Description
PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.
Product information
CAS Number: 2639882-69-0
Molecular Weight: 960.13
Formula: C50H58FN11O6S
Chemical Name: (2S, 4R)-1-[(2S)-2-(5-{3-[5-(5-{[(5-fluoro-2, 3-dihydro-1-benzofuran-4-yl)methyl]amino}-[1, 2, 4]triazolo[4, 3-c]pyrimidin-8-yl)-6-methylpyridin-2-yl]propanamido}pentanamido)-3, 3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1, 3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide
Smiles: CC1N=CSC=1C1=CC=C(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCNC(=O)CCC2=CC=C(C3=CN=C(NCC4=C(F)C=CC5OCCC4=5)N4C=NN=C43)C(C)=N2)C(C)(C)C)C=C1
InChiKey: CQSOTYMFUWTIIR-HUSBZTEESA-N
InChi: InChI=1S/C50H58FN11O6S/c1-29-35(38-25-55-49(62-27-57-60-46(38)62)54-24-37-36-19-21-68-41(36)17-16-39(37)51)15-13-33(58-29)14-18-42(64)52-20-7-6-8-43(65)59-45(50(3,4)5)48(67)61-26-34(63)22-40(61)47(66)53-23-31-9-11-32(12-10-31)44-30(2)56-28-69-44/h9-13,15-17,25,27-28,34,40,45,63H,6-8,14,18-24,26H2,1-5H3,(H,52,64)(H,53,66)(H,54,55)(H,59,65)/t34-,40+,45-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (104.15 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pKD of 9.27±0.05 and inhibits PRC2 function with a pIC50 of 8.11±0.09. PROTAC EED degrader-2 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422. PROTAC EED degrader-2 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells. PROTAC EED degrader-2 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells.
Products are for research use only. Not for human use.
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