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Chemical Structure| 1403783-31-2 Chemical Structure| 1403783-31-2

Structure of Nexturastat A
CAS No.: 1403783-31-2

Chemical Structure| 1403783-31-2

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Nexturastat A is a selective inhibitor of HDAC6 with IC50 of 5 nM.

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Product Details of Nexturastat A

CAS No. :1403783-31-2
Formula : C19H23N3O3
M.W : 341.40
SMILES Code : O=C(NO)C1=CC=C(CN(CCCC)C(NC2=CC=CC=C2)=O)C=C1
MDL No. :MFCD28099804
InChI Key :JZWXMCPARMXZQV-UHFFFAOYSA-N
Pubchem ID :71462653

Safety of Nexturastat A

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Nexturastat A

epigenetics

Isoform Comparison

Biological Activity

Target
  • HDAC6

    HDAC6, IC50:5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
WM164 human melanoma cells 5 µM 24 hours HDAC6 knockdown downregulated CD47 expression and prevented IFNγ-driven CD47 upregulation. J Exp Clin Cancer Res. 2024 Feb 27;43(1):60.
B16 melanoma cells 5 µM 24 hours Nexturastat A repressed IFNγ-driven Cd47 upregulation. J Exp Clin Cancer Res. 2024 Feb 27;43(1):60.
SM1 melanoma cells 5 µM 24 hours Nexturastat A repressed IFNγ-driven Cd47 upregulation. J Exp Clin Cancer Res. 2024 Feb 27;43(1):60.
THP-1-derived macrophages 5 µM 24 hours Nexturastat A significantly upregulated M1-associated markers NOS2, CD86, and IL1B and downregulated M2-associated markers MRC1 and CD209. J Exp Clin Cancer Res. 2024 Feb 27;43(1):60.
A31A7 macrophages 5 µM 24 hours Nexturastat A significantly upregulated surface expression of M1-associated markers Cd80 and H2 and downregulated surface expression of M2-associated marker Cd206. J Exp Clin Cancer Res. 2024 Feb 27;43(1):60.
Bone marrow-derived macrophages (BMDMs) 5 µM 24 hours Nexturastat A significantly upregulated M1-associated markers Nos2 and Cd80 and downregulated M2-associated markers Arg1 and Mrc1 at the transcriptional level. J Exp Clin Cancer Res. 2024 Feb 27;43(1):60.
Mouse peritoneal elicited macrophage (PEM) 5 µM 24 hours To evaluate the effect of Nexturastat A on macrophage polarization, results showed that NextA reduced the expression of M2 marker CD206 and increased the M1 phenotype. Sci Rep. 2019 Apr 16;9(1):6136.
SM1 melanoma cells 2.5 and 5 µM 24 hours To evaluate the effect of Nexturastat A on PD-L1 expression, results showed that NextA neutralized the anti-PD1 antibody-mediated upregulation of IFNγ on PD-L1 production. Sci Rep. 2019 Apr 16;9(1):6136.
RPMI-8226/BTZ100 cells 20 µM 48 hours To evaluate the effect of NexA on BTZ-resistant cell viability, results showed that NexA remarkably suppressed the viability of RPMI-8226/BTZ100 cells. Biosci Rep. 2019 Mar 22;39(3):BSR20181916.
U266 cells 30 µM 48 hours To evaluate the effect of NexA on cell viability, results showed that NexA dose-dependently impaired the viability of the two cell lines. Biosci Rep. 2019 Mar 22;39(3):BSR20181916.
RPMI-8226 cells 30 µM 48 hours To evaluate the effect of NexA on cell viability, results showed that NexA dose-dependently impaired the viability of the two cell lines. Biosci Rep. 2019 Mar 22;39(3):BSR20181916.
OVSAHO 12500 nM 48 hours preincubation followed by 72 hours incubation Nexturastat A increased cisplatin potency in OVSAHO cells, with IC50 values in the micromolar range. Int J Mol Sci. 2019 Jun 22;20(12):3052.
Kuramochi 5000 nM 48 hours preincubation followed by 72 hours incubation Nexturastat A increased cisplatin potency in Kuramochi cells, with IC50 values in the micromolar range. Int J Mol Sci. 2019 Jun 22;20(12):3052.
HEY 5000 nM 48 hours preincubation followed by 72 hours incubation Nexturastat A increased cisplatin potency in HEY cells, with IC50 values in the micromolar range. Int J Mol Sci. 2019 Jun 22;20(12):3052.
CaOV3 7500 nM 48 hours preincubation followed by 72 hours incubation Nexturastat A increased cisplatin potency in CaOV3 cells, with IC50 values in the micromolar range. Int J Mol Sci. 2019 Jun 22;20(12):3052.
A2780 7500 nM 48 hours preincubation followed by 72 hours incubation Nexturastat A increased cisplatin potency in A2780 cells, with IC50 values in the micromolar range. Int J Mol Sci. 2019 Jun 22;20(12):3052.
HeLa cells 2.5 µM 72 hours Nexturastat A increased BE3-mediated gene editing efficiency in HeLa cells, with an average improvement of 4.90-fold. Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986.
HT1080 cells 2.5 µM 72 hours Nexturastat A significantly improved BE3-mediated gene editing efficiency in HT1080 cells, with an average improvement of 7.96-fold. Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986.
HEK-293 cells 2.5 µM 72 hours Nexturastat A increased BE3-mediated gene editing efficiency, with an average improvement of 3.46-fold. Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986.
BT474 0.37 nM to 100 µM 72 hours Evaluate the cytotoxic effect of Nexturastat A on HER2+ breast cancer cells, showing that NextA was effective in both SKBR3 and BT474 cell lines. Cancers (Basel). 2024 Nov 6;16(22):3752.
SKBR3 0.37 nM to 100 µM 72 hours Evaluate the cytotoxic effect of Nexturastat A on HER2+ breast cancer cells, showing that NextA was effective in both SKBR3 and BT474 cell lines, with the lowest IC50 in SKBR3 clones. Cancers (Basel). 2024 Nov 6;16(22):3752.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Oct4-eGFP mice Added to embryo culture medium 0.5 µM 24 hours Nexturastat A significantly improved BE3-mediated gene editing efficiency, with a 1.57-fold improvement in embryos. Nucleic Acids Res. 2021 Sep 7;49(15):8974-8986.
C57BL/6 mice SM1 melanoma model Subcutaneous injection 15 mg/kg 5 days a week for 25 days To evaluate the effect of Nexturastat A in combination with anti-PD-1 antibody, results showed that the combination significantly reduced tumor growth and enhanced immune cell infiltration. Sci Rep. 2019 Apr 16;9(1):6136.
C57BL/6 mice SM1 melanoma model Intraperitoneally 20 mg/kg Every other day until the end of the study The combination of Nexturastat A and anti-CD47 significantly decreased tumor growth, increased immune cell infiltration in the tumor microenvironment (TME), and modulated macrophage and natural killer (NK) cell populations. J Exp Clin Cancer Res. 2024 Feb 27;43(1):60.
Mice Listeria infection model Intraperitoneal injection 3 mg/kg 5 days post infection Reduced Listeria burdens, increased Th1 cell numbers Cell Death Differ. 2022 Nov;29(11):2303-2315

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.93mL

0.59mL

0.29mL

14.65mL

2.93mL

1.46mL

29.29mL

5.86mL

2.93mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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