhances the acetylation of tubulin p53 and histone H4. | |||
T23916 |
CRT-0105446
CRT0105446 |
||
CRT-0105446 is an effective LIMK inhibitor that acts by suppressing cofilin phosphorylation and increasing αTubulin acetylation in cells. | |||
T20364 |
Aspartylglutamate
Asp-glu |
||
Aspartylglutamate is a precursor molecule. When it upon acetylation to N-acetyl-aspartyl-glutamate (NAAG) is used as a metabotropic glutamate mGlu receptor agonist. | |||
T39580 |
Histone H3 (23-34)
Histone H3 (23-34) |
||
Histone H3 (23-34) is a peptide consisting of amino acid residues 23 to 34 of the histone H3 protein. This peptide specifically includes lysine residues at positions 23 and 27, which can undergo methylation and acetylation modifications. | |||
T36576 |
Histone H3 (21-44)-GK-biotin (trifluoroacetate salt)
Histone H3 (21-44)-GK-biotin (trifluoroacetate salt) |
||
Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.1 and 3.2 sequences and is biotinylated via a C-terminal GK linker. Histone H3 (21-44) contains a lysine residue at position 23 that is subject to acetylation, an arginine at position 26 subject to methylation, and a serine at position 28 subject to phosphorylation, as well as lysine residues at positions 27 and 36 that are subject to methylation and acetylation.... | |||
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. | |||
T72503 |
Antitubulin agent 1
|
||
Antitubulin agents-1 是一种抗微管蛋白剂,可诱导微管 (microtubules) (Microtubule/Tubulin) 破坏并增加 α-微管蛋白乙酰化。Antitubulin agents-1 具有抗癌作用。 | |||
T35818 |
CAY10669
|
||
CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid . At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro. | |||
T35825 |
Trichostatin C
|
||
Trichostatin C is a glycosylated derivative of trichostatin A , the antifungal antibiotic that reversibly inhibits histone deacetylase. Trichostatin C is reported to be the first example of a glucopyranosyl hydroxamate identified in nature. It has been shown to induce the differentiation of a mouse erythroleukemia cell line and to increase histone H4 acetylation in B cells, though at higher concentrations than trichostatin A. | |||
T62917 |
MIR002
|
||
MIR002 是一种有效的、口服具有活力的 DNA polymerase α (POLA1) 和 HDAC 11 双重抑制剂,具有显著的体内抗肿瘤活性。MIR002 能够诱导 p53 乙酰化、激活 p21,将细胞周期阻滞在 G1/S 期,并诱导细胞凋亡。 | |||
T79586 |
3′-Acetate-ATP
|
||
3’-Acetate-ATP为ATP的乙酰化衍生物,表现为ATP类似物,其在中性pH值的水溶液中于259 nm波长处展现出最大的紫外线吸收。该化合物能够抑制核酸聚合酶活性,从而阻断核酸的延伸。 | |||
T61433 | HDAC1-IN-5 | ||
HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1] | |||
T62916 |
GEM144
|
||
GEM144 是一种有效的、口服具有活力的 DNA polymerase α(POLA1) 和HDAC 11 双重抑制剂。GEM144 能够诱导 p53 乙酰化、激活 p21,将细胞周期阻滞在 G1/S 期,并诱导细胞凋亡。 | |||
T82343 | Gamma-Glutamyl Transferase-IN-1 | ||
Gamma-Glutamyl Transferase-IN-1 (compound 4de) 是一种 β-羰基酰肼类抑制剂,靶向谷氨酰转移酶,具有抗真菌和抗菌活性。它通过促进活性氧积累、破坏细胞膜和失调组蛋白乙酰化来发挥作用。 | |||
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... | |||
T76158 | Phosphate acetyltransferase | ||
Phosphate acetyltransferase (磷酸乙酰转移酶) 为一转移酶类,主要应用于生化领域。该酶通过将乙酰基从 acetyl-P 可逆地转移至 CoA,生成 acetyl-CoA 及无机磷酸盐,从而参与乙酸的同化及异化过程。 | |||
T62920 |
HDAC-IN-38
|
||
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。 | |||
T73000 |
SIRT2-IN-11
|
||
SIRT2-IN-11 (AEM1) 是选择性的SIRT2抑制剂,IC50值为 18.5 μM。SIRT2-IN-11 以 p53 依赖的诱导细胞凋亡,激活CDKN1A,PUMA 和NOXA 的表达,并且促进 p53 的乙酰化。SIRT2-IN-11 可用于 p53 相关的癌症研究。 | |||
T73805 | Acetyl coenzyme A | ||
Acetyl-coenzyme A (Acetyl-CoA) 是一种具有膜非渗透性的中枢代谢中间体,参与 TCA 循环和氧化磷酸化代谢过程。Acetyl-coenzyme A 通过向目标氨基酸残基提供乙酰基团,来完成蛋白质的翻译后乙酰化反应,从而调节各种细胞机制。Acetyl Coenzyme A 也是脂质合成的关键前体。 | |||
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8160 |
EGCG Octaacetate
乙酰化表没食子儿茶素没食子酸酯,乙酰化EGCG |
Others; Antibacterial | Microbiology/Virology; Others |
EGCG Octaacetate 是表没食子儿茶素没食子酸酯的前药,对革兰氏阳性菌和革兰氏阴性菌有潜在抗菌可能。它可下调 PI3K/Akt/NFκB 磷酸化和 p65 乙酰化来降低促炎介质水平,减少小鼠结肠炎引起的结肠癌。 | |||
T1437 |
D-Panthenol
D-泛醇,D-Pantothenyl alcohol,Ilopan,Dexpanthenol,Pantothenol |
Endogenous Metabolite | Metabolism |
D-Panthenol (D-Pantothenyl alcohol) 是 D-pantothenic acid 和胆碱能剂的酒精类似物。D-Panthenol 作为乙酰化反应所必需的辅酶A的前体,参与乙酰胆碱的合成。虽然 D-Panthenol 作用的确切机制尚不清楚,但它可能增强乙酰胆碱的作用。D-Panthenol 作用于胃肠道,增加下肠蠕动。它也适用于局部皮肤,以缓解瘙痒和促进愈合。 |