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
- Cat.No. 产品名称 Information
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GC16015
A 366
A potent inhibitor of G9a
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GC10259
BRD4770
HMTase Inhibitor VI
An inhibitor of EHMT2/G9a -
GC10021
CPI-360
A selective EZH2 inhibitor
-
GC17956
PFI-2
(R)-PFI-2
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride 是一种有效的选择性 SET 结构域,含有赖氨酸甲基转移酶 7 (SETD7) 抑制剂。 -
GC16741
UNC0379
A selective SET8 inhibitor
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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 -
GC16130
C 21
Protein arginine methyltransferase 1 (PRMT1) inhibitor
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GC17672
TC-E 5003
N,N'-[磺酰基二(4,1-亚苯基)]二(2-氯乙酰胺)
A PRMT1 inhibitor -
GC11340
(R)-PFI 2 hydrochloride
(R)-PFI-2 hydrochloride
A SET7/9 inhibitor -
GC16599
CPI-169
A selective EZH2 inhibitor
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GC15259
EPZ004777 HCl
EPZ004777 HCl 是一种有效的选择性 DOT1L 抑制剂,IC50 为 0.4 nM。
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GC14756
EI1
6-氰基-N-[(1,2-二氢-4,6-二甲基-2-氧代-3-吡啶基)甲基]-1-(1-乙基丙基)-1H-吲哚-4-甲酰胺,KB-145943
A selective inhibitor of EZH2 -
GC13103
AZ505 ditrifluoroacetate
N-环己基-3-[[2-(3,4-二氯苯基)乙基]氨基]-N-[2-[[2-(3,4-二氢-5-羟基-3-氧代-2H-1,4-苯并恶嗪-8-基)乙基]氨基]乙基]丙酰胺二(2,2,2-三氟乙酸盐)
An inhibitor of SMYD2 -
GC13744
AZ505
N-环己基-3-(3,4-二氯苯乙基氨基)-N-[2-[[2-[5-羟基-3-氧代-3,4-二氢-2H-苯并[B][1,4]恶嗪-8-基]乙基]氨基]乙基]丙酰胺
An inhibitor of SMYD2 -
GC12548
UNC 0631
An inhibitor of G9a/GLP methyltransferases
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GC14364
SGI-1027
DNA Methyltransferase Inhibitor II
A DNA methyltransferase inhibitor -
GC11375
UNC1999
A selective, cell-permeable EZH2 inhibitor
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GC14652
MM-102
HMTase Inhibitor IX
An inhibitor of WDR5/MLL interactions -
GC18096
UNC669
A selective MBT inhibitor
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GC14062
EPZ-6438
E-7438,Tazemetostat
EPZ-6438 是一种有效且具有生物利用度的 EZH2 抑制剂,EZH2 是多梳抑制复合物 2 (PRC2) 的催化亚基,可催化组蛋白 H3 (H3K27) 的赖氨酸 27 甲基化,从而抑制含有人 PRC2 的活性抑制常数 Ki 值为 2.5 nM 的野生型 EZH2。
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GC15688
UNC 0224
A potent inhibitor of G9a histone methyltransferase
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GC16256
BVT 948
4-羟基-3,3-二甲基-2H-苯并[G]吲哚-2,5(3H)-二酮
An inhibitor of protein tyrosine phosphatases -
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 -
GC14936
Chaetocin
毛壳素
据报道毛壳素是组蛋白甲基转移酶 (HMT)(例如 SUV39H1)的非特异性抑制剂,从而影响基因表达。 -
GC16794
UNC1215
UNC 1215;UNC-1215
Potent L3MBTL3 domain inhibitor -
GC17534
GSK343
GSK-343;GSK 343
A selective, cell-permeable EZH2 inhibitor -
GC15783
GSK126
EZH2 inhibitor;GSK-126;GSK 126
GSK126(GSK2816126A, GSK2816126)是一种高选择性EZH2甲基转移酶抑制剂,在体外的IC50为12.6~17.4nM;在体内的IC50为9.9nM。 -
GC13383
EPZ004777
EPZ004777 作为一种有效的表观遗传调节剂,可以逆转 TGF-β1 诱导的 T 调节细胞,可用于治疗多种免疫疾病。
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GC11491
SGC 0946
A potent inhibitor of DOT1L
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GC13878
EPZ005687
EPZ 005687,EPZ-005687
A potent, selective inhibitor of EZH2 -
GC17334
Entacapone
恩他卡朋
Entacapone是一种有效的、可逆的、外周作用和具有口服活性的儿茶酚-O-甲基转移酶(COMT)抑制剂,可有效抑制大鼠肝脏总COMT,IC50和Ki值分别为20.1nM和10.7nM。 -
GC12932
EPZ5676
(2R,3R,4S,5R)-2-(6-氨基-9H-嘌呤-9-基)-5-((((1R,3S)-3-(2-(6-(叔丁基)-1H-苯并[D]咪唑-2-基)乙基)环丁基)(异丙基)氨基)甲基)四氢呋喃-3,4-二醇,EPZ-5676
A highly potent DOT1L inhibitor -
GC17907
3-Deazaneplanocin A (DZNep) hydrochloride
3-去氮腺嘌呤A盐酸盐; DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
3-Deazaneplanocin A (DZNep) hydrochloride 是一种腺苷类似物,是一种竞争性 S-腺苷高半胱氨酸水解酶抑制剂,在无细胞试验中的 Ki 为 50 pM。 -
GC15610
UNC0638
A G9a and GLP histone methyltransferase inhibitor
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GC12171
BIX 01294
An inhibitor of G9a histone methyltransferase
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GC17275
AMI-1
猩红酸钠盐,Arginine N - methyltransferase inhibitor - 1
A cell permeable inhibitor of PRMTs -
GC13145
3-Deazaneplanocin,DZNep
3-去氮腺嘌呤A; DZNep; 3-Deazaneplanocin
An inhibitor of lysine methyltransferase EZH2
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GP10020
Histone-H2A-(107-122)-Ac-OH
Ac-Gly-Val-Leu-Pro-Asn-Ile-Gln-Ala-Val-Leu-Leu-Pro-Lys-Lys-Thr-Glu-OH
Histone-H2A peptide