Histone Methyltransferase(组蛋白甲基转移酶)

Histone methyltransferases are a group of enzymes that catalyze the methylation of histone lysine and arginine by adding methyl groups to specific histone arginine or lysine residues. Histone methyltransferaes can be classified into 3 classes, including SET domain lysine methyltransferases, non-SET domain lysine methyltransferases and arginine methyltransferases (PRMTs), all of which use S-adenosylmethionine as a cosubstrate for the transfer of the methyl group. Aberrant histone methylation has been associated with a wide range of human cancers (such as hematological malignancies), which leads to the development of novel cancer chemotherapies targeting cancer-associated histone methyltransferases (more than 20 lysine methyltransferases and 9 arginine methyltransferases in humans).

Products for Histone Methyltransferase

dummy(1)

Cat.No. 产品名称 Information
GC18642 SW155246 A DNA methyltransferase 1 inhibitor
GC62390 SW2_110A SW2_110A 是一种选择性 chromobox 8 chromodomain (CBX8 ChD) 抑制剂，Kd 为 800 nM。SW2_110A 在体外对 CBX8 ChD 的选择性比所有其他 CBX 旁系同源物低 5 倍。
GC69980 SW2_152F SW2_152F 是一种有效的选择性 chromobox 2 chromodomain (CBX2 ChD) 抑制剂，Kd 为 80 nM。SW2_152F 在体外对 CBX2 ChD 的选择性比其他 CBX paralogs 高 24-1000 倍。
GC67676 Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) 是一种 EZH2 降解剂，可以用于淋巴瘤的研究。
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。
GC17672 TC-E 5003

N,N'-[磺酰基二(4,1-亚苯基)]二(2-氯乙酰胺)
A PRMT1 inhibitor
GC73681 TNG-462 TNG-462是一种口服活性和选择性PRMT5抑制剂，具有抗甲硫腺苷磷酸化酶（MTAP）缺乏和/或甲硫腺苷（MTA）积聚癌症的抗肿瘤活性。
GC70041 TNG908 TNG908 是一种可通过血脑屏障的 MTAP-协同 PRMT5 抑制剂，TNG908 对 MTAPnull 细胞系的选择性比 MTAPWT 细胞系高 15倍，可用于癌症研究。
GC45763 Tolcapone-d4

托卡朋-D4,Ro 40-7592-d4
An internal standard for the quantification of tolcapone
GC41263 TP-064 A potent inhibitor of PRMT4
GC15688 UNC 0224 A potent inhibitor of G9a histone methyltransferase
GC12548 UNC 0631 An inhibitor of G9a/GLP methyltransferases
GC14249 UNC 0642

2-(4,4-二氟-1-哌啶基)-6-甲氧基-N-[1-异丙基-4-哌啶基]-7-[3-(1-吡咯烷基)丙氧基]-4-喹唑啉胺
A G9a histone methyltransferase inhibitor
GC16518 UNC 0646

N-(1-环己基-4-哌啶基)-2-[六氢-4-异丙基-1H-1,4-二氮杂卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺
An inhibitor of G9a/GLP methyltransferases
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。
GC15652 UNC 2400 UNC 2400 与 UNC1999 非常相似，作为细胞研究的阴性对照，其效力比 UNC1999 低 1,000 倍以上。
GC37856 UNC0321 A highly potent inhibitor of G9a histone methyltransferase
GC16741 UNC0379 A selective SET8 inhibitor
GC34160 UNC0379 trifluoroacetate (UNC-0379 trifluoroacetate) A selective SET8 inhibitor
GC15610 UNC0638 A G9a and GLP histone methyltransferase inhibitor
GC16794 UNC1215

UNC 1215;UNC-1215
Potent L3MBTL3 domain inhibitor
GC11375 UNC1999 A selective, cell-permeable EZH2 inhibitor
GC45117 UNC2327 An allosteric inhibitor of PRMT3
GC17207 UNC3866 An inhibitor of CBX7
GC70091 UNC4976 TFA UNC4976 TFA 是一种 CBX7 染色质结构域与核酸结合的正变构调节剂 (PAM) 拟肽。UNC4976 TFA 拮抗 H3K27me3 特异性募集 CBX7 至靶基因，同时增加与 DNA 和 RNA 的非特异性结合。
GC18096 UNC669 A selective MBT inhibitor
GC64083 UNC6934 UNC6934 is a a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2. UNC6934 is a potent antagonist of NSD2-PWWP1 with a Kd (SPR) of 80 nM and is selective for NSD2-PWWP1 over 14 other PWWP domains including NSD3-PWWP1 UNC6934 disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 μM.
GC91061 UNC8153 (trifluoroacetate salt)
NSD2的降解剂
GC33397 Valemetostat

DS-3201
A dual EZH1 and EZH2 inhibitor
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。
GC14763 WDR5 0103

WD-Repeat Protein 5-0103
An inhibitor of WDR5 peptide binding
GC62558 WDR5-IN-1 WDR5-IN-1 是一种有效的选择性 WD 重复结构域 5 (WDR5) 抑制剂，Kd 为 <0.02 nM。WDR5-IN-1 抑制 MLL1 组蛋白甲基转移酶活性 (HMT)，IC50为 2.2 nM。WDR5-IN-1 减少 WDR5 移位基因的 MYC 募集，并在 CHP-134 (神经母细胞瘤) 和 Ramos (Burkitt淋巴瘤) 细胞系中显示出有效的抗增殖作用。
GC73315 WDR5-IN-5 WDR5-IN-5是WD重复结构域5 (WDR5) WIN位点的口服选择性抑制剂。
GC73478 WM-586 WM-586是一种共价WDR5抑制剂，可破坏WDR5与MYC的结合。
GC73306 XF067-68 XF067-68是靶向降解WD40重复结构域蛋白5 （WDR5）的PROTAC（专利号WO2019246570A1）。
GC19388 XY1

N-2-萘基-N'-[2-氧代-2-(1-吡咯烷基)乙基]脲
A negative control for SGC707
GC45609 ZLD1039 An inhibitor of EZH2
GC73630 ZZM-1220 ZZM-1220是一种组蛋白赖氨酸金属转移酶G9a/GLP共价抑制剂，IC50分别为458 nM和924 nM。