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> Nexturastat A [1403783-31-2]

Nexturastat A [1403783-31-2]

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Katalog-Nummer HY-16699-10mg

Size : 10mg

Marke : MedChemExpress

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Nexturastat A is a potent, selective HDAC6 inhibitor. Nexturastat A has inhibitory for HDAC6 with an IC50 of 5 nM. Nexturastat A can be used for the research of multiple myeloma (MM).

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Nexturastat A Chemische Struktur

Nexturastat A Chemische Struktur

CAS. Nr. : 1403783-31-2

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Nexturastat A Related Antibodies

  • •Cell Death Dis. 2022 Aug 17;13(8):717.  [Abstract]
  • •Patent. US20180263995A1.

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Nexturastat A is a potent, selective HDAC6 inhibitor. Nexturastat A has inhibitory for HDAC6 with an IC50 of 5 nM. Nexturastat A can be used for the research of multiple myeloma (MM).

HDAC6

5.02 nM (IC50)

HDAC8

0.954 μM (IC50)

HDAC1

3.02 μM (IC50)

HDAC7

4.46 μM (IC50)

HDAC11

5.14 μM (IC50)

HDAC3

6.68 μM (IC50)

HDAC9

6.72 μM (IC50)

HDAC2

6.92 μM (IC50)

HDAC10

7.57 μM (IC50)

HDAC4

9.39 μM (IC50)

HDAC5

11.7 μM (IC50)

In Vitro

Nexturastat A (5 g) has inhibitory for HDAC6 with IC50 values of 0.005 μM.
Nexturastat A (0-10 μM; 24 h) has substrate selectivity for HDAC62.
Nexturastat A has antiproliferative activity against B16 murine melanoma cells with IC50 values of 14.3 μM.
Nexturastat A (NexA) (0-40 µM; 48 h) suppresses viability and induced G1 phase arrest of human MM cells.
Nexturastat A (0, 30, 40 μM; 48 h) promotes apoptosis of MM cells via transcriptional activation of the p21 promoter.

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

Nexturastat A Related Antibodies

Western Blot Analysis

Cell Line: B16 murine melanoma cells
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Increased the level of acetyl α-tubulin levels in a dose-dependent.

Cell Viability Assay

Cell Line: RPMI-8226 and U266 cells
Concentration: 0-40 µM
Incubation Time: 48 h
Result: Impaired multiple myeloma (MM) cells viability in a dose- and time-dependent manner.

Apoptosis Analysis

Cell Line: RPMI-8226 and U266 cells
Concentration: 0, 30, 40 μM
Incubation Time: 48 h
Result: Induced cell apoptosis in human MM cells.

RT-PCR

Cell Line: RPMI-8226 and U266 cells
Concentration: 30 µM
Incubation Time: 48 h
Result: Increased the levels of p21 mRNA in RPMI-8226 and U266 cells.
In Vivo

Nexturastat A (NexA) (every two days, 20 days) inhibits tumor growth in murine xenograft models of MM.

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

341.40

Solid

C19H23N3O3

1403783-31-2

O=C(NO)C1=CC=C(CN(CCCC)C(NC2=CC=CC=C2)=O)C=C1

Room temperature in continental US; may vary elsewhere.
In Vitro: 

DMSO : ≥ 56 mg/mL (164.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9291 mL 14.6456 mL 29.2912 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL
10 mM 0.2929 mL 1.4646 mL 2.9291 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

*All of the co-solvents are available by MCE.

  • [1]. Bergman JA, et al. Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J Med Chem. 2012 Nov 26;55(22):9891-9.  [Content Brief]

    [2]. Xiaoyang Sun, et al. The selective HDAC6 inhibitor Nexturastat A induces apoptosis, overcomes drug resistance and inhibits tumor growth in multiple myeloma. Biosci Rep. 2019 Mar 22;39(3):BSR20181916.  [Content Brief]

  • [1]. Bergman JA, et al. Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J Med Chem. 2012 Nov 26;55(22):9891-9.

    [2]. Xiaoyang Sun, et al. The selective HDAC6 inhibitor Nexturastat A induces apoptosis, overcomes drug resistance and inhibits tumor growth in multiple myeloma. Biosci Rep. 2019 Mar 22;39(3):BSR20181916.

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  • Cell Cycle/DNA Damage Epigenetics
  • HDAC
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.

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