≥98% para fluxos de trabalho cromatográficos e analíticos sensíveis que exigem interferência mínima da linha de base.
Store at -20°C,Desiccated Envio Ice chest + Ice pads. Consulte o COA específico do lote para obter as especificações exatas.
SDS, COA, ficha técnica e folha de especificações disponíveis para download. COA específico do lote acessível por meio de pesquisa por número de lote.
Citado em 0 publicações revisadas por pares nas áreas de cromatografia, síntese orgânica e reações de acoplamento cruzado.
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a K d of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects
In Vitro
MS67 (0.001-1 μM) induces WDR5 degradation at a concentration as low as 1 nM. MS67 induces WDR5 depletion much more effectively in all six mixed lineage leukemia (MLL)-r acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines without a hook effect and in a concentration-dependent manner in PDAC cells. MS67 decreases H3K4me2/3 in both MV4;11 and MIA PaCa-2 cells, whereas other examined histone methylation marks such as H3K9me3, H3K27me3, and H3K36me3 are not affected . MS67 is effective in suppressing both WDR5-related gene expression programs and WDR5/MLL-induced H3K4 methylations on chromatin. The GI 50 values of MS67 in the two most sensitive AML lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively. MLL-r acute leukemia cell lines including MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1 are sensitive to MS67, whereas leukemia cell lines that did not harbor MLL-r (including K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1) are insensitive to MS67. .\nMS67 binds to VCB (VHL-Elongin C-Elongin B ternary complex), with a K d of 140 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MV4;11 cells Concentration: 0.001 μM, 0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM Incubation Time: 18 hours Result: Induced WDR5 degradation at a concentration as low as 1 nM with DC 50 of 3.7 nM.
In Vivo
MS67 (75 mg/kg; i.p.; twice daily; 5 days a week; for 20 days) significantly inhibits tumor growth in vivo and prolongs survival of the treated mice . After a single intraperitoneal (i.p.) injection of MS67 at a dose of 75 mg/kg, the Cmax reached at about 4.2 μM, and the concentration of MS67 retained above 0.5 μM over 12 hours . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MV4;11 MLL-r AML xenograft mouse Dosage: 75 mg/kg Administration: i.p.; twice daily; 5 days a week; for 20 days Result: Inhibited tumor growth in vivo.
Form:Solid
IC50& Target:VHL WDR5 63 nM (Kd)
Documento abrangente sobre perigos, manuseamento, armazenamento e conformidade regulamentar.
<<<<<<< HEAD Baixar SDS → ======= Baixar SDS → >>>>>>> release248-p3Dados de qualidade específicos do lote. Introduza o número de lote para obter o COA exato.
Consultar COA →Resumo de referência rápida das especificações e aplicações do produto.
Ver ficha técnica →Atributos de qualidade completos e critérios de aceitação para este grau.
Ver folha de especificações →| Solubilidade | DMSO : 100 mg/mL (97.07 mM; ultrasonic and warming and heat to 60°C) |
|---|
