| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
MLCK (myosin light chain kinase). MLCK is a calcium/calmodulin-dependent kinase that phosphorylates myosin regulatory light chain, regulating smooth muscle contraction and non-muscle cell motility. The peptide is a selective competitive inhibitor that binds to the catalytic site of MLCK.
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|---|---|
| ln Vitro |
Peptide 18, the MLCK inhibitor, has a coupling effect on the peptide substrate consumption of MLCK; it has no discernible inhibitory activity on the closely related CaMPKII; it has no effect on PKA; and it does not interfere with the intermittent activation of CaM [1].
MLCK inhibitor peptide 18 inhibits MLCK with an IC₅0 of 50 nM. It displays 4000-fold selectivity over CaM kinase II and does not inhibit PKA. The peptide selectively inhibits MLCK's utilization of peptide substrates without interfering with CaM-dependent kinase activation. It is a potent and specific tool for studying MLCK function. |
| ln Vivo |
In vivo, MLCK inhibitor peptide 18 would be expected to inhibit smooth muscle contraction and cell motility. The peptide is typically used in cell-based or ex vivo studies rather than systemic in vivo administration due to its peptidic nature. It is useful for studying the role of MLCK in vascular tone, airway hyperresponsiveness, and cancer cell invasion.
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| Enzyme Assay |
MLCK enzymatic activity is measured using a kinase assay with myosin light chain or a synthetic peptide substrate. MLCK is incubated with ATP (typically 32P-ATP or a fluorescent ATP analog) and substrate in the presence of serial dilutions of test peptide. Phosphorylation of the substrate is quantified by scintillation counting or fluorescence polarization. IC₅0 values are calculated from dose-response curves.
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| Cell Assay |
Cells (e.g., smooth muscle cells, endothelial cells, or cancer cells) are treated with MLCK inhibitor peptide 18 (often using cell-penetrating peptide delivery methods such as TAT conjugation or lipofection). Myosin light chain phosphorylation is assessed by Western blotting using phospho-specific antibodies. Cell migration and contraction are evaluated using appropriate functional assays.
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| Animal Protocol |
Due to its peptidic nature, MLCK inhibitor peptide 18 is typically used in ex vivo tissue preparations (e.g., isolated blood vessels, tracheal rings) or in cell culture rather than systemic animal models. In these systems, the peptide is applied directly to the tissue or cells, and effects on contraction or motility are measured.
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| ADME/Pharmacokinetics |
MLCK inhibitor peptide 18 has a molecular weight of 1324.62 g/mol and formula C₆0H10₅N23O11. As a peptide, it has limited oral bioavailability and is typically used in vitro or administered locally. The peptide is soluble in aqueous buffers and DMSO. Its peptidic nature makes it susceptible to proteolytic degradation.
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| Toxicity/Toxicokinetics |
Toxicology data for MLCK inhibitor peptide 18 are not publicly available. As a peptide, it is expected to have low systemic toxicity due to its limited bioavailability and rapid degradation. Standard in vitro cytotoxicity assays would be performed to assess safety in cell-based studies.
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| References | |
| Additional Infomation |
MLCK inhibitor peptide 18 is a research peptide for studying myosin light chain kinase function. It is not clinically approved. The peptide's high selectivity for MLCK over CaM kinase II (>4000-fold) and lack of PKA inhibition make it a valuable tool for dissecting MLCK-specific signaling pathways. It is widely used in studies of smooth muscle physiology, cell migration, and cancer invasion.
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| Molecular Formula |
C60H105N23O11
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|---|---|
| Molecular Weight |
1324.6232
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| Exact Mass |
1323.84
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| CAS # |
224579-74-2
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| PubChem CID |
10102940
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| Appearance |
White to off-white solid powder
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| LogP |
5.781
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
49
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| Heavy Atom Count |
94
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| Complexity |
2380
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C1=CC(=CC=C1C[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)N)O
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| InChi Key |
JPOKAKNGULMYHZ-UILVTTEASA-N
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| InChi Code |
InChI=1S/C60H105N23O11/c61-27-5-1-13-41(49(66)86)76-51(88)45(17-10-32-74-59(69)70)79-53(90)46(18-11-33-75-60(71)72)81-57(94)48(35-37-21-25-39(85)26-22-37)83-55(92)44(16-4-8-30-64)80-56(93)47(34-36-19-23-38(84)24-20-36)82-54(91)43(15-3-7-29-63)78-52(89)42(14-2-6-28-62)77-50(87)40(65)12-9-31-73-58(67)68/h19-26,40-48,84-85H,1-18,27-35,61-65H2,(H2,66,86)(H,76,88)(H,77,87)(H,78,89)(H,79,90)(H,80,93)(H,81,94)(H,82,91)(H,83,92)(H4,67,68,73)(H4,69,70,74)(H4,71,72,75)/t40-,41-,42-,43-,44-,45-,46-,47-,48-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~75.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (75.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7549 mL | 3.7747 mL | 7.5493 mL | |
| 5 mM | 0.1510 mL | 0.7549 mL | 1.5099 mL | |
| 10 mM | 0.0755 mL | 0.3775 mL | 0.7549 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.
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.
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