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Cat. No.: HY-134085

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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
화학식: C₁₆H₁₄ClN₃OS
분자량:331.82

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

NSD-IN-1 Chemical Structure

CAS No.: 2351225-68-6

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

NSD1

All Histone Methyltransferase Isoforms :

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.

RT-PCR^[1]

Cell Line:

Nup98-NSD1 cells
Concentration:

1, 2 μM
Incubation Time:

4 days
Result:

Downregulated Meis1, Hoxa5 and Hoxa9 expression.

In Vivo

NSD-IN-1 (compound 159) (25 mg/kg; intraperitoneal injection; once daily; 20 days) significantly inhibited tumor growth in the Nup98-NSD1 subcutaneous leukemia model, reduced Hoxa7 expression and H3K36me2 levels in tumors, and was well tolerated[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nup98‑NSD1 Subcutaneous Xenograft Model^[1]
Dosage:

25 mg/kg
Administration:

i.p.; q.d.; 20 days
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.

Related Protocols :

Chemical Information

CAS No. 2351225-68-6
분자량 331.82
화학식 C₁₆H₁₄ClN₃OS
SMILES

ClC=1C=CC=CC1CC2N(C=3C=C(O)C=4N=C(SC4C3)N)C2
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Cierpicki T, et al. Nsd family inhibitors and methods of treatment therewith. WO2019113469A1. WIPO. 2019‑06‑13.

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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NSD-IN-1

All Histone Methyltransferase Isoforms