2. Apoptosis
  3. Caspase
  4. M190S

M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability.

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

M190S Chemical Structure

M190S Chemical Structure

CAS No. : 2578300-07-7

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Based on 1 publication(s) in Google Scholar

M190S Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

  • References

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Description

M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability[1].

IC50 & Target

caspase-3

23.4 nM (EC50)

Caspase 3

23.4 nM (EC50)

In Vitro

M109S (0.1-10000 nM, 24-48 h) inhibits apoptosis induced by Bax as well as Bak[1].
M109S (0-10μM, 4 h) suppresses Staurosporine (HY-15141 STS)-induced apoptosis in MEFs [1].
M109S (0-10μM, 24 h) inhibits Etoposide (HY-13629)-induced apoptosis in Neuro2a cells[1].
M109S (500 nM, 24 h) inhibits Obatoclax (HY-10969A)-induced apoptosis in ARPE19 cells[1].
M109S (500 nM, 48 h) suppresses the conformation change (N-terminal exposure) and mitochondrial translocation of Bax[1].
M109S (1.0 μM, 4h) decreases mitochondrial oxygen consumption and reactive oxygen species, whereas M109S (0.1-1 nM, 4 h) increases glycolysis[1].

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

M190S Related Antibodies

Apoptosis Analysis[1]

Cell Line: MEF(Wt, Bax only, Bak only)
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 10000 nM
Incubation Time: 24 h((WT and Bax-only), 48 h (Bak-only)
Result: Showed a dose-dependent suppression of caspase activation in all three types of MEFs.

Apoptosis Analysis[1]

Cell Line: MEF
Concentration: 0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 10000 nM
Incubation Time: 4 h
Result: Suppressed STS-induced caspase activation in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: Neuro2a
Concentration: 0 nM, 40 nM, 200 nM, 10000 nM
Incubation Time: 24 h
Result: Suppressed Etoposide-induced caspase activation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: ARPE19
Concentration: 500 nM
Incubation Time: 24 h
Result: Significantly inhibited Obatoclax-induced apoptosis in ARPE19 cells comparing to control.

Western Blot Analysis[1]

Cell Line: iBax cells
Concentration: 500 nM
Incubation Time: 48 h
Result: Significantly suppressed the amount of immunoprecipitated Bax without a significant change in the total Bax expression.

Immunofluorescence[1]

Cell Line: iBax cells
Concentration: 500 nM
Incubation Time: 48 h
Result: Showed the frequency of the punctuated staining was significantly reduced.
In Vivo

M109S (10mg/kg p.o., three time in 48 h) protects the retina from the bright-light-induced photoreceptor death[1].
M109S (1 mg/kg, i.p., i.v., 5 mg/kg, o.p. 10 mg/kg 1 time) is an orally bioactive cell death inhibitor penetrating blood-brain/retina-barrier[1].

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

Animal Model: Abca4-/-Rdh8-/- mice
Dosage: 10 mg/kg
Administration: Oral Gavage (p.o.)
Result: Comparing to mice with M109S, the number of AF spots was similar to that detected in the dark-adapted mice.
Animal Model: Mice and Rat
Dosage: Intraperitoneal injection (i.p., 1 mg/kg), Intravenous injection (i.v., 5 mg/kg), or Oral gavage (p.o., 10 mg/kg)
Administration: Intraperitoneal injection (i.p.), Intravenous injection (i.v.), or Oral gavage (p.o.).
Result: Showed plasma concentration reached 1.0 mg/mL (2.6 mM) within 30 min from p.o. in mice, and it remained at 596± 134 ng/mL (1.6±0.36 mM) after 24 h, the same as in rat. Plasmic M109S was 565.3±188.3 nM in rats, and 171.0±52.0 nM in retina, 222.7±74.7 nM in brain, respectively.
Molecular Weight

375.42

Formula

C21H21N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=NC(OC(C)=C2)=C2C(N[C@@H](C)C3=CC=C(C4=NC(C5CC5)=NO4)C=C3)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (266.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6637 mL 13.3184 mL 26.6368 mL
5 mM 0.5327 mL 2.6637 mL 5.3274 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: 2.5 mg/mL (6.66 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (6.66 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6637 mL 13.3184 mL 26.6368 mL 66.5921 mL
5 mM 0.5327 mL 2.6637 mL 5.3274 mL 13.3184 mL
10 mM 0.2664 mL 1.3318 mL 2.6637 mL 6.6592 mL
15 mM 0.1776 mL 0.8879 mL 1.7758 mL 4.4395 mL
20 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3296 mL
25 mM 0.1065 mL 0.5327 mL 1.0655 mL 2.6637 mL
30 mM 0.0888 mL 0.4439 mL 0.8879 mL 2.2197 mL
40 mM 0.0666 mL 0.3330 mL 0.6659 mL 1.6648 mL
50 mM 0.0533 mL 0.2664 mL 0.5327 mL 1.3318 mL
60 mM 0.0444 mL 0.2220 mL 0.4439 mL 1.1099 mL
80 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8324 mL
100 mM 0.0266 mL 0.1332 mL 0.2664 mL 0.6659 mL
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M190S Related Classifications

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:

M190S2578300-07-7CaspaseInhibitorinhibitorinhibit

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