GNA002|GNA-002

Cas No.:	1385035-79-9
Chemical Name:	(Z)-4-((1S,3aR,5S,12aS)-9-((E)-3,7-dimethylocta-2,6-dien-1-yl)-8,10-dihydroxy-2,2-dimethyl-11-(3-methylbut-2-en-1-yl)-4,7-dioxo-1,2,5,7-tetrahydro-1,5-methanofuro[2,3-d]xanthen-3a(4H)-yl)-N-(2-ethoxyethyl)-2-methylbut-2-enamide
Synonyms:	GNA-002
SMILES:	C(NCCOCC)(=O)/C(/C)=C\C[C@@]12OC(C)(C)[C@]([H])3C[C@@]([H])(C1=O)/C=C1\[C@@]23OC2=C(C\1=O)C(O)=C(C/C=C(\C)/CC/C=C(/C)\C)C(O)=C2C/C=C(/C)\C
Formula:	C₄₂H₅₅NO₈
M.Wt:	701.901
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination; GNA002 is a relatively more potent EZH2 interacting agent than GNA, significantly suppresses H3K27Me3 and effectively reactivated PRC2-silenced tumor suppressor genes.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47618	PRMT5-IN-10	PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex.
DC47617	EED ligand 1	EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
DC47615	PRMT5-IN-9	PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC50 of 0.01 μM.
DC47613	PRMT5-IN-12	PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5.
DC47612	PRMT5-IN-11	PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
DC47611	PRMT5-IN-14	PRMT5-IN-14 is a PRMT5 inhibitor to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
DC47610	PRMT5-IN-3	PRMT5-IN-3 is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
DC47609	PRMT1-IN-1	PRMT1-IN-1 is a PRMT1 inhibitor.
DC47608	EZH2-IN-2	EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
DC47264	MS67	MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.