yingweiwo

BIP-135

Cat No.:V12730 Purity: ≥98%
BIP-135 is a highly efficient, selective, ATP-competitive GSK-3 inhibitor (antagonist) with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β respectively.
BIP-135
BIP-135 Chemical Structure CAS No.: 941575-71-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Product Description
BIP-135 is a highly efficient, selective, ATP-competitive GSK-3 inhibitor (antagonist) with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β respectively. BIP 135 is neuro-protective (neuro-protection).
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In human SMA fibroblasts, BIP-135 (20-30 μM; 72 hours) raises survival motor neuron (SMN) protein levels at the 25 μM dose. A commonly observed dose-response curve with a bell shape is caused by some toxicity at higher dosages [1]. In oxidative stress models, BIP-135 (20 μM; 48 hours) is a highly effective neuroprotective drug [1].
ln Vivo
Animals seem to tolerate BIP-135 well; they do not appear to lose weight as a result [1]. BIP-135 (i.p.; 75 mg/kg; daily; from postnatal day 0 to 21) increases median survival in the spinal muscular atrophy model of the Δ7 SMA KO mouse [1].
Cell Assay
Western Blot Analysis[1]
Cell Types: Human SMA fibroblasts
Tested Concentrations: 20 μM, 25 μM, 30 μM
Incubation Duration: 72 hrs (hours)
Experimental Results: SMN levels increased 7-fold at 25 μM.
Animal Protocol
Animal/Disease Models: Male and female SMN2+/+, SMN2Δ7+/+, Smn+/– mice [1]
Doses: 75 mg/kg
Route of Administration: intraperitoneal (ip) injection; daily; from postnatal day 0 to day 21
Experimental Results: The median survival of SMA KO animals was modestly prolonged by two days.
References

[1]. Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. ACS Chem Neurosci. 2012 Jan 18;3(1):5-11.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H13N2O3BR
Molecular Weight
421.24352
Exact Mass
420.011
CAS #
941575-71-9
PubChem CID
16741475
Appearance
Light yellow to orange solid powder
Density
1.64±0.1 g/cm3 (20 °C, 760 mmHg)
Boiling Point
643.5±55.0 °C (760 mmHg)
LogP
4.583
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
2
Heavy Atom Count
27
Complexity
693
Defined Atom Stereocenter Count
0
InChi Key
QKQJCKAXFJBYKJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H13BrN2O3/c1-24-9-14(13-8-11(22)6-7-16(13)24)18-19(21(26)23-20(18)25)15-10-27-17-5-3-2-4-12(15)17/h2-10H,1H3,(H,23,25,26)
Chemical Name
3-(1-benzofuran-3-yl)-4-(5-bromo-1-methylindol-3-yl)pyrrole-2,5-dione
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~62.5 mg/mL (~148.37 mM)
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
View More

Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
View More

Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3739 mL 11.8697 mL 23.7394 mL
5 mM 0.4748 mL 2.3739 mL 4.7479 mL
10 mM 0.2374 mL 1.1870 mL 2.3739 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Acute treatment of primary cortical neurons with BIP-135 protects from oxidative stress. Graphs showing the survival of cortical neurons upon exposure to the GSK-3 inhibitors: (A) BIP-135, (B) AR-A014418, or (C) SB-216763, in the absence (blue bar) or presence (red bar) of HCA (5 mM) after 48 h, using the MTT assay. Data are presented as percent of control ± SEM. (D) Representative micrographs showing live/dead staining of primary cortical neurons after 48 h incubation with BIP-135 (c, d), AR-A014418 (e, f), or SB-216763 (g, h) in the absence (a, c, e, g) or presence (b, d, f, h) of HCA (5 mM). Live and dead neurons were stained with calcein AM (green fluorescence) and ethidium homodimer (red fluorescence), respectively. The control contains no GSK-3 inhibitors.[1].Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. ACS Chem Neurosci. 2012 Jan 18;3(1):5-11.
  • Total intracellular glutathione levels of the primary cortical neuron cultures after 8 h incubation with BIP-135, AR-A014418, or SB-216763 in the absence (blue bar) or presence (red bar) of HCA (5 mM). The control contains no GSK-3 inhibitor.[1].Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. ACS Chem Neurosci. 2012 Jan 18;3(1):5-11.
  • Effect of BIP-135 on several phenotypes of SMA disease that are observed in transgenic mice. (A) Kaplan–Meier survival curve of SMA KO mice treated once a day with BIP-135 at 75 mg/kg or vehicle (100% DMSO) from postnatal day 0 to 21. Post hoc Logrank and Wilcoxon tests showed significant differences between the two treatment groups (p = 0.0294 and 0.0266, respectively). The mean survival for KOs treated with BIP-135 was 14.7 ± 0.4 and 12.8 ± 0.6 days for vehicle treated control [F(1,45) = 5.314, p = 0.0258)]. (B) Effects of GSK-3 inhibitor BIP-135 at 75 mg/kg or its vehicle once a day on the SMA KO body weight. KO animals treated with BIP-135 showed an improvement in body weight in comparison to vehicle treated control (B). ANOVA indicated a significant main effect for treatment [F(1,43) = 4.33, p = 0.0435)] and no significant treatment/age [F(15,540) = 1.43, p = 0.1289)] or treatment/gender/age interactions [F(30,540) = 1.12, p = 0.3016]. Improvement in body weight measures was observed after around P6. (C) Geotaxis test results for KO mice receiving BIP-135 at 75 mg/kg or its vehicle once a day. (a) Latency to complete the negative geotaxis test. There were no significant treatment effects [F(1,43) = 3.50, p = 0.0683] or treatment/age interaction [F(3,111) = 1.81, p = 0.1487] in the latency to reorient upward in the geotaxis test between the two groups. (b) Percent of KO mice that completed the geotaxis test. Chi square test (4.625) indicated significant treatment effect at P12 (p = 0.0315), where more KO animals treated with BIP-135 completed the geotaxis test in comparison to the vehicle treated controls.[1].Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. ACS Chem Neurosci. 2012 Jan 18;3(1):5-11.
Contact Us