Description
PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.
Product information
CAS Number: 2639882-72-5
Molecular Weight: 1054.20
Formula: C55H60FN11O8S
Chemical Name: (2S, 4R)-1-[(2S)-2-{2-[4-(2-{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}ethoxy)phenoxy]acetamido}-3, 3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1, 3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide
Smiles: CC1=NC(CCC(=O)NCCOC2C=CC(=CC=2)OCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCC2C=CC(=CC=2)C2SC=NC=2C)C(C)(C)C)=CC=C1C1=CN=C(NCC2=C(F)C=CC3OCCC2=3)N2C=NN=C21
InChiKey: FSFJUWLIBSALJI-FENRPDQVSA-N
InChi: InChI=1S/C55H60FN11O8S/c1-32-40(43-27-60-54(67-30-62-65-51(43)67)59-26-42-41-20-22-74-46(41)18-17-44(42)56)16-10-36(63-32)11-19-47(69)57-21-23-73-38-12-14-39(15-13-38)75-29-48(70)64-50(55(3,4)5)53(72)66-28-37(68)24-45(66)52(71)58-25-34-6-8-35(9-7-34)49-33(2)61-31-76-49/h6-10,12-18,27,30-31,37,45,50,68H,11,19-26,28-29H2,1-5H3,(H,57,69)(H,58,71)(H,59,60)(H,64,70)/t37-,45+,50-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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-1 (Compound PROTAC 2) binds to EED with a pKD of 9.02±0.09 and inhibits PRC2 function with a pIC50 of 8.17±0.24. PROTAC EED degrader-1 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422. PROTAC EED degrader-1 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells. PROTAC EED degrader-1 (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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