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

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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
Purity & Documentation
References
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M190S Related Classifications

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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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