NC-III-49-1

Cat. No.: HY-150683: FAQs
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NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with K_d values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc.

For research use only. We do not sell to patients.

NC-III-49-1 Chemical Structure

CAS No. : 3031654-46-0

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Description

IC₅₀ & Target^[1]

BRD4-1

0.095 nM (Kd)

BRD4-2

0.032 nM (Kd)

BRD4-T

0.29 nM (Kd)

BRDT-1

0.089 nM (Kd)

BRDT-2

5.5 nM (Kd)

BRDT-T

0.058 nM (Kd)

In Vitro

NC-III-49-1 (0-10 µM; 72 h) shows antiproliferative activity with an IC₅₀ value of 0.69 nM in MM1.S cells^[1].
NC-III-49-1 (0-10 µM; 6 h) decreases the expression of c-Myc in a dose dependent manner^[1].
. NC-III-49-1 shows inhibition by interact with both KAc sites^[1].

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

Cell Viability Assay^[1]

Cell Line:	MM1.S cells
Concentration:	0-10 µM
Incubation Time:	72 h
Result:	Showed subnanomolar growth inhibition with an IC₅₀ value of 0.69 nM in multiple myeloma MM1.S cells.

Western Blot Analysis^[1]

Cell Line:	MM1.S cells
Concentration:	0-10 µM
Incubation Time:	6 h
Result:	Decreased the expression of c-Myc in a dose dependent manner.

In Vivo

NC-III-49-1 shows metabolic stability in human and mouse liver microsomes with an T_1/2 values of <2.3, <2.3 min, respectively^[1].

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

Molecular Weight

875.02

Formula

C₄₄H₅₀N₄O₁₁S₂

CAS No.

3031654-46-0

SMILES

CCS(=O)(NC1=CC=C(C(C(C2=C3C=CC=C2)=CN(C3=O)C)=C1)OCCOCCOCCOCCOC4=CC=C(C=C4C(C5=C6C=CC=C5)=CN(C6=O)C)NS(CC)(=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Guan X, et al. Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity. J Med Chem. 2022 Jul 22. [Content Brief]

NC-III-49-1 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NC-III-49-13031654-46-0Epigenetic Reader Domainantiproliferativec-MycMM1.S cellsmetabolic stabilityInhibitorinhibitorinhibit

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