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
GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling
GC39081 Reticuline
番荔枝碱
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
伪原薯蓣皂苷
A steroidal saponin with diverse biological activities
GC38767 Deoxyshikonin
去氧紫草素
Deoxyshikonin 是从 Lithospermum erythrorhizon Sieb 中分离得到的，具有抗肿瘤活性。
GC38742 BRD-6929
JQ12
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
NSC39047
An inhibitor of PARP10
GC45772 6(5H)-Phenanthridinone
6(5H)-菲啶酮
An inhibitor of PARP1 and 2
GC45763 Tolcapone-d4
托卡朋-D4,Ro 40-7592-d4
An internal standard for the quantification of tolcapone
GC45717 Chlamydocin An HDAC inhibitor
GC45640 TP-238 (hydrochloride) A chemical probe for the bromodomains of CECR2 and BPTF
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
ABT-348 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
巴豆苷; Isoguanosine
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
新藤黄酸
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
梣酮
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。
GA20481 Ac-Arg-Gly-Lys(Ac)-AMC Ac-Arg-Gly-Lys(Ac)-AMC 是 HDAC 的底物。
GC45548 Photoswitchable PAD Inhibitor (technical grade) A photoactivated PAD inhibitor
GC45503 L-Moses (hydrochloride)
L-45
A PCAF bromodomain inhibitor
GC45489 K-Biotin-W-Histone H2B (108-125) (trifluoroacetate salt)
Histone H2BK-Biotin (108-125), K(Biotin)-W-Histone H2B (108-125), K(Biotin)WKHAVSEGTKAVTKYTSSK
A biotinylated peptide fragment of histone H2B
GC45485 Histone H4R3Me2s (1-21)-GGK-biotin (trifluoroacetate salt)
Ac-SG-R(me2s)-GKGGKGLGKGGAKRHRKV-GGK(Biotin), Arg(Me2s)3-Histone H4 (1-21)-GGK(Biotin), Histone H4 (1-21) (Arg3me2s)
A biotinylated peptide fragment of histone H4
GC45484 Histone H3K9Me3 (3-17) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)
H-Thr-Lys-Gln-Thr-Ala-Arg-Lys(Me3)-Ser-Thr-Gly-Gly-Lys-Ala-Pro-Arg-OH, H3K9me3, Histone H3 (3-17) (Lys9me3), Lys(Me3)9-Histone H3 (3-17), TKQTAR-K(Me3)-STGGKAPR
A peptide fragment of histone H3
GC45483 Histone H3K9Me2 (3-17) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)
Histone H3 (3-17) (Lys9me2), H-Thr-Lys-Gln-Thr-Ala-Arg-Lys(Me2)-Ser-Thr-Gly-Gly-Lys-Ala-Pro-Arg-OH, Lys(Me2)9-Histone H3 (3-17), TKQTAR-K(Me2)-STGGKAPR
A peptide fragment of histone H3
GC45482 Histone H3K9Me1 (3-17) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)
Histone H3 (3-17) (Lys9me1), Lys(Me1)9-Histone H3 (3-17), TKQTAR-K(Me1)-STGGKAPR
A peptide fragment of histone H3
GC45481 Histone H3K79Me1 (69-89) amide (human, mouse, rat, bovine) (trifluoroacetate salt)
Histone H3 (69-89) (Lys79me1) amide, Lys(Me1)79-Histone H3 (69-89) amide, RLVREIAQDF-K(Me1)-TDLRFQSSAV-NH2
A peptide fragment of histone H3
GC45480 Histone H3K4Me3 (1-25) amide (human mouse, rat, porcine, bovine) (trifluoroacetate salt)
ART-K(Me3)-QTARKSTGGKAPRKQLATKAA-NH2, Histone H3 (1-25) (Lys4me3), H3K4me3, Lys(Me3)4-Histone H3 (1-25) amide

A peptide fragment of histone H3
GC45479 Histone H3K36Me3 (31-41) (trifluoroacetate salt)
Histone H3 (31-41) (Lys36me3), Lys(Me3)36-Histone H3 (31-41), STGGV-K(Me3)-KPHRY
A peptide fragment of histone H3
GC45478 Histone H3K36Me3 (26-46)-K-biotin (trifluoroacetate salt)
Histone H3 (26-46) (Lys36me3), Lys(Me3)36-Histone H3 (26-46)-K(Biotin), RKAAPATGGV-K(Me3)-KPHRYRPGTV-K(biotin)
A peptide fragment of histone H3
GC45477 Histone H3K14Ac/K18Ac/K23Ac/K27Ac (1-30)-GGK-biotin (trifluoroacetate salt)
ARTKQTARKSTGG-K(Ac)-APR-K(Ac)-QLAT-K(Ac)-AAR-K(Ac)-SAPGG-K(biotin), Histone H3 (1-30) (Lys14ac/Lys18ac/Lys23ac/Lys27ac), Lys(Ac)14/18/23/27-Histone H3 (1-30)-GGK(biotin)
A biotinylated fragment of histone H3
GC45476 Histone H3K14Ac/H3K23Ac (1-24)-GGK-biotin (trifluoroacetate salt)
ARTKQTARKSTGG-K(Ac)-APRKQLAT-K(Ac)-AGG-K(Biotin), Histone H3 (1-24) (Lys14ac/Lys23ac), Lys(Ac)14/23-Histone H3 (1-24)-GGK(Biotin)
A biotinylated peptide fragment of histone H3
GC45475 Histone H3 (1-35) (human, mouse, rat, bovine) (trifluoroacetate salt)
ARTKQTARKSTGGKAPRKQLATKAARKSAPATGGV
A peptide fragment of histone H3
GC45474 Histone H3 (1-25) amide (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)
ARTKQTARKSTGGKAPRKQLATKAA-NH2
A peptide fragment of histone H3
GC45402 CAY10729 (trifluoroacetate salt) (technical grade) A PAD1 inhibitor
GC45389 BAY-6035 An inhibitor of SMYD3
GC37971 ZM39923 A potent inhibitor of JAK3
GC37966 ZINC13466751 ZINC13466751 是一种 HIF-1α/von Hippel-Lindau 相互作用的有效抑制剂，IC50 值为 2.0 ?M。
GC37956 YUKA1 YUKA1 是一种有效、可透过细胞的赖氨酸脱甲基化酶 (KDM5A) 抑制剂，IC50 值为 2.66 μM，对 KDM5C 的作用较弱，IC50 值为 7.12 μM，对 KDM5B，KDM6A 或 KDM6B 无作用。YUKA1 可增加人细胞中 H3K4me3 的水平，具有抗肿瘤活性。
GC37889 VCE-004.8
VCE-?004.8
VCE-004.8 (VCE-004.8) 是一种具有口服活性的特异性 PPARγ；和 CB2 受体双重激动剂。
GC37881 Valemetostat tosylate
DS-3201 tosylate
Valemetostat tosylate (DS-3201 tosylate) 是一种首创的 EZH1/2 抑制剂，用于复发/难治性周围 T 细胞淋巴瘤的研究。
GC37856 UNC0321 A highly potent inhibitor of G9a histone methyltransferase
GC37847 Tyk2-IN-8 Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).
GC37846 Tyk2-IN-7 Tyk2-IN-7 (Compound 48) 是 TYK2 JH2 抑制剂，与 TYK2 JH2 结构域结合，IC50 和 Ki.app 分别为 0.00053 μM 和 0.00007 μM。Tyk2-IN-7 (Compound 48) 是常规 TYK2 正构抑制剂的高选择性替代，抑制 TYK2/JAK1/JAK2 激酶结构域。Tyk2-IN-7 (Compound 48) 抑制小鼠 IL-12 诱导的 IFNγ 药效学模型中以及抑制在 IL-23 和 IL-12 依赖性小鼠结肠炎模型中的功效。