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
- GC34160 UNC0379 trifluoroacetate (UNC-0379 trifluoroacetate) A selective SET8 inhibitor
- GC34136 EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate) An orally bioavailable EZH2 inhibitor
- GC34108 CARM1-IN-1 A selective inhibitor of PRMT4/CARM1
- GC33397 Valemetostat A dual EZH1 and EZH2 inhibitor
- GC33320 CM-579 CM-579是一线的、可逆的,G9a和DNA甲基转移酶(DNMT)的双抑制剂,其IC50值分别为16nM和32nM。在多种癌细胞中发挥有效活性作用。
- GC33301 BIX-01338 hydrate (BIX01338 hydrate) BIX-01338 hydrate (BIX01338 hydrate) 是一种组蛋白赖氨酸甲基转移酶抑制剂。
- GC33278 MM-589 MM-589是WD重复结构域5(WDR5)和混合谱系白血病(MLL)相互作用的有效抑制剂。MM-589结合WDR5的IC50为0.90nM。抑制MLLH3K4甲基转移酶活性的IC50为12.7nM。
- GC33220 EBI-2511 EBI-2511是具有口服活性的、EZH2的有效抑制剂,其在Pfeffiera细胞中的IC50值为6nM。
- GC33208 Dot1L-IN-1 Dot1L-IN-1是高效,选择性,结构新颖的Dot1L抑制剂,Ki为2pM。
- GC33187 A-395 (A395) A-395 (A395) 是一种多梳抑制复合物 2 (PRC2) 蛋白质-蛋白质相互作用的拮抗剂,有效抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12),IC50 为 18 nM。
- GC33184 LLY-283 A PRMT5 inhibitor
- GC32988 BRD9539 An inhibitor of EHMT2/G9a and PRC2 in enzyme assays
- GC32977 PF-06726304 PF-06726304是有效,选择性的EZH2抑制剂,Ki值为0.7nM。
- GC32861 A-196 A selective inhibitor of SUV420H1 and SUV420H2
- GC32693 GSK3326595 (EPZ015938) A PRMT5 inhibitor
- GC30530 Dot1L-IN-2 Dot1L-IN-2是一种有效的,选择性的,可口服的Dot1L(一种histonemethyltransferase),IC50值和Ki值分别为0.4nM和0.08nM。
- GC30503 A-893 A-893是一个有细胞活性的,SMYD2的抑制剂,其IC50值为2.8nM。
- GC19465 JNJ-64619178 A PRMT5 inhibitor
- GC19388 XY1 A negative control for SGC707
- GC19329 SGC2085 A PRMT4/CARM1 inhibitor
- GC19211 JQEZ5 An EZH2 inhibitor
- GC19181 GSK2807 Trifluoroacetate GSK2807 Trifluoroacetate 是一种有效的、选择性的、SAM 竞争性的 SMYD3 抑制剂,Ki 为 14 nM,IC50 为 130 nM。
- GC19149 EZM 2302 A PRMT4 inhibitor
- GC19141 EPZ011989 An orally bioavailable EZH2 inhibitor
- GC19130 EED226 A potent and allosteric inhibitor of PRC2
- GC18949 CAY10677 An inhibitor of protein prenylation
- GC18650 S-(5'-Adenosyl)-L-methionine (tosylate) A methyl donor and cofactor
- GC18642 SW155246 A DNA methyltransferase 1 inhibitor
- GC18577 CID-2818500 An inhibitor of PRMT1
- GC18428 SGC2085 (hydrochloride) A PRMT4/CARM1 inhibitor
- GC18161 BCI-121 An inhibitor of SMYD3
- GC18159 BAY-598 An inhibitor of SMYD2
- GC12530 PFI-2 (hydrochloride)
- GC12367 CM-272 An inhibitor of G9a, GLP, and DNA methyltransferases
- GC13634 (S)-PFI-2 (hydrochloride) Negative control of (R)-PFI 2
- GC14240 MS049 (hydrochloride) A selective, dual PRMT4/PRMT6 inhibitor
- GC16432 MS023 (hydrochloride) An inhibitor of type I PRMTs
- GC16298 CPI-1205 EZH2抑制剂
- GC17023 HLCL-61 A PRMT5 inhibitor
- GC10099 MS023 An inhibitor of type I PRMTs
- GC14585 GSK591 A chemical probe for PRMT5
- GC16397 OICR-9429 A probe for WDR5
- GC10905 Amodiaquine dihydrochloride dihydrate A prodrug form of N-desethyl amodiaquine
- GC16509 Adox An irreversible inhibitor of SAH hydrolase
- GC16261 LLY507 A SMYD2 inhibitor
- GC15102 EPZ020411 A PRMT6 inhibitor
- GC17546 AMI5 曙红 Y(二钠)是一种可溶性酸性红色染料分子。
- GC16224 EPZ031686 EPZ031686 是一种有效且具有口服活性的 SMYD3 抑制剂,IC50 值为 3 nM。 EPZ031686 可用于癌症研究。
- GC12874 SGC707 A potent allosteric inhibitor of PRMT3
- GC17207 UNC3866 An inhibitor of CBX7