Hypothemycin (Synonyms: NSC 354462) |
| Katalog-Nr.GC43885 |
Hypothemycin, ein Pilz-Polyketid, ist ein Multikinase-Inhibitor mit Kis von 10/70 nM, 17/38 nM, 90 nM, 900 nM/1,5 μM und 8,4/2,4 μM fÜr VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRa bzw. ERK1/ERK2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 76958-67-3
Sample solution is provided at 25 µL, 10mM.
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Hypothemycin is a resorcylic acid lactone polyketide originally isolated from H. tricothecoides that has diverse biological activities, including fungicidal, kinase inhibitory, and anticancer properties.[1],[2],[3],[4,][5],[6] It is active against the pathogenic fungi P. litchii, completely inhibiting spore germination when used at a concentration of 0.78 µg/ml.[2] Hypothemycin inhibits MEK (IC50 = 15 nM) and other protein kinases containing a conserved cysteine residue in the ATP-binding domain, including ERK, PDGFR, VEGFR, PKD1, and MAPKAP5/MK5.[3],[4] It also inhibits transforming growth factor β-activated kinase 1 (TAK1) in vitro (IC50 = 33 nM).[5] Hypothemycin inhibits proliferation of cancer cell lines dependent on activating mutations, including A549, MV-4-11, and EOL1 cells (IC50s = 6, 0.006, and 0.0004 µM, respectively) and reduces tumor growth in Ma44 and HCT116 mouse xenograft models when administered at a dose of 25 mg/kg per day.[4],[6]
Reference:
1. Agatsuma, T., Takahashi, A., Kabuto, C., et al. Revised structure and stereochemistry of hypothemycin. Chem. Pharm. Bull. 41(2), 373-375 (1993).
2. Xu, L., Xue, J., Wu, P., et al. Antifungal activity of hypothemycin against Peronophythora litchii in vitro and in vivo. J. Agric. Food Chem. 61(42), 10091-10095 (2013).
3. Zhao, A., Lee, S.H., Mojena, M., et al. Resorcylic acid lactones: Naturally occurring potent and selective inhibitors of MEK. J. Antibiot. (Tokyo) 52(12), 1086-1094 (1999).
4. Schirmer, A., Kennedy, J., Murli, S., et al. Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides. Proc. Nat. Acad. Sci. USA 103(11), 4234-4239 (2006).
5. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).
6. Tanaka, H., Nishida, K., Sugita, K., et al. Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor. Jpn. J. Cancer Res. 90(10), 1139-1145 (1999).
| Cas No. | 76958-67-3 | SDF | |
| Überlieferungen | NSC 354462 | ||
| Chemical Name | (1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione | ||
| Canonical SMILES | COC1=CC(O)=C(C(O[C@@H](C)C/C=C\C2=O)=O)C([C@@H]3[C@](O3)([H])C[C@H](O)[C@@H]2O)=C1 | ||
| Formula | C19H22O8 | M.Wt | 378.4 |
| Löslichkeit | DMSO: 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6427 mL | 13.2135 mL | 26.4271 mL |
| 5 mM | 0.5285 mL | 2.6427 mL | 5.2854 mL |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6427 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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