[CAS NO. 880107-52-8] Psalmotoxin 1
PRODUCTS SPECIFICATIONS [880107-52-8]
DESCRIPTION [880107-52-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 4689.41 |
| Molecular Formula | C200H312N62O57S6 |
| SMILES | - |
1 Publications Citing Use of MCE
Summary
Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a) . Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC 50 : 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 can induce cell apoptosis , also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease [1] [3] [4] [6] .
IC50 & Target
IC50: 0.9 nM (ASIC1a), 50 nM (ASIC1b, ASIC2a, and ASIC3) [6] .
In Vitro
Psalmotoxin 1 (20 nM, 125 s) inhibits ASIC1a currents by drastically shifting the steady-state desensitization curve to lower H
+
concentrations
[1]
.
Psalmotoxin 1 (30 nM) competes with Ca
2+
in binding to ASIC1a channels
[1]
.
Psalmotoxin 1 (100 or 200 ng, 24-72 h) significantly weakens the migration, proliferation and invasion of MCF-7 and MDA-MB-231 cells
[4]
.
Psalmotoxin 1 (100 ng/mL, 24 h) significantly inhibits acid-induced increases in intracellular calcium and LDH release, induces cell apoptosis and cell cycle arrest in nucleus pulposus cells (NPCs)
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [4]
| Cell Line: | MCF-7 and MDA-MB-231 cells |
| Concentration: | 100 or 200 ng |
| Incubation Time: | 24, 48, 72 h |
| Result: | Inhibited the cell migration, proliferation and invasion of breast cancer cells. |
Western Blot Analysis [5]
| Cell Line: | Nucleus pulposus cells (NPCs) |
| Concentration: | 100 ng/mL |
| Incubation Time: | 24 h |
| Result: | Decreased Bax and cleaved caspase-3 expression, and increased Bcl-2 expression. |
In Vivo
Psalmotoxin 1 (i.c.v., 1 ng/kg, a single dose) is neuroprotective in a conscious model of stroke via direct inhibition of ASIC1a
[2]
.
Psalmotoxin 1 (tail vein injection, 10 ng/kg, daily for 7 days) inhibits tumor growth in breast cancer mice model
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male spontaneously hypertensive rats (SHR) [2] |
| Dosage: | 1 ng/kg, a single dose. |
| Administration: | Intracerebroventricular (i.c.v.) injection |
| Result: |
Reduced cortical and striatal infarct volumes measured 72 h post-stroke.
Reduced the severity of motor deficit at 1 and 3 days after stroke compared to control rats. Displayed an anti-apoptotic effect in the occluded hemisphere (reduced stroke-induced caspase-3 positive cells). |
| Animal Model: | Female nude BALB/C mice (orthotopic implantation, MCF-7 and MDA-MB-231 cells) [3] |
| Dosage: | 10 ng/kg, daily for 7 days. |
| Administration: | Tail vein injection |
| Result: | Inhibited breast tumor growth. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O
Peptide Solubility and Storage Guidelines:
1. Calculate the length of the peptide.
2. Calculate the overall charge of the entire peptide according to the following table:
| Contents | Assign value | |
| Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 |
| Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH 2 | +1 |
| Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution:
| Overall charge of peptide | Details |
| Negative (<0) |
1. Try to dissolve the peptide in water first.
2. If water fails, add NH 4 OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. |
| Positive (>0) |
1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. |
| Zero (=0) |
1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
References
- [1] Chen X, et al. The tarantula toxin psalmotoxin 1 inhibits acid-sensing ion channel (ASIC) 1a by increasing its apparent H affinity. J Gen Physiol. 2005 Jul;126(1):71-9.
- [2] Claudia A McCarthy, et al. PcTx1 affords neuroprotection in a conscious model of stroke in hypertensive rats via selective inhibition of ASIC1a. Neuropharmacology. 2015 Dec;99:650-7.
- [3] Niko Joeres, et al. Functional and pharmacological characterization of two different ASIC1a/2a heteromers reveals their sensitivity to the spider toxin PcTx1. Sci Rep. 2016 Jun 9;6:27647. doi: 10.1038/srep27647.
- [4] Chao Yang, et al. Overexpression of acid-sensing ion channel 1a (ASIC1a) promotes breast cancer cell proliferation, migration and invasion. Transl Cancer Res. 2020 Dec;9(12):7519-7530.
- [5] Feng Cai, et al. Acid-sensing ion channel 1a regulates the survival of nucleus pulposus cells in the acidic environment of degenerated intervertebral discs. Iran J Basic Med Sci. 2016 Aug;19(8):812-820.
- [6] P Escoubas, et al. Isolation of a tarantula toxin specific for a class of proton-gated Na+ channels. J Biol Chem. 2000 Aug 18;275(33):25116-21.
