Chromatin/Epigenetics
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.
- Bromodomain(50)
- Aurora Kinase(63)
- DNA Methyltransferase(35)
- HDAC(210)
- Histone Acetyltransferases(78)
- Histone Demethylases(110)
- Histone Methyltransferase(240)
- HIF(102)
- JAK(173)
- MBT Domains(1)
- PARP(122)
- Pim(32)
- Protein Ser/Thr Phosphatases(34)
- RNA Polymerase(7)
- Sirtuin(77)
- Sphingosine Kinase-2(1)
- Polycomb repressive complex(2)
- SUMOylation(3)
- PAD(21)
- Epigenetic Reader Domain(246)
- MicroRNA(24)
- Protein Arginine Deiminase(7)
- Chromodomain(1)
- Citrullination(20)
- DNA/RNA Demethylation(2)
- DNA/RNA Methylation(8)
- Histone Deacetylation(44)
- 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)
Chromatin/Epigenetics 相关产品(1617)
- GC31866JAK inhibitor 1CAS: 2096999-92-5
JAK inhibitor 1 是从专利 US20170121327A1 化合物实施例 283 中提取的 JAK 抑制剂。
- GC31881MS417 (GTPL7512)CAS: 916489-36-6纯度: >99.50%
MS417 (GTPL7512) 是一种选择性 BET 特异性 BRD4 抑制剂,与 BRD4-BD1 和 BRD4-BD2 结合,IC50 分别为 30、46 nM 和 Kds 分别为 36.1、25.4 nM,对 CBP BRD 的选择性较弱 (IC50, 32.7 μ ;M)。
- GC31887KDM4D-IN-1CAS: 2098902-68-0纯度: >99.50%
KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.
- GC31902JAK3-IN-6CAS: 1443235-95-7纯度: >98.00%
Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.
- GC32023Abrocitinib (PF-04965842)CAS: 1622902-68-4纯度: >98.00%
Abrocitinib (PF-04965842)是一种口服活性且选择性的Janus激酶(JAK)抑制剂,对JAK1和JAK2的IC 50 值分别为29nM和803nM。
- GC32081GNE-781CAS: 1936422-33-1纯度: >98.00%
GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.
- GC32435Targapremir-210CAS: 1049722-30-6纯度: >98.00%
Targapremir-210是有效的miR-210抑制剂,作用于MDA-MB-231细胞系的IC50值为200nM。Targapremir-210通过和miR-210的发夹前体结构结合,进而抑制miRNA的成熟。
- GC32693GSK3326595 (EPZ015938)CAS: 1616392-22-3纯度: >99.50% / >99.00%
GSK3326595 (EPZ015938) 是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5(PRMT5)抑制剂。
- GC32724LW6 (HIF-1α inhibitor)CAS: 934593-90-5纯度: >98.00%
LW6是一种缺氧诱导因子1(hypoxia inducing factor 1, HIF)抑制剂,通过降解HIF-1α有效抑制HIF-1α的积累,但不影响缺氧时HIF- 1a mRNA水平。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC31731 | GSK 4027 | 2079896-25-4 | >98.50% | |
A PCAF/GCN5 bromodomain inhibitor | ||||
| GC31831 | BET-IN-1 | 1422554-34-4 | >99.00% | |
BET-IN-1 是所有八个 BET 溴结构域的泛抑制剂,并且比其他具有代表性的含溴结构域的蛋白质具有选择性。 | ||||
| GC31866 | JAK inhibitor 1 | 2096999-92-5 | - | |
JAK inhibitor 1 是从专利 US20170121327A1 化合物实施例 283 中提取的 JAK 抑制剂。 | ||||
| GC31881 | MS417 (GTPL7512) | 916489-36-6 | >99.50% | |
MS417 (GTPL7512) 是一种选择性 BET 特异性 BRD4 抑制剂,与 BRD4-BD1 和 BRD4-BD2 结合,IC50 分别为 30、46 nM 和 Kds 分别为 36.1、25.4 nM,对 CBP BRD 的选择性较弱 (IC50, 32.7 μ ;M)。 | ||||
| GC31887 | KDM4D-IN-1 | 2098902-68-0 | >99.50% | |
KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM. | ||||
| GC31902 | JAK3-IN-6 | 1443235-95-7 | >98.00% | |
Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK. | ||||
| GC31999 | JAK-IN-1 | 1334673-53-8 | - | |
JAK-IN-1是JAK1/2/3抑制剂,IC50分别为0.26,0.8和3.2nM。JAK-IN-1对JAK3的选择性比JAK1高。 | ||||
| GC32023 | Abrocitinib (PF-04965842) | 1622902-68-4 | >98.00% | |
Abrocitinib (PF-04965842)是一种口服活性且选择性的Janus激酶(JAK)抑制剂,对JAK1和JAK2的IC 50 值分别为29nM和803nM。 | ||||
| GC32028 | BMS-066 | 914946-88-6 | - | |
BMS-066是IKKβ/Tyk2的抑制剂,其IC50值分别为9nM,72nM。 | ||||
| GC32052 | Tyk2-IN-3 | 1779493-12-7 | - | |
Tyk2-IN-3是Tyk2pseudokinase的一个抑制剂,其IC50值为485nM。 | ||||
| GC32081 | GNE-781 | 1936422-33-1 | >98.00% | |
GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity. | ||||
| GC32083 | Acriflavine | 8048-52-0 | >98.00% | |
Acriflavine是用于标记高分子量RNA的荧光染料。它也是一种局部防腐剂。 | ||||
| GC32228 | Tilorone dihydrochloride | 27591-69-1 | >99.50% | |
An interferon-inducing antiviral agent | ||||
| GC32435 | Targapremir-210 | 1049722-30-6 | >98.00% | |
Targapremir-210是有效的miR-210抑制剂,作用于MDA-MB-231细胞系的IC50值为200nM。Targapremir-210通过和miR-210的发夹前体结构结合,进而抑制miRNA的成熟。 | ||||
| GC32449 | Desidustat | 1616690-16-4 | >98.00% | |
An inhibitor of HIF-PH | ||||
| GC32565 | CRA-026440 | 847460-34-8 | - | |
CRA-026440 是一种有效的广谱 HDAC 抑制剂。 | ||||
| GC32677 | A-485 | 1889279-16-6 | >99.50% / >98.00% | |
A-485是有效的选择性p300/CBP(组蛋白乙酰转移酶旁系同源物/CREB结合蛋白)的催化抑制剂,对p300 HAT的IC 50 值为60nM。A-485可抑制p300-BHC(溴域HAT-C/H3)和CBP-BHC结构域的活性,IC 50 分别为9.8nM和2.6nM。 | ||||
| GC32680 | PT-2385 | 1672665-49-4 | >99.00% | |
PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity. | ||||
| GC32685 | ARV-771 | 1949837-12-0 | >99.50% | |
ARV-771是一种泛BET-PROTAC,能有效降解BRD2/3/4蛋白,DC 50 值低于5nM。 | ||||
| GC32689 | 666-15 | 1433286-70-4 | >99.50% | |
666-15是一种选择性环磷酸腺苷反应元件结合蛋白(CREB)抑制剂,IC 50 值为0.081±0.04μM。 | ||||
| GC32693 | GSK3326595 (EPZ015938) | 1616392-22-3 | >99.50% / >99.00% | |
GSK3326595 (EPZ015938) 是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5(PRMT5)抑制剂。 | ||||
| GC32699 | QC6352 | 1851373-36-8 | >98.00% | |
QC6352是一种有效的KDM4C抑制剂,其IC50值为35nM。 | ||||
| GC32719 | dBET6 | 1950634-92-0 | >99.50% | |
dBET6是一种新型的、具有口服活性的BRD4降解剂,可抑制c-Myc等致癌基因的转录和表达。 | ||||
| GC32724 | LW6 (HIF-1α inhibitor) | 934593-90-5 | >98.00% | |
LW6是一种缺氧诱导因子1(hypoxia inducing factor 1, HIF)抑制剂,通过降解HIF-1α有效抑制HIF-1α的积累,但不影响缺氧时HIF- 1a mRNA水平。 | ||||
