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(43)
- Aurora Kinase(57)
- DNA Methyltransferase(32)
- HDAC(167)
- Histone Acetyltransferases(64)
- Histone Demethylases(91)
- Histone Methyltransferase(193)
- HIF(87)
- JAK(137)
- MBT Domains(1)
- PARP(100)
- Pim(27)
- Protein Ser/Thr Phosphatases(31)
- RNA Polymerase(6)
- Sirtuin(65)
- Sphingosine Kinase-2(1)
- Polycomb repressive complex(2)
- SUMOylation(3)
- PAD(17)
- Epigenetic Reader Domain(195)
- MicroRNA(13)
- Chromodomain(1)
- Citrullination(15)
- DNA/RNA Demethylation(1)
- DNA/RNA Methylation(6)
- Histone Deacetylation(38)
- Histones/Histone Peptides(7)
- Tandem Tudor & Tudor-like Domains(1)
- PRMT(2)
- Cat.No. 产品名称 Information
- 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。
- 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。
- GC50480 PF 06651600 malonate Potent and selective JAK3 inhibitor
- GC50395 L Moses 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。
- GC50367 PF 06726304 acetate Highly potent and SAM-competitive EZH2 inhibitor
- GC50340 TC AC 28 High affinity BET bromodomain ligand
- GC50322 BRD 9757 Potent and selective HDAC6 inhibitor
- GC50211 TAT-cyclo-CLLFVY TAT-cyclo-CLLFVY 是 HIF-1 异二聚化的环肽抑制剂,可抑制癌细胞中的缺氧信号传导。 TAT-cyclo-CLLFVY 破坏 HIF-1α/HIF-1β 蛋白质-蛋白质相互作用,IC50 为 1.3 μM。
- GC50182 ent-LP 99 ent-LP 99 是一种有效的选择性 BRD7 和 BRD9 抑制剂,对 BRD9 的 KD 为 99 nM。
- GC50136 NSC 636819 NSC 636819 是 KDM4A/KDM4B 的竞争性和选择性抑制剂。 KDM4A/KDM4B 是前列腺癌的潜在进展因素。 NSC 636819 具有研究癌症疾病,尤其是前列腺癌的潜力。
- GC50128 TC-S 7009 An inhibitor of HIF-2α PAS-B domain heterodimerization
- GC50082 UNC 2399 UNC 2399 是一种生物素化的 UNC1999,是一种选择性 EZH2 降解剂,对 EZH2 保持高效的体外效力,IC50 为 17 nM。
- GC50070 I-BET 151 dihydrochloride A BRD2, BRD3, and BRD4 inhibitor
- GC50066 Atiprimod dihydrochloride JAK2 inhibitor
- GC50050 Hesperadin hydrochloride A multi-kinase inhibitor
- GC39302 PARP14 inhibitor H10 PARP14 inhibitor H10 (化合物 H10) 是针对 PARP14 的选择性抑制剂 (IC50=490 nM),是其他 PARP 的抑制剂 (约为 PARP1 的 24 倍)。PARP14 抑制剂 H10 诱导 caspase-3/7 介导的细胞凋亡 (apoptosis)。
- GC39252 MS31 trihydrochloride MS31 trihydrochloride 是一种高亲和性和选择性的,片段样的甲基赖氨酸读写蛋白 spindlin 1 (SPIN1) 抑制剂,有效破坏 SPIN1 与 H3K4me3 蛋白互相作用 (IC50=77 nM,AlphaLISA;243 nM,FP). MS31 trihydrochloride 选择性结合 SPIN1 的 Tudor 结构域 II (Kd=91 nM)。MS31 trihydrochloride 能有效抑制含三甲基赖氨酸肽与 SPIN1 的结合,对非肿瘤性细胞无毒。
- GC39214 1-Naphthohydroxamic acid 1-Naphthohydroxamic acid是强效、细胞渗透性和选择性组蛋白脱乙酰酶抑制剂 (HDAC8) 抑制剂(IC?50?= 14 μM)。在体外有抗癌活性。
- GC46226 SS-208 An HDAC6 inhibitor
- GC46213 Ro 41-0960 A COMT inhibitor
- GC46152 GS-441524 An antiviral nucleoside analog
- GC46148 Filgotinib-d4 An internal standard for the quantification of filgotinib
- GC46104 Butyric Acid-d7 An internal standard for the quantification of sodium butyrate
- GC39180 PROTAC BRD4 ligand-1 PROTAC BRD4 ligand-1 是一种有效的 BET 抑制剂,是靶向 BRD4 蛋白的配体。
- GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling
- GC39081 Reticuline Reticuline 分离自 Litsea cubeba,通过 JAK2/STAT3 和 NF-κB 信号通路显示抗炎作用。Reticuline 还可抑制 TNF-α 和 IL-6 的 mRNA 表达,并降低 JAK2 和 STAT3 的磷酸化水平。
- GC38839 Pseudoprotodioscin A steroidal saponin with diverse biological activities
- GC38767 Deoxyshikonin Deoxyshikonin 是从 Lithospermum erythrorhizon Sieb 中分离得到的,具有抗肿瘤活性。
- GC38742 BRD-6929 An HDAC1 and HDAC2 inhibitor
- GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7
- GC45908 (R)-BAY-598 An inhibitor of SMYD2
- GC45906 MC1742 An inhibitor of class I and class IIb HDACs
- GC45808 OUL35 An inhibitor of PARP10
- GC45772 6(5H)-Phenanthridinone An inhibitor of PARP1 and 2
- GC45763 Tolcapone-d4 An internal standard for the quantification of tolcapone
- GC45717 Chlamydocin An HDAC inhibitor
- GC45609 ZLD1039 An inhibitor of EZH2
- GC38709 KDOAM-25 citrate KDOAM-25 citrate 是有效,高选择性的 KDM5 抑制剂,对 KDM5A,KDM5B,KDM5C,KDM5D 的 IC50 分别为 71 nM,19 nM,69 nM,69 nM。KDOAM-25 citrate 可增加转录起始位点的整体 H3K4 甲基化,并损害多发性骨髓瘤 MM1S 细胞的增殖。
- GC38519 Ilorasertib hydrochloride A multi-kinase inhibitor
- GC38474 MS645 MS645 是一种 BET bromodomains (BrD) 抑制剂,对于 BRD4-BD1/BD2 的 Ki 值为 18.4 nM。MS645 在空间上限制 BRD4 BrDs 的二价抑制,从而导致实体肿瘤细胞中 BRD4 转录活性的持续抑制。
- GC38469 CBP/p300-IN-3 P300/CBP-IN-3, a p300/CBP 组蛋白乙酰转移酶 (histone acetyltransferase) 抑制剂,化合物 6,来源于专利 WO 2019049061 A1。
- GC38412 Crotonoside A guanosine analog with diverse biological activities
- GC38163 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) 是一种有效,选择性,口服的 EZH2 抑制剂。Tazemetostat hydrobromide 抑制含有 PRC2 复合体的野生型 EZH2 的活性, Ki 值为 2.5±0.5 nM。Tazemetostat hydrobromide 抑制 EZH2,在肽测定和核小体测定中 IC50 分别为 11 和 16 nM。Tazemetostat hydrobromide 抑制大鼠 EZH2,IC50 为 4 nM。Tazemetostat hydrobromide 还抑制 EZH1,IC50 为 392 nM。
- GC38062 Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
- GC38049 GSK8573 GSK8573 是 GSK2801 的非活性对照化合物。GSK8573 与 BRD9 具有结合活性,Kd 值为 1.04 μM,并且对 BAZ2A/B 和其他溴结构域家族无抑制活性。
- GC38044 Fraxinellone A liminoid degradant with diverse biological activities
- GA20605 Ac-Lys-AMC Ac-Lys-AMC(己酰胺),也称为 MAL,是组蛋白去乙酰化酶 HDAC 的荧光底物。