1. PI3K/Akt/mTOR
    Stem Cell/Wnt
  2. GSK-3

BIO-acetoxime (Synonyms: BIA)

Cat. No.: HY-15356 Purity: >98.0%
Handling Instructions

BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.

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

BIO-acetoxime Chemical Structure

BIO-acetoxime Chemical Structure

CAS No. : 667463-85-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 290 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 740 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.

IC50 & Target[1]

GSK-3α

10 nM (IC50)

GSK-3β

10 nM (IC50)

CDK5/p35

2.4 μM (IC50)

CDK2/cyclin A

4.3 μM (IC50)

CDK1/cyclin B

63 μM (IC50)

In Vitro

BIO-acetoxime (BIA; Compound 13) is a potent and selective GSK-3α/β inhibitor, with IC50s of both 10 nM. BIO-acetoxime (BIA) shows weak effect on CDK5/p35 (IC50, 2.4 μM), CDK2/cyclin A (IC50, 4.3 μM), and CDK1/cyclin B (IC50, 63 μM)[1]. BIO-acetoxime (BIA) (5 μM and 10 μM) increases the viability of HSV-1-infected cells but shows little effect on morphology and viability of mockin-fected cells. Moreover, BIO-acetoxime (BIA) (0.625, 1.25, 2.5, 5, and 10 μM) significantly reduces the release of HSV-1 particles in OC3 cells, with an EC50 of 0.68 ± 0.28 μM. BIO-acetoxime (BIA) inhibits the expression of HSV-1 genes, and may not affect the nuclear targeting of HSV-1 capsids. In addition, delayed addition of BIO-acetoxime (BIA) also inhibits HSV-1 infection[2].

In Vivo

BIO-acetoxime (BIA) shows anticonvulsant effects in the focal pilocarpine rat model at 0.5 mg/kg, and in 6-Hz fully kindled FVB/N mice at 0.5, 2.5, and 5 mg/kg via i.p. administration[3].

Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (52.31 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5112 mL 12.5562 mL 25.1124 mL
5 mM 0.5022 mL 2.5112 mL 5.0225 mL
10 mM 0.2511 mL 1.2556 mL 2.5112 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

  • 2.

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

    Solubility: 2.08 mg/mL (5.22 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

References
Cell Assay
[2]

OC3 cells are seeded in 3.5- and 6-cm diameter dishes for western blot analysis and RNA isolation, respectively. Cells are mock treated or exposed to HSV-1 at a multiplicity of infection (m.o.i.) of 5 unless otherwise specified. The glycogen synthase kinase-3 (GSK-3) inhibitor BIO-acetoxime (BIA), is first dissolved in DMSO to make a stock solution. Medium containing DMSO serves as a solvent control. Cells are pretreated with medium only, medium containing 0.1 % DMSO or BIO-acetoxime (BIA) for 45 min prior to mock or HSV-1 infection. BIO-acetoxime (BIA) is also present throughout the infection period. To examine the direct effect on viruses, HSV-1 is treated directly with medium containing 5 μM BIO-acetoxime (BIA) for 1 h at room temperature. Cell morphology is observed with an inverted microscope[2].

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

Animal Administration
[3]

Mice[3]
Male FVB/N mice are used to test the anticonvulsant effects of BIO-acetoxime in fully kindled mice. To achieve the fully kindled state, mice are stimulated at a fixed subconvulsive threshold current twice daily, except the weekends, with a 4 h minimum interval between stimulations. Kindled mice are then stimulated for only 2 days a week, twice daily to maintain the fully kindled state. Meanwhile nonkindled mice are kept at the original stimulation scheme for maximum 1-2 more weeks. The anticonvulsant effect of BIO-acetoxime (BIA) is investigated in the “epileptic” fully kindled mice by stimulating these animals on Monday morning. On Monday afternoon, the animals are intraperitoneally (i.p.) injected with vehicle, 30 min prior to stimulation. On Tuesday morning, mice are again stimulated. On Tuesday afternoon, mice are injected i.p. with BIO-acetoxime (BIA) and are stimulated 30 min later. Seizure severity is assessed using Racine’s scale. The pretreatment scores are compared with the post-treatment scores, obtained after the treatment on Tuesday. To confirm any observed effects, the experiment is repeated, respecting 1 week of washout. During this washout week, all mice are stimulated for 2 days (twice daily) to maintain the kindled state. Compound testing during a longer period has not been validated so far. This means that only one dose of BIO-acetoxime can be tested in one batch of kindled mice[3].

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

References
Molecular Weight

398.21

Formula

C₁₈H₁₂BrN₃O₃

CAS No.

667463-85-6

SMILES

O=C1NC2=C(C=CC(Br)=C2)/C1=C3NC4=C(C=CC=C4)C/3=N\OC(C)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BIO-acetoxime
Cat. No.:
HY-15356
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BIO-acetoxime

Cat. No.: HY-15356