MS9117
MS9117 is a PROTAC molecule that targets and degrades LSD1/BHC110 by recruiting CRBN. MS9117 effectively increases the level of histone H3 lysine 4 monomethylation. MS9117 significantly inhibits the proliferation and colony formation of cancer cells, promotes their myeloid differentiation, and enhances the sensitivity of non-acute promyelocytic leukemia-type AML cells to all-trans retinoic acid (ATRA).
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- CAS No.: 3098670-37-9
- Formule: C46H48F2N10O10
- Masse moléculaire:938.93
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MS9117 (5-1000 nM; 2-72 h) induces time- and concentration-dependent degradation of LSD1 in THP-1 AML cells, with complete degradation at 50 nM after 24 h, and increases cellular H3K4me1 levels[1].
MS9117 (50-100 nM; 24 h) degrades LSD1 and increases H3K4me1 levels in NB4, MOLM-13, and Kasumi-1 AML cells[1].
MS9117 (72 h) inhibits THP-1 AML cell proliferation with an EC50 of 49 nM after 72 h of treatment[1].
MS9117 (10-1000 nM; 24 h) induces proteasome-, LSD1-, and CRBN-dependent degradation of LSD1 in THP-1 AML cells, acts selectively on LSD1 without altering IKZF1 or GSPT1 levels, and does not affect LSD1 mRNA expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 acute myeloid leukemia (AML) cells
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Concentration:5-1000 nM (24 h); 50 nM (time-course)
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Incubation Time:2-72 h (50 nM); 24 h (5-1000 nM)
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Result:Induced LSD1 degradation in a time- and concentration-dependent manner.
First induced detectable LSD1 degradation at 12 h, with near-complete degradation by 24 h; this effect persisted through 72 h, with over 80% of LSD1 remaining degraded.
Induced over 50% LSD1 degradation at 40 nM, while 50 nM caused complete degradation.
Exhibited a hook effect at concentrations >500 nM.
Increased the level of H3K4me1 in THP-1 cells.
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Cell Line:NB4, MOLM-13, and Kasumi-1 AML cells
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Concentration:50-100 nM
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Incubation Time:24 h
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Result:Degraded LSD1 in all three cell lines at both tested concentrations.
Increased the level of H3K4me1 in all three cell lines at both tested concentrations.
Chemical Information
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CAS No. 3098670-37-9
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Masse moléculaire 938.93
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Formule C46H48F2N10O10
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SMILES
N#CC1=CC=C(C(N=C(N2CCC(CC2)N)N3CC(NCCOCCOCCNC(CNC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)=O)=C(C7=CC(F)=C(OC)C=C7)C3=O)C=C1F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Hosseini A, et al. Discovery of an LSD1 PROTAC degrader. Proceedings of the National Academy of Sciences of the United States of America. 2025 May 20;122(20):e2425812122. [Content Brief]
[2]. Khan SA, et al. Therapeutic advances in acute myeloid leukemia: from LSD1 blockade to PROTAC-based strategies. Annals of medicine and surgery (2012). 2026 Feb;88(2):2166-2167. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS9117 Related Classifications
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