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
GC62187 PROTAC EED degrader-1 PROTAC EED degrader-1 是靶向 EED 的 PROTAC 分子，pKD 为 9.02。PROTAC EED degrader-1 是靶向 EED 亚基的多梳抑制复合物 2 (PRC2) 抑制剂 (pIC50=8.17)。
GC62154 N-Descyclopropanecarbaldehyde Olaparib
1-[5-[(3,4-二氢-4-氧代-1-酞嗪基)甲基]-2-氟苯甲酰基]哌嗪
N-Descyclopropanecarbaldehyde Olaparib 是含有 DOTA 的奥拉帕尼的类似物。Descyclopropanecarbaldehyde Olaparib 是一种 CRBN 配体，可用于合成新型靶向 EGFR 和 PARP 的双靶点 PROTAC，DP-C-4。N-Descyclopropanecarbaldehyde Olaparib 可以用 F-18 或荧光团进行放射性标记用于正电子发射断层扫描 (PET) 或几种类型的肿瘤的光学成像。
GC62145 Chiauranib
CS2164
Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
GC62144 653-47 hydrochloride 653-47 hydrochloride 是一种增强剂，能显著增强 666-15 的 cAMP 反应元件结合蛋白 (CREB) 抑制活性。653-47 hydrochloride 也是一种很弱的抑制剂，其 IC50 为 26.3 μM。
GC62130 (2R,5S)-Ritlecitinib
(2R,5S)-PF-06651600
(2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) 是一种有效的选择性的 JAK3 抑制剂 (IC50=144.8 nM)。详细信息请参考专利US20150158864A1，example 68。
GC62129 Venadaparib
IDX-1197
Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.
GC62121 Fluzoparib
氟唑帕利; SHR3162; Fuzuloparib
Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.
GC62112 Zotiraciclib Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
GC62105 Senaparib
IMP4297
Senaparib (IMP4297) 是强效的、选择性的、口服有效的 PARP1/2 抑制剂。Senaparib (IMP4297) 在动物模型中表现强效的抗肿瘤活性。
GC62104 WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.
GC61995 PKCβ inhibitor 1
3-[1-[3-(1H-咪唑-1-基)丙基]-1H-吲哚-3-基]-4-(苯氨基)-1H-吡咯-2,5-二酮
A PKCβ Inhibitor
GC61949 1,4-DPCA ethyl ester 1,4-DPCA ethyl ester 是 1,4-DPCA 的乙酯形式，可以抑制 FIH。
GC61947 Triciferol Triciferol 是一种具有 VDR 激动剂和 HDAC 拮抗剂联合作用的多配体。Triciferol 直接与 VDR结合 (IC50=87 nM)，在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化，并增强组蛋白乙酰化。抗增殖和细胞毒性活性。
GC61863 Verucopeptin Verucopeptin 是一种有效的 HIF-1 (IC50=0.22 µM) 抑制剂，可以降低 HIF-1 靶基因的表达和 HIF-1α 的蛋白水平。通过直接靶向 v-ATPase ATP6V1G 亚基 (但不靶向 ATP1V1B2 或 ATP6V1D)，Verucopeptin 强烈抑制 v-ATPase 活性。Verucopeptin 对耐药性癌细胞表现出抗肿瘤活性，常用作癌症相关研究。
GC61841 Naphthol AS-E
色酚AS-E
Naphthol AS-E 是有效的，具有细胞渗透性的 KIX-KID 相互作用的抑制剂。Naphthol AS-E 直接结合 CBP 的 KIX 域 (Kd: 8.6 µM)，阻断 KIX 域和 KID 域的相互作用 (IC50: 2.26 µM)。Naphthol AS-E 可用于癌症研究。
GC19747 CX-6258 HCl
Pim-Kinase Inhibitor X
A pan-Pim kinase inhibitor
GC61807 (E/Z)-AG490
酪氨酸磷酸化抑制剂AG490,(E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42

(E/Z)-AG490((E/Z)-TyrphostinAG490)是(E)-AG490和(Z)-AG490的消旋体。(E)-AG490是一种酪氨酸激酶抑制剂，可抑制EGFR，Stat-3和JAK2/3。
GC61669 Ethyl 3,4-dihydroxybenzoate
3,4-二羟基苯甲酸乙酯,Ethyl protocatechuate
Ethyl3,4-dihydroxybenzoate(Ethylprotocatechuate)是一种抗氧化剂，是一种在花生种子的种皮中发现的脯氨酰羟化酶(prolyl-hydroxylase)抑制剂。Ethyl3,4-dihydroxybenzoate通过激活NO合酶(NOsynthase)并产生线粒体ROS来保护心肌。Ethyl3,4-dihydroxybenzoate可诱导ESCC细胞自噬(autophagy)和凋亡(apoptosis)。Ethyl3,4-dihydroxybenzoate是胶原蛋白合成抑制剂，具有骨骼保护作用。
GC61662 5-Fluoro-2'-deoxycytidine
5-氟脱氧胞苷
2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR), a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.
GC61595 (+)-JQ-1-aldehyde (+)-JQ-1-aldehyde是(+)-JQ1的醛形式。(+)-JQ-1-aldehyde可作为合成PROTACs的前体，靶向BET溴结构域.。
GC61577 CBP/p300-IN-1 CBP/p300-IN-1是CBP/EP300溴结构域抑制剂。
GC61468 MR837
4-氰基-N-环丙基-N-(噻吩-2-基甲基)苯甲酰胺
MR837是一种NSD2-PWWP1的抑制剂。MR837可以与人核受体结合SET结构域蛋白(PWWP结构域)结合。
GC48967 D-Homoserine lactone
D-HSL
An enantiomer of L-homoserine lactone
GC48805 Methapyrilene (hydrochloride)
盐酸美沙吡林,Thenylpyramine hydrochloride
An H₁ receptor antagonist and non-genotoxic carcinogen
GC48775 AES-350 An inhibitor of class I and class IIb HDACs
GC48620 BPKDi A PKD inhibitor
GC48600 Panobinostat-d4 (hydrochloride)
LBH589-d4 hydrochloride; NVP-LBH589-d4 hydrochloride
An internal standard for the quantification of panobinostat
GC48495 BMS-P5 A PAD4 inhibitor
GC48463 Bisubstrate Inhibitor 78 An inhibitor of NNMT
GC48460 NR-160 An inhibitor of HDAC6
GC48408 TW9 A dual inhibitor of BRD4 and HDAC1
GC48382 Ac-QPKK(Ac)-AMC
Ac-Gln-Pro-Lys-Lys-(Ac)-AMC, Ac-Gln-Pro-Lys-Lys-(Ac)-7-amino-4-methylcoumarin, p53317-320 Substrate (Ac-QPKK(Ac)-AMC)
A fluorogenic substrate for SIRT1, SIRT2, and SIRT3
GC50721 iP300w Potent p300/CBP inhibitor
GC50699 SGC 6870 Potent and selective protein arginine methyltransferase 6 (PRMT6) inhibitor (IC50 = 77 nM)
GC50697 GSK 591 dihydrochloride A chemical probe for PRMT5
GC50659 BIX NHE1 inhibitor BIX NHE1 inhibitor 是有效的钠氢交换异构体 1 (NHE1) 抑制剂，在细胞内 pH 恢复 (pHi) 和人血小板肿胀试验中的 IC50 分别为 6 和 31 nM。
GC48263 YW3-56 (hydrochloride) (technical grade) A PAD2 and PAD4 inhibitor
GC48084 Sodium 4-Phenylbutyrate-d11
4-PBA-d11 sodium; 4-Phenylbutyric acid-d11 sodium; Benzenebutyric acid-d11 sodium
An internal standard for the quantification of sodium 4-phenylbutyrate
GC48066 SAHO2 A radical SAM enzyme substrate
GC48065 SAHO A radical SAM enzyme substrate
GC47693 m-Methoxybenzamide
3-甲氧基苯甲酰胺,3-MBA
A PARP inhibitor
GC47586 Lysine-specific Demethylase Inhibitor (1C) (hydrochloride) An LSD1 inhibitor
GC47579 L-Pyrohomoglutamic Acid
(S)-2-哌啶酮-6-羧基酸
An amino acid building block
GC47450 IL-4 Inhibitor An IL-4 inhibitor
GC47439 Hydralazine-d4 (hydrochloride)
盐酸肼屈嗪 d4 (盐酸盐)
A neuropeptide with diverse biological activities
GC47432 Histone H3 (69-89) amide (human, mouse, rat, bovine) (trifluoroacetate salt)
RLVREIAQDFKTDLRFQSSAV-NH2
A neuropeptide with diverse biological activities
GC47294 Entacapone-d10
恩他卡朋 d10
An internal standard for the quantification of entacapone
GC47180 Decitabine-15N4
5-aza-2’-Deoxycytidine-15N4, DAC-15N4
A neuropeptide with diverse biological activities
GC47056 CAY10753 A TNKS2 inhibitor
GC47055 CAY10749 A dual inhibitor of PARP and PI3K