| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Peptide 74 is the activated form of the 72-kDa type IV collagenase, also known as MMP-2. As a synthetic peptide containing the prodomain sequence of MMP, it acts as an inhibitor of this enzyme. By inhibiting MMP-2, which is involved in the degradation of extracellular matrix components like type IV collagen, Peptide 74 can modulate cell invasion and metastasis. It shows no cytotoxic action and does not inhibit chemotaxis.
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|---|---|
| ln Vitro |
A2058 and HT 1080 tumor cell invasion is 60–80% lessened by peptide 74 (30 μM)[1]. Peptide 74 (30 μM) did not block chemotaxis, cause cytotoxicity, or change the quantity of HT1080 and A2058 human tumor cells [1].
In vitro, Peptide 74 inhibits the activated form of the 72-kDa type IV collagenase (MMP-2). At a concentration of 30 μM, it reduces the invasion of A2058 and HT1080 human tumor cells by 60-80%. Importantly, Peptide 74 shows no cytotoxic action and does not inhibit chemotaxis or affect the number of HT1080 and A2058 cells. This suggests its anti-invasive effect is specific and not due to general toxicity. |
| ln Vivo |
In vivo, Peptide 74's potential to inhibit tumor cell invasion has been demonstrated in vitro, suggesting it could have anti-metastatic activity in vivo. Its ability to inhibit MMP-2, a key enzyme in the metastatic cascade, makes it a compound of interest for cancer research. However, its in vivo efficacy and pharmacokinetic properties require further investigation. The peptide is a research tool for studying the role of MMP-2 in invasion and metastasis.
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| Enzyme Assay |
In vitro enzyme assays for Peptide 74 measure its inhibition of MMP-2 activity. The enzyme's activity can be assessed using a fluorogenic substrate that is cleaved by active MMP-2, producing a fluorescent signal. The peptide is incubated with the enzyme and substrate, and the inhibition of fluorescence is measured. The concentration required for 50% inhibition (IC₅₀) can be determined. These assays are standard for characterizing MMP inhibitors and are for research purposes only.
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| Cell Assay |
In vitro cell-based assays for Peptide 74 evaluate its anti-invasive effects. Tumor cell lines such as HT1080 (fibrosarcoma) or A2058 (melanoma) are used in invasion assays. Cells are placed in the upper chamber of a Transwell insert coated with Matrigel, which mimics the basement membrane. The lower chamber contains a chemoattractant. The number of cells that invade through the Matrigel is counted after treatment with 30 μM Peptide 74. Cytotoxicity is assessed using standard MTT or LDH assays to confirm that the anti-invasive effect is not due to cell death.
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| Animal Protocol |
In vivo animal studies for Peptide 74 would typically involve mouse models of metastasis. For example, tumor cells could be injected intravenously, and the compound would be administered to assess its ability to reduce the number of metastatic nodules in the lungs. Alternatively, orthotopic tumor models could be used. The peptide's stability and delivery would be important considerations. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Peptide 74 are not characterized in the available literature. As a peptide, it may be susceptible to proteolytic degradation in vivo, which could limit its oral bioavailability. Its half-life and distribution would need to be determined. The compound is typically stored as a powder at -80°C for up to 2 years or in solvent at -80°C for 6 months. The peptide is intended for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of Peptide 74 is not detailed in the provided literature. However, in vitro studies show it has no cytotoxic action at 30 μM. It is classified for research use only and not for human consumption. Standard safety precautions for handling peptides should be followed.
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| References |
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| Additional Infomation |
Additional information: Peptide 74 has the CAS number 132116-39-3. Its sequence is TMRKPRCGNPDVAN. It inhibits the activated form of MMP-2 and reduces tumor cell invasion. Peptide 74 is a research tool for studying MMP-2 biology and cancer metastasis. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C62H107N23O20S2
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|---|---|
| Molecular Weight |
1558.78508
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| Exact Mass |
1557.75
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| CAS # |
132116-39-3
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| PubChem CID |
164323
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| Appearance |
White to off-white solid powder
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| LogP |
-14
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
49
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| Heavy Atom Count |
107
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| Complexity |
3200
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| Defined Atom Stereocenter Count |
14
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| SMILES |
N/C(=N/CCC[C@@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(=O)O)CC(=O)N)=O)C)=O)C(C)C)=O)CC(=O)O)=O)=O)CC(=O)N)=O)=O)CS)=O)CCC/N=C(\N)/N)=O)=O)CCCCN)=O)NC([C@@H](NC([C@H]([C@H](O)C)N)=O)CCSC)=O)/N
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| InChi Key |
DAZBILQQVFBVPE-XKKUQSFHSA-N
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| InChi Code |
InChI=1S/C62H107N23O20S2/c1-29(2)47(57(101)74-30(3)48(92)81-38(60(104)105)25-43(65)88)83-53(97)36(26-45(90)91)80-55(99)41-16-11-22-85(41)59(103)37(24-42(64)87)75-44(89)27-73-49(93)39(28-106)82-51(95)33(14-9-20-72-62(69)70)77-54(98)40-15-10-21-84(40)58(102)35(12-6-7-18-63)79-50(94)32(13-8-19-71-61(67)68)76-52(96)34(17-23-107-5)78-56(100)46(66)31(4)86/h29-41,46-47,86,106H,6-28,63,66H2,1-5H3,(H2,64,87)(H2,65,88)(H,73,93)(H,74,101)(H,75,89)(H,76,96)(H,77,98)(H,78,100)(H,79,94)(H,80,99)(H,81,92)(H,82,95)(H,83,97)(H,90,91)(H,104,105)(H4,67,68,71)(H4,69,70,72)/t30-,31+,32-,33-,34-,35-,36-,37-,38-,39-,40-,41-,46-,47-/m0/s1
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| Chemical Name |
(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[2-[[(2R)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-sulfanylpropanoyl]amino]acetyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-4-oxobutanoic acid
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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 (~64.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (64.15 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 | 0.6415 mL | 3.2076 mL | 6.4152 mL | |
| 5 mM | 0.1283 mL | 0.6415 mL | 1.2830 mL | |
| 10 mM | 0.0642 mL | 0.3208 mL | 0.6415 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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