NSD-IN-1
NSD-IN-1 is a benzothiazole-based covalent inhibitor of NSD1. NSD-IN-1 covalently binds the NSD1 SET domain and reduces H3K36me2 levels, thereby inhibiting the proliferation of Nup98-NSD1 leukemia cells, downregulating the expression of Meis1, Hoxa5, and Hoxa9, and inducing cell differentiation. NSD-IN-1 can be used for research on Nup98-NSD1 acute myeloid leukemia.
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- CAS No.: 2351225-68-6
- Formule: C16H14ClN3OS
- Masse moléculaire:331.82
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
NSD1 |
In Vitro
NSD-IN-1 (compound 159) (5 μM) stabilizes NSD1 in HeLa cells in the CETSA assay[1].
NSD-IN-1 (1-2 μM; 4 days) downregulates the expression of Meis1, Hoxa5, and Hoxa9 in Nup98-NSD1 cells[1].
NSD-IN-1 (1.5 μM) induces differentiation of Nup98-NSD1 cells[1].
NSD-IN-1 (3-10 days) inhibited Nup98-NSD1 cell proliferation in a time-dependent manner (GI50 = 0.5-1.3 μM), without affecting the proliferation of control HM-2 cells[1].
NSD-IN-1 was confirmed by mass spectrometry to covalently bind to NSD1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Nup98-NSD1 cells
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Concentration:1, 2 μM
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Incubation Time:4 days
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Result:Downregulated Meis1, Hoxa5 and Hoxa9 expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nup98‑NSD1 Subcutaneous Xenograft Model[1]
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Dosage:25 mg/kg
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Administration:i.p.; q.d.; 20 days
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Result:Significantly inhibited Tumor growth compared to the vehicle group.
Significantly reduced Hoxa7 expression in tumors.
Significant decrease in H3K36me2 levels in tumor tissues.
No significant weight loss was observed in the treatment group.
Chemical Information
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CAS No. 2351225-68-6
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Masse moléculaire 331.82
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Formule C16H14ClN3OS
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SMILES
ClC=1C=CC=CC1CC2N(C=3C=C(O)C=4N=C(SC4C3)N)C2
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NSD-IN-1 Related Classifications
HY-134085 Related Classifications
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