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
- Bromodomain(45)
- Aurora Kinase(62)
- DNA Methyltransferase(35)
- HDAC(201)
- Histone Acetyltransferases(77)
- Histone Demethylases(104)
- Histone Methyltransferase(238)
- HIF(101)
- JAK(162)
- MBT Domains(1)
- PARP(118)
- Pim(31)
- Protein Ser/Thr Phosphatases(31)
- RNA Polymerase(6)
- Sirtuin(74)
- Sphingosine Kinase-2(1)
- Polycomb repressive complex(2)
- SUMOylation(3)
- PAD(21)
- Epigenetic Reader Domain(243)
- MicroRNA(24)
- Chromodomain(1)
- Citrullination(20)
- DNA/RNA Demethylation(2)
- DNA/RNA Methylation(8)
- Histone Deacetylation(42)
- Histones/Histone Peptides(62)
- PHD Domains(1)
- Tandem Tudor & Tudor-like Domains(1)
- PRMT(2)
- Readers(1)
- Small Interfering RNA (siRNA)(1)
- METTL3(2)
- WDR5(1)
- TET Protein(2)
- HuR(1)
- SF3B1(1)
- Cat.No. 产品名称 Information
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GC47050
CAY10727
A PAD3 inhibitor
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GC46935
Bobcat 339
BC339
A cytosine derivative -
GC46900
AZ9482
A PARP inhibitor
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GC46892
ATRA-BA Hybrid
A prodrug form of all-trans retinoic acid and butyric acid
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GC46736
7-Bromoheptanoic Acid
7-溴庚酸
A building block -
GC46675
4-Phenyl-2-pyrrolidinone
4-苯基-2-吡咯烷酮
A precursor and synthetic intermediate -
GC46628
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline
4-氯-6,7-二(2-甲氧基乙氧基)喹唑啉
A building block and synthetic intermediate -
GC46607
4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone
4-甲基亚硝胺基-1-3-吡啶基-1-丁酮(NNK),NNK
4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone是一种主要存在于烟草制品中的强效烟草特异性致癌物,对α7烟碱型乙酰胆碱受体(α7 nAChR)具有很高的亲和力,在小细胞肺癌(SCLCs)中的EC50值为0.03μM,在肺神经内分泌细胞(PNECs)中的EC50值为0.005μM。 -
GC46508
2',2'-Difluoro-2'-deoxyuridine
2'-脱氧-2',2'-二氟尿嘧啶核苷
An active metabolite of gemcitabine -
GC46503
2-(1,8-Naphthyridin-2-yl)phenol
3-氨基-2-氯-6-三氟甲基吡啶
An enhancer of STAT1 activity -
GC61279
SIRT-IN-3
2-(苯基氨基)苯甲酰胺
SIRT-IN-3是一种有效的SIRT抑制剂,对SIRT1的IC50为17μM。SIRT-IN-3对SIRT1的选择性分别是SIRT-2和SIRT3的4倍和14倍(IC50forSIRT2=74μM;IC50forSIRT3=235μM)。 -
GC61212
PROTAC BRD4 Degrader-5
PROTACBRD4Degrader-5是一种基于PROTAC的BRD4降解剂,可有效降解HER2阳性和阴性乳腺癌细胞系中的BRD4。
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GC61142
NSC745885
NSC745885是一种有效的抗肿瘤(anti-tumor)试剂,对多种癌细胞株有选择性毒性,但对正常细胞没有毒性。NSC745885是一种有效的EZH2的下调因子通过蛋白酶体降解途径。NSC745885为晚期膀胱癌和口腔鳞癌的研究提供了可能性。
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GC61058
Metoprine
氯苯氨啶,BW 197U
Metoprine(BW197U)是一种有效的组胺N-甲基转移酶(HMT)抑制剂。Metoprine是一种二氨基嘧啶衍生物,可以透过血脑屏障,并通过抑制HMT增加脑组胺水平。Metoprine是一种抗叶酸(antifolate)和抗肿瘤药。 -
GC61029
Marein
马里甙
A glucoside chalcone with diverse biological activities -
GC60925
IACS-9571 hydrochloride
ASIS-P040 hydrochloride
IACS-9571(ASIS-P040)hydrochloride是溴结构域蛋白TRIM24和BRPF1的抑制剂,对TRIM24的IC50和Kd值分别为8nM和31nM,对BRPF1的Kd值为14nM。 -
GC60919
Hydroxycitric acid tripotassium hydrate
三水合钾柠檬酸; Potassium citrate monohydrate
Hydroxycitricacidtripotassiumhydrate(Potassiumcitratemonohydrate)是藤黄果的主要活性成分,也是柠檬酸的衍生物。Hydroxycitricacidtripotassiumhydrate可竞争性抑制柠檬酸裂解酶(ATPcitratelyase),并具有减肥效果。Hydroxycitricacidtripotassiumhydrate有效抑制结石形成并抑制HIF,具有抗氧化,抗炎和抗肿瘤作用。 -
GC60833
FB23
FB23 is a potent and selective inhibitor of FTO demethylase with IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.
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GC60579
Amodiaquine dihydrochloride
盐酸阿莫地喹,Amodiaquin dihydrochloride
A prodrug form of N-desethyl amodiaquine -
GC18750
NEO2734
EP31670
NEO2734 (EP31670) 是一种口服有效的双重 p300/CBP 和 BET 溴结构域选择性抑制剂,对 p300/CBP 和 BET 溴结构域的 IC50 值均 <30 nM。 NEO2734 在 SPOP 突变型和野生型前列腺癌中具有活性。 -
GC60310
Psammaplin A
PsammaplinA是一种海洋代谢产物,是HDAC和DNA甲基转移酶(DNAmethyltransferases)的有效抑制剂。PsammaplinA是一种高效的选择性HDAC1抑制剂,IC50为0.9nM,对HDAC1的选择性是DAC6的360倍,对HDAC7和HDAC8的效力低1000倍以上。PsammaplinA对革兰氏阳性细菌(Gram-positivebacteria)具有抗菌作用,并抑制DNA合成和DNA促旋酶(DNAgyrase)活性。抗肿瘤活性。
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GC60184
GSK8814
GSK8814 是一种高效、选择性的 ATAD2/2B 溴代苯胺化学探针和抑制剂,结合常数pKd=8.1,在 BROMOscan 中的 pKi=8.9。GSK8814 分别以 7.3 和 4.6 的 pIC50 与 ATAD2 和 BRD4 BD1 结合。GSK8814 对 ATAD2 的选择性是 BRD4 BD1 的 500 倍。
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GC60182
GSK046
iBET-BD2
A BD2 bromodomain inhibitor -
GC60172
Gardenia yellow
西红花苷 I
Crocin-I, a major member of the crocin family, has antidepressant activity and ameliorates the disruption of lipid metabolism and dysbiosis of the gut microbiota induced by chronic corticosterone in mice. -
GC60004
(rel)-Tranylcypromine D5 hydrochloride
反式-2-(苯基-D5)环丙胺盐酸盐,SKF 385-d5 hydrochloride
Tranylcypromine-d5 (SKF 385-d5) hydrochloride 是氘标记的 (rel)-Tranylcypromine hydrochloride。 -
GC39840
AMI-1 free acid
猩红酸
AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. -
GC39699
Aurintricarboxylic acid
金精三羧酸
A protein synthesis inhibitor with diverse biological activities -
GC39679
CG347B
CG347B 是一种选择性的 HDAC6 抑制剂。
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GC39665
CMP-5
CMP-5 是一种有效的选择性 PRMT5 抑制剂,对 PRMT1,PRMT4 和 PRMT7 酶无活性。CMP-5 在组蛋白的准备过程中,通过抑制 PRMT5 甲基转移酶活性选择性地阻断 S2Me-H4R3。CMP-5 阻断 EBV 驱动的 B 淋巴细胞转化,但对正常 B 细胞没有影响。
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GC39663
BI-9321 trihydrochloride
BI-9321 trihydrochloride 是一种有效的,选择性的,具有细胞活性的 NSD3-PWWP1 拮抗剂,Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 trihydrochloride 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用,IC50 为 1.2 μM。
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GC39551
BRD3308
An HDAC3 inhibitor
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GC39491
GSK-3484862
GSK-3484862 是 DNA 甲基转移酶 Dnmt1 的非共价抑制剂,通过诱导 DNA 低甲基化起抗癌作用。
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GC39485
CK2/ERK8-IN-1
A dual inhibitor of CK2 and ERK8
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GC39435
Scopolin
东莨菪苷
A coumarin glucoside with anti-inflammatory activity -
GC39417
OXFBD04
OXFBD04 是一种有效的选择性 BRD4 抑制剂,IC50 为 166 nM。OXFBD04 是一种有效的 BET 溴结构域配体,对 CREBBP 溴结构域具有额外的适度亲和力。OXFBD04 具有抗癌活性。
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GC39407
MS1943
A PROTAC that drives EZH2 degradation
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GC39394
KDM5-C70
KDOAM-21
An inhibitor of JARID1B -
GC39365
CPTH2
A HAT inhibitor
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GC50633
BMS 986094
N-(2'-C-甲基-6-O-甲基-P-1-萘基-5'-鸟苷酰基)-L-丙氨酸2,2-二甲基丙酯,INX-08189
BMS 986094 (INX-08189) 是一种有效的丙型肝炎病毒 (HCV) 复制抑制剂,在 Huh-7 细胞中 24 小时的 EC50 为 35 nM。 -
GC50576
MRK 740
Potent PRDM9 inhibitor
-
GC50542
TP 238
A chemical probe for the bromodomains of CECR2 and BPTF
-
GC50540
BI 9321
Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain
-
GC50537
FM19G11
FM19G11 是一种低氧诱导因子-1-α (HIF-1α) 抑制剂,在 HeLa 细胞中抑制低氧诱导的荧光素酶活性,IC50 为 80 nM。
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GC50506
Fluorescein-NAD+
荧光素-NAD+ 是放射性标记的 NAD 的替代品,也是 ADP 核糖基化的底物。
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GC50480
PF 06651600 malonate
Potent and selective JAK3 inhibitor
-
GC50395
L Moses dihydrochloride
L-45 dihydrochloride
High affinity and selective PCAF bromodomain inhibitor -
GC50378
GSK 9311 hydrochloride
GSK 9311 hydrochloride 是 GSK6853 活性较低的类似物,可用作阴性对照。 GSK 9311 hydrochloride 抑制 BRPF 溴结构域,对 BRPF1 和 BRPF2 的 pIC50 值分别为 6.0 和 4.3。
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GC50367
PF 06726304 acetate
Highly potent and SAM-competitive EZH2 inhibitor
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GC50340
TC AC 28
High affinity BET bromodomain ligand
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GC50322
BRD 9757
Potent and selective HDAC6 inhibitor