Chromatin/Epigenetics(染色质/表观遗传学)

Epigenetics

Epigenetics means above genetics. It determines how much and whether a gene is expressed without changing DNA sequences. Epigenetic regulations include, 1. DNA methylation: the addition of methyl group to DNA, converting cytosine to 5-methylcytosine, mostly at CpG sites; 2. Histone modifications: posttranslational modificationEpigeneticss of histone proteins including acetylation, methylation, ubiquitylation, phosphorylation and sumoylation; 3. miRNAs: non-coding microRNA downregulating gene expression; 4. Prions: infectious proteins viewed as epigenetic agents capable of inducing a phenotype without changing the genome.

Products for Chromatin/Epigenetics

Cat.No. 产品名称 Information
GC13148 MS436 MS436 是一类新的溴结构域抑制剂，对 BRD4 BrD1 具有估计的 Ki=30-50 nM 的强亲和力，对 BrD2 的选择性是 10 倍。
GC12548 UNC 0631 An inhibitor of G9a/GLP methyltransferases
GC15747 I-BET151 (GSK1210151A)
7-(3,5-二甲基异噁唑-4-基)-8-甲氧基-1-((R)-1-(吡啶-2-基)乙基)-1H-咪唑并[4,5-C]喹啉-2(3H)-酮,GSK1210151A
A BRD2, BRD3, and BRD4 inhibitor
GC17073 I-BET-762
(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-A][1,4]苯并二氮杂卓-4-乙酰胺,I-BET762; GSK525762; GSK525762A
Inhibitor of BET proteins
GC11537 MK-4827 tosylate
尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate
An orally bioavailable PARP1/2 inhibitor
GC12756 MK-4827 hydrochloride
MK-4827 hydrochloride
MK-4827 hydrochloride (MK-4827 hydrochloride) 是一种高效且具有口服生物利用度的 PARP1 和 PARP2 抑制剂，IC50 分别为 3.8 和 2.1 nM。 MK-4827 hydrochloride 抑制 DNA 损伤的修复，激活细胞凋亡并显示出抗肿瘤活性。
GC11424 Valproic acid
丙戊酸; VPA; 2-Propylpentanoic Acid
A class I HDAC inhibitor
GC16143 Varenicline Hydrochloride
6,7,8,9-四氢-6,10-甲桥-6H-吡嗪并[2,3-H][3]苯并氮杂卓盐酸盐,CP 526555 hydrochloride
Varenicline Hydrochloride (CP 526555 hydrochloride) 是一种高亲和力、选择性的 α4β2 尼古丁乙酰胆碱受体 (nAChR) 部分激动剂和完整的 α7 nAChR 激动剂。
GC11439 MG 149
Tip60 HAT inhibitor
A HAT inhibitor
GC12891 CCT007093
(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮
An inhibitor of PPM1D
GC14755 Inauhzin
INZ
A selective SIRT1 inhibitor
GC14364 SGI-1027
DNA Methyltransferase Inhibitor II
A DNA methyltransferase inhibitor
GC14676 Pacritinib (SB1518)
帕克替尼
An equipotent inhibitor of FLT3 and JAK2
GC11375 UNC1999 A selective, cell-permeable EZH2 inhibitor
GC14652 MM-102
HMTase Inhibitor IX
An inhibitor of WDR5/MLL interactions
GC15603 JIB-04
5-氯-2(1H)-吡啶酮(2E)-(苯基-2-吡啶基亚甲基)腙
A pan Jumonji histone demethylase inhibitor
GC14199 RVX-208
阿帕他隆; RVX-208; RVX000222
A selective BET bromodomain antagonist
GC18096 UNC669 A selective MBT inhibitor
GC13419 ME0328 A selective PARP3 inhibitor
GC10442 MK-8745 An Aurora A kinase inhibitor
GC17703 TMP269
TMP 269;TMP-269
A selective class IIa HDAC inhibitor
GC14285 RGFP966
RGFP 966;RGFP-966
RGFP966是一种N-(o-aminophenyl)carboxamide HDAC抑制剂，对HDAC3的IC50为0.08 μM，是一类针对HDAC3的慢开/慢关竞争性紧密结合抑制剂。
GC11548 Tankyrase Inhibitors (TNKS) 49
TNKS 49;TNKS49;TNKS-49
Tankyrase inhibitor
GC15041 Tankyrase Inhibitors (TNKS) 22
TNKS 22;TNKS22;TNKS-22
Tankyrase inhibitor
GC12337 Tenovin-3
Tenovin 3;Tenovin3
A small molecule activator of p53
GC10322 Tubastatin A HCl
TubastatinA盐酸盐,TSA HCl;Tubastatin A hydrochloride
A potent HDAC6 inhibitor
GC16436 Tenovin-6 A small molecule activator of p53
GC12781 XAV-939
3,5,7,8-四氢-2-[4-(三氟甲基)苯基]-4H-噻喃并[4,3-D]嘧啶-4-酮
XAV-939 选择性抑制 β-连环蛋白介导的转录。
GC10555 Splitomicin
斯普利特麻一辛
Inhibitor of yeast Sir2p
GC17455 TAK-632 A selective pan-Raf inhibitor
GC15718 CID 2011756 An inhibitor of protein kinase D
GC14062 EPZ-6438
E-7438,Tazemetostat

EPZ-6438 是一种有效且具有生物利用度的 EZH2 抑制剂，EZH2 是多梳抑制复合物 2 (PRC2) 的催化亚基，可催化组蛋白 H3 (H3K27) 的赖氨酸 27 甲基化，从而抑制含有人 PRC2 的活性抑制常数 K_i 值为 2.5 nM 的野生型 EZH2。
GC14562 Nanaomycin A
七尾霉素,Nanafrocin, Nanafrocine, Nanafrocinum, Rosanomycin A
A bacterial metabolite
GC12450 BI 2536
BI-2536;BI2536
A potent inhibitor of Plk1
GC16277 α-Amanitin
alpha-鹅膏覃碱; α-Amatoxin
A selective RNA polymerase II inhibitor
GC12020 TCS 401 A selective PTP1B inhibitor
GC17762 NSC 33994 NSC 33994 (G6) 是一种选择性 JAK2 抑制剂，IC50 为 60 nM。
GC16973 DMOG
二甲基乙二酰氨基乙酸,Dimethyloxallyl Glycine
DMOG（二羟基丙氨酸）是 α-酮戊二酸辅助因子的拮抗剂和 HIF-脯氨酸羟化酶的抑制剂，导致 HIF-1α 蛋白在细胞核中的稳定和积累。
GC15688 UNC 0224 A potent inhibitor of G9a histone methyltransferase
GC12019 TCS HDAC6 20b An HDAC6 inhibitor
GC13237 LMK 235
N-[[6-(羟基氨基)-6-氧代己基]氧基]-3,5-二甲基-苯甲酰胺
A selective inhibitor of HDAC4 and HDAC5
GC11972 NU 9056 NU 9056 是一种有效且选择性的 Tip60 (KAT5) 组蛋白乙酰转移酶抑制剂，浓度为 2 µM。 NU 9056 对 Tip60 的选择性比 PCAF、p300 和 GCN5 高 16 倍以上。 NU 9056 诱导前列腺癌细胞凋亡。
GC10174 SGC-CBP30
SGCCBP30,SGC CBP30
A potent inhibitor of CREBBP/EP300 bromodomains
GC17944 I-CBP 112 A p300 and CBP inhibitor
GC16378 TC-A 2317 hydrochloride TC-A 2317 hydrochloride 是一种具有口服活性的 Aurora A 激酶抑制剂 (Ki=1.2 nM)。 TC-A 2317 hydrochloride 对 Aurora B 激酶 (Ki=101 nM) 和其他 60 种激酶具有出色的选择性、良好的细胞渗透性和良好的 PK 曲线。抗肿瘤活性。
GC17241 Thiolutin
硫藤黄素,Acetopyrrothin
An inhibitor of Hsp27 and RNA polymerases
GC15060 Mithramycin A
光辉霉素,Mithramycin A
A DNA-binding antitumor antibiotic
GC10169 NSC 87877 A potent inhibitor of SHP-1 and SHP-2
GC16256 BVT 948
4-羟基-3,3-二甲基-2H-苯并[G]吲哚-2,5(3H)-二酮
An inhibitor of protein tyrosine phosphatases
GC17344 Alexidine dihydrochloride
己联双辛胍二盐酸盐
An alkyl bis(biguanide) antiseptic