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
GC16614 SCH-1473759
SCH1473759;SCH 1473759
SCH-1473759 是一种极光抑制剂，对极光 A 和 B 的 IC50 分别为 4 和 13 nM。
GC12064 SB1317
14-甲基-20-氧杂-5,7,14,27-四氮杂四环[19.3.1.1(2,6).1(8,12)]二十七碳-1(25),2,4,6(27),8,10,12(26),16,21,23-十烯,TG02;SB 1317;TG 02;SB-1317;TG-02
A multi-kinase inhibitor
GC16124 Ruxolitinib phosphate
鲁索利替尼磷酸盐,INCB018424 phosphate;INCB 018424 phosphate;INCB-018424 phosphate;Ruxolitinib
A potent and selective JAK1/JAK2 inhibitor
GC10423 RG2833
RG 2833;RG-2833;RGFP-109;RGFP109;RGFP 109
An HDAC inhibitor
GC14651 Reversine
逆转素
A purine derivative
GC14243 Resminostat hydrochloride
RAS2410 hydrochloride;4SC-201 hydrochloride;RAS 2410 hydrochloride;RAS-2410 hydrochloride
An orally bioavailable HDAC inhibitor
GC11525 Pyridone 6
吡啶酮6
吡啶酮 6 抑制 Jak3，K(I)=5 nM； Pyridone 6 还抑制 Jak 家族成员 Tyk2 和 Jak2，IC(50)=1 nM 和 Jak1，IC(50)=15 nM。
GC10995 PJ34
PJ-34;PJ 34
An inhibitor of poly (ADP-ribose) polymerases
GC17973 OTX-015
OTX 015;OTX015
OTX-015 以浓度依赖性方式抑制 BRD2、BRD3 和 BRD4 与乙酰化组蛋白 4 的结合，IC50 值为 92-112nM .OTX-015 在九个 AML 细胞系中的六个和所有四个 ALL 细胞系中测量到显着的生长抑制:HEL IC50 值为 248 nM，NB4 IC50值为 233 nM，NOMO-1 IC50 值为 229 nM，KG1 IC50 值为 198 nM，OCI-AML3 IC50 值为Kasumi IC50 值为 60 nM，Kasumi IC50 值为 17 nM，JURKAT IC50 值为 249 nM，BV-173 IC50 值为 161 nM , TOM-1 IC50 值为 133 nM, RS4-11 IC50 值为 34 nM。
GC13229 NVP-BSK805
BSK 805;BSK-805;BSK805;NVP-BSK 805

A potent, selective JAK2 inhibitor
GC17802 MK-4827
尼拉帕尼; MK-4827
An orally bioavailable PARP1/2 inhibitor
GC12199 MI-3
Menin-MLL inhibitor 3;Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)-
An inhibitor of menin-MLL fusion protein interactions
GC11418 MI-2
Menin-MLL inhibitor 2;Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-propyl-
An inhibitor of menin-MLL fusion protein interactions
GC13154 LKB1(AAK1 dual inhibitor)
N-[5-(4-氰基苯基)-1H-吡咯并[2,3-B]吡啶-3-基]-3-吡啶甲酰胺,LKB1/AAK1 dual inhibitor
LKB1(AAK1 dual inhibitor) 是一种有效的多激酶抑制剂，对 Pim1/AKK1/MST2/LKB1 的 Kd 值分别为 35 nM/53 nM/75 nM/380 nM，并且还抑制 MPSK1 和 TNIK。
GC14671 JANEX-1
4-(4'-羟基苯基)氨基-6,7-二甲氧基喹唑啉,WHI-P131;Janex 1;WHI-P 131
A selective JAK3 inhibitor
GC13826 JAK2 Inhibitor V, Z3
Z3; NSC 42834;1-Butanone, 2-methyl-1-phenyl-4-(2-pyridinyl)-2-[2-(2-pyridinyl)ethyl]-
A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK
GC17534 GSK343
GSK-343;GSK 343
A selective, cell-permeable EZH2 inhibitor
GC15783 GSK126
EZH2 inhibitor;GSK-126;GSK 126

A selective EZH2 inhibitor
GC10524 GSK 525768A
GSK525768A;GSK-525768A
GSK 525768A 是 GSK525762A 的非活性对映异构体。 GSK 525768A 对 BET 没有任何活动。
GC15830 Daminozide
丁酰肼
Selective inhibitor of KDM2/7 histone demethylases
GC16468 CYT387 sulfate salt
N-(氰基甲基)-4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯甲酰胺硫酸盐(1:2),CYT-387 sulfate;CYT 387 sulfate
A potent inhibitor of JAK1 and JAK2
GC13056 CX-6258
CX6258;CX 6258
A pan-Pim kinase inhibitor
GC14787 Curcumin
姜黄素; Diferuloylmethane; Natural Yellow 3; Turmeric yellow
A yellow pigment with diverse biological activities
GC11975 CHAPS
3-[3-(胆酰胺丙基)二甲氨基]丙磺酸内盐
CHAPS 是胆酸的衍生物，是一种用于溶解膜蛋白的两性离子去污剂。
GC10920 BMN-673 8R,9S
他拉唑帕利 (8R,9S); (8R,9S)-BMN-673; (8R,9S)-LT-673
BMN-673 8R,9S ((8R,9S)-BMN-673) 是 Talazoparib 的对映异构体。 BMN-673 8R,9S 是一种 PARP1 抑制剂，IC50 为 144 nM。
GC13830 Baricitinib phosphate
磷酸巴瑞克替尼; LY3009104 phosphate; INCB028050 phosphate
A JAK1 and JAK2 inhibitor
GC11572 Bardoxolone methyl
甲基巴多索隆; RTA 402; NSC 713200; CDDO Methyl ester
A synthetic triterpenoid with potent anticancer and antidiabetic activity
GC14709 AZD1152
5-[[7-[3-[乙基[2-(磷酰氧基)乙基]氨基]丙氧基]-4-喹唑啉基]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺,AZD-1152;AZD 1152
AZD1152 (AZD1152) 是 AZD1152-hQPA 的前药，是一种高选择性的 Aurora B 抑制剂，在无细胞试验中 IC50 为 0.37 nM。 AZD1152 (AZD1152) 在癌细胞中诱导生长停滞和凋亡。
GC12454 BMS-911543 A potent, selective JAK2 inhibitor
GC10402 Bromosporine A non-specific bromodomain inhibitor
GC13383 EPZ004777 EPZ004777 作为一种有效的表观遗传调节剂，可以逆转 TGF-β1 诱导的 T 调节细胞，可用于治疗多种免疫疾病。
GC11491 SGC 0946 A potent inhibitor of DOT1L
GC17428 SGI-110
SGI-110
SGI-110 (SGI-110) 是第二代 DNA 甲基转移酶 (DNMT) 抑制剂，用于研究急性髓性白血病 (AML) 和骨髓增生异常综合征 (MDS)。
GC14165 Tenovin-1 A small molecule activator of p53
GC11104 SMI-4a A Pim kinase inhibitor
GC18074 PF-03814735
N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺
PF-03814735 是一种有效的、具有口服生物利用度的 Aurora1 和 Aurora2 激酶的可逆抑制剂，IC50 值分别为 0.8nM 和 5nM 。
GC10008 GSK1070916
GSK-1070916A
A potent inhibitor of Aurora B and C kinases
GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase
GC15106 CYC116 A potent Aurora kinase inhibitor
GC11085 TAK-901
5-[3-(乙基磺酰基)苯基]-3,8-二甲基-N-(1-甲基-4-哌啶基)-9H-吡啶并[2,3-B]吲哚-7-甲酰胺
A non-selective inhibitor of Aurora kinases
GC14592 KW 2449
[4-[2-(1H-吲唑-3-基)乙烯基]苯基]-1-哌嗪基甲酮
A multi-kinase inhibitor
GC10479 PHA-680632
Pha 680632
An Aurora kinase inhibitor
GC13837 SNS-314 Mesylate
N-(3-氯苯基)-N'-[5-[2-(噻吩并3,2-D]嘧啶-4-基氨基)乙基]-2-噻唑基]脲甲磺酸盐(1:1)
A pan-Aurora kinase inhibitor
GC17162 MK-5108 (VX-689)
VX-689
A potent inhibitor of Aurora kinases
GC13198 AMG-900 A selective pan-Aurora kinase inhibitor
GC17196 Hesperadin A multi-kinase inhibitor
GC10638 AT9283 A broad spectrum kinase inhibitor
GC15217 Danusertib (PHA-739358)
达鲁舍替,5-Amido-pyrrolopyrazole 9d
A pan-Aurora kinase and Abl inhibitor
GC12612 JNJ-7706621
JNJ7706621, JNJ 7706621
A dual inhibitor of CDKs and Aurora kinases
GC12208 MLN8054
4-[[9-氯-7-(2,6-二氟苯基)-5H-嘧啶并[5,4-D][2]苯并氮杂卓-2-基]氨基]苯甲酸
An inhibitor of Aurora A kinase