GlpBio

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.

研究方向

Chromatin/Epigenetics 相关产品(1617)

  • GC34784 structure
    GC34784Sinefungin
    CAS: 58944-73-3
    纯度: >95.00%

    Sinefungin是一种S-腺苷甲硫氨酸类似物的天然核苷类抗生素，可抑制多种甲基转移酶（包括蛋白、DNA和RNA甲基转移酶）的活性。

  • GC34785 structure
    GC34785Sirt2-IN-1
    CAS: 1862238-00-3
    纯度: >98.00%

    Sirt2-IN-1(Compound9)是一种sirtuin2(Sirt2)抑制剂，IC50为163nM。

  • GC34849 structure
    GC34849UBCS039
    CAS: 358721-70-7
    纯度: >98.50%

    UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines.

  • GC34958 structure
    GC34958(+)-JQ1 PA
    CAS: 2115701-93-2
    纯度: >98.50%

    A clickable form of (+)-JQ1

  • GC34964 structure
    GC34964(1S,3R,5R)-PIM447 dihydrochloride
    纯度: >98.00%

    (1S,3R,5R)-PIM447 (dihydrochloride)是PIM的抑制剂，来自专利US 20100056576 A1化合物实例72。对Pim1，Pim2和Pim3的IC50分别为0.095，0.522和0.369 μM。

  • GC34971 structure
    GC34971(3R,4S)-Tofacitinib
    CAS: 1092578-46-5

    Tofacitinib(CP-690550)是高效JAK3抑制剂，IC50为1 nM，比对JAK2和JAK1的抑制性高20倍和100倍。

  • GC34972 structure
    GC34972(3S,4R)-Tofacitinib
    CAS: 1092578-48-7

    Tofacitinib(CP-690550)是高效JAK3抑制剂，IC50为1 nM，比对JAK2和JAK1的抑制性高20倍和100倍。

  • GC34973 structure
    GC34973(3S,4S)-Tofacitinib
    CAS: 1092578-47-6
    纯度: >99.00%

    Tofacitinib(CP-690550)是高效JAK3抑制剂，IC50为1 nM，比对JAK2和JAK1的抑制性高20倍和100倍。

  • GC35150 structure
    GC351505,7,4'-Trimethoxyflavone
    CAS: 5631-70-9
    纯度: >99.50%

    4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.

  • GC35175 structure
    GC351756-Demethoxytangeretin
    CAS: 6601-66-7
    纯度: >99.00%

    6-?Demethoxytangeretin 6-去甲氧基三苯甲基黄嘌呤是从柑橘 (Citrus depressa) 分离的黄酮。 6-Demethoxytangeretin 具有抗炎和抗过敏活性，通过间变性淋巴瘤激酶 (ALK) 和丝裂原活化蛋白激酶 (MAPK) 途径抑制人肥大细胞中 IL-6 的产生和基因表达。6-?Demethoxytangeretin 促进 CRE 介导的转录 (与海马神经元的学习和记忆相关)。

  • GC35180 structure
    GC351806-Methyl-5-azacytidine
    CAS: 105330-94-7

    6-Methyl-5-azacytidine 是一种有效的甲基转移酶抑制剂。

  • GC35216 structure
    GC35216AAPK-25
    CAS: 2247919-28-2

    AAPK-25 是一种有效选择性的 Aurora/PLK 激酶双重抑制剂，具有抗肿瘤活性。AAPK-25 可引起有丝分裂延迟并阻滞前中期细胞，通过生物标志物组蛋白 H3Ser10 磷酸化反应，随后细胞凋亡激增。AAPK-25 靶向 Aurora-A, -B, -C 的 Kd 值为 23 nM-289 nM，靶向 PLK-1, -2, -3 的 Kd 值为 55-456 nM。

  • GC35227 structure
    GC35227ACBI1
    CAS: 2375564-55-7
    纯度: >98.00%

    ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 induces anti-proliferative effects and apoptosis.

  • GC35230 structure
    GC35230Acetylarenobufagin
    CAS: 184673-79-8

    Acetylarenobufagin 是一种类固醇缺氧诱导因子-1 (HIF-I) 调节剂。

  • GC35297 structure
    GC35297Alobresib
    CAS: 1637771-14-2
    纯度: >98.00%

    A BET bromodomain inhibitor

  • GC35447 structure
    GC35447AZD1208 hydrochloride
    CAS: 1621866-96-3

    A pan-Pim kinase inhibitor

  • GC35448 structure
    GC35448AZD5153 6-Hydroxy-2-naphthoic acid
    CAS: 1869912-40-2
    纯度: >99.50%

    AZD-5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD-5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.

  • GC35505 structure
    GC35505BET-BAY 002
    CAS: 1588521-78-1
    纯度: >99.50%

    BET-BAY 002是BET小分子抑制剂，对多发性骨髓瘤模型有效。

  • GC35506 structure
    GC35506BET-BAY 002 S enantiomer
    CAS: 2070009-49-1

    BET-BAY 002 S enantiomer 是 BET-BAY 002 的 S 型对映异构体。BET-BAY 002 是 BET 抑制剂。

  • GC35547 structure
    GC35547BR102375
    CAS: 2366255-59-4

    BR102375 是一种用于治疗 2 型糖尿病的 non-TZD (噻唑烷二酮类) PPAR γ 完全激动剂， 其 EC50 值和 Amax比率值分别为 0.28 μM 和 98%。

  • GC35550 structure
    GC35550BRCA1-IN-2
    CAS: 1622262-55-8
    纯度: >98.00%

    BRCA1-IN-2 (compound 15) 是具有细胞渗透性的 BRCA1 蛋白-蛋白相互作用 (PPI) 的抑制剂，IC50 值 0.31 μM，Kd 值为 0.3 μM， BRCA1-IN-2 通过阻断 BRCA1 (BRCT)2/ 蛋白质相互作用而具有抗肿瘤活性。

  • GC35551 structure
    GC35551BRD 4354 ditrifluoroacetate

    BRD 4354 (ditrifluoroacetate) 是 HDAC5 和 HDAC9 抑制剂，其 IC50 值分别为 0.85，1.88 μM。

  • GC35552 structure
    GC35552BRD-IN-3
    CAS: 2351938-32-2

    BRD-IN-3 ((R,R)-36n) 是一个强效的P300/CBP 相关因子溴端结构域 (PCAF BRD) 的抑制剂，其IC50 值为 7 nM。BRD-IN-3 也能抑制GCN5 和FALZ。

  • GC35554 structure
    GC35554Brevilin A
    CAS: 16503-32-5
    纯度: >98.00%

    A sesquiterpene lactone with anticancer activity