ND-L11B TFA
ND-L11B TFA is an NSD2 degrader with a Kd value of 8.77 μM, degrading the NSD2-long and RE-IIBP isoforms in multiple myeloma cells with DC50 values of 1.48 μM and 0.8 μM, respectively. ND-L11B TFA reduces H3K36me2 levels and inhibits the proliferation of multiple myeloma cells. ND-L11B TFA serves as a starting point for the further development of NSD2-targeted compounds and is also a chemical knockdown tool for elucidating the multiple functions of NSD2 isoforms. ND-L11B TFA can be used for research on multiple myeloma.
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- 화학식: C39H52F6N10O4
- 분자량:838.89
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
NSD2 8.77 μM (Kd) |
In Vitro
ND-L11B TFA (0.63-2.50 μM for KMS11 cells; 2.0-8.0 μM for 22RV1 cells) downregulates H3K36 methylation levels in KMS11 multiple myeloma cells and 22RV1 prostate cancer cells[1].
ND-L11B TFA (12-day exposure of KMS11 cells; 8-day exposure of 293T cells) potently inhibits the proliferation of KMS11 multiple myeloma cells with an IC50 of 0.90 μM, while showing very low cytotoxicity against non-malignant human embryonic kidney 293T cells (IC50 > 100 μM)[1].
ND-L11B TFA (1.25-2.50 μM; 2 days) downregulates the expression of NSD2-regulated cancer-related genes in KMS11 multiple myeloma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KMS11 multiple myeloma cells
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Concentration:0.09, 0.13, 0.20, 0.29, 0.44, 0.66, 0.99, 1.48, 2.22, 3.33, 5.0 μM; 5 μM (time-dependent assay)
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Incubation Time:6, 12, 24, 36, 48 h (5 μM concentration)
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Result:Induced simultaneous concentration-dependent degradation of NSD2-long and RE-IIBP isoforms, with DC50 values of 1.48 μM (NSD2-long) and 0.80 μM (RE-IIBP), and a maximum degradation (D_max) of approximately 80%.
Induced time-dependent degradation of NSD2 protein over 6 to 48 hours.
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Cell Line:KMS11 multiple myeloma cells
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Concentration:1.25, 2.50 μM
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Incubation Time:2 days
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Result:Downregulated the expression of NSD2-regulated oncogenes and cancer-related genes including JAM2, MET, PAK1, RRAS2, BACE2, CA2, IGF2BP2, and CR2.
Chemical Information
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분자량 838.89
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화학식 C39H52F6N10O4
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SMILES
O=C(NCCCCCCCCCCCN)COC1=CC(C2=NC=C(N3C[C@](CC(F)F)(N)CCC3)C(CN4C=NC5=C(N)N=CN=C45)=C2)=CC=C1F.O=C(O)C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)