YO-2
YO-2 is a plasmin inhibitor and TP53 upregulator with anti-tumor and apoptosis-inducing activities. YO-2 upregulates the expression of TP53 and the tumor-suppressive miR-103/107, downregulates LRP1, and induces cellular DNA fragmentation and caspase cascade activation. YO-2 effectively blocks the growth of melanoma. YO-2 has been widely used in studies related to melanoma and colon cancer.
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- CAS No.: 288254-44-4
- 화학식: C31H46N4O3
- 분자량:522.72
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
YO-2 (10-30 μM; 24 h) dose-dependently inhibits plasminogen-induced proliferation of murine B16F10 melanoma cells after 24 h of incubation[1].
YO-2 (10-30 μM; 24 h) dose-dependently activates caspase 3/7 in murine B16F10 melanoma cells, with a ~10-fold increase in activity at 30 μM after 24 h of incubation[1].
YO-2 (10-30 μM; 24 h) dose-dependently downregulates anti-apoptotic BCL2 gene expression in murine B16F10 melanoma cells after 24 h of incubation[1].
YO-2 (10-20 μM) increases p53 protein levels in murine B16F10 melanoma cells at concentrations of 10 μM and 20 μM[1].
YO-2 (10-30 μM) dose-dependently upregulates p53 protein levels in murine B16F10 melanoma cells at concentrations of 10 μM, 20 μM, and 30 μM[1].
YO-2 (30 μM; 1-6 h) induces apoptotic morphological changes in rat thymocytes, including time-dependent phosphatidylserine translocation and chromatin condensation, when treated with 30 μM YO-2 for 1 to 6 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine B16F10 melanoma cells
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Concentration:10-30 μM
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Incubation Time:24 h
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Result:Increased caspase 3/7 activity in a dose-dependent fashion.
Induced a ~3-fold increase at 10 μM compared to PBS-treated controls.
Induced a ~6-fold increase at 20 μM compared to PBS-treated controls.
Induced a ~10-fold increase at 30 μM compared to PBS-treated controls.
In Vivo
Cotreatment with YO-2 (5 mg/kg; i.p.; every other day; starting day 5 post-tumor inoculation) and a single 1 mg/kg dose of Doxorubicin (HY-15142A) (day 0 post-tumor inoculation) significantly reduces melanoma tumor weight more effectively than either agent alone in a murine subcutaneous melanoma model[1].
YO-2 (5 mg/kg; i.p.; daily; starting day 5 post-tumor inoculation) significantly reduces tumor weight in mice bearing LRP1-overexpressing subcutaneous melanoma tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (8- to 12-week-old male; wild-type; subcutaneous inoculation of 1×106 B16F10 melanoma cells)[1]
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Dosage:5 mg/kg
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Administration:i.p.; daily; starting day 5 post-tumor inoculation
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Result:Reduced mean tumor weight from ~3.2 g (control) to ~1.0 g.
Increased expression of TP53, p21, miR-103, and miR-107 in tumor tissues.
Decreased expression of LRP1 in tumor tissues.
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Animal Model:C57BL/6 (8- to 12-week-old male; wild-type; subcutaneous inoculation of 1×106 B16F10 melanoma cells)[1]
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Dosage:5 mg/kg (YO-2); 1 mg/kg (doxorubicin)
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Administration:i.p. (YO-2; every other day; starting day 5 post-tumor inoculation); single dose (doxorubicin; day 0 post-tumor inoculation)
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Result:Reduced mean tumor weight to ~0.7 g, compared to ~2.8 g (untreated control), ~1.5 g (YO-2 alone), and ~2.5 g (doxorubicin alone).
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Animal Model:C57BL/6 (8- to 12-week-old male; wild-type; subcutaneous inoculation of 1×106 LRP1-overexpressing B16F10 melanoma cells)[1]
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Dosage:5 mg/kg
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Administration:i.p.; daily; starting day 5 post-tumor inoculation
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Result:Reduced mean tumor weight from ~4.0 g (untreated control) to ~2.0 g in LRP1-overexpressing tumors.
Chemical Information
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CAS No. 288254-44-4
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분자량 522.72
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화학식 C31H46N4O3
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SMILES
O=C([C@H]1CC[C@@H](CC1)CN)N[C@H](C(NCCCCCCCC)=O)CC2=CC=C(C=C2)OCC3=CC=NC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Salama Y, et al. YO2 Induces Melanoma Cell Apoptosis through p53-Mediated LRP1 Downregulation. Cancers (Basel). 2022;15(1):288. Published 2022 Dec 31. [Content Brief]
[2]. Lee E, et al. A selective plasmin inhibitor, trans-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-octylamide (YO-2), induces thymocyte apoptosis. Biochem Pharmacol. 2002;63(7):1315-1323. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YO-2 Related Classifications
HY-183877 Related Classifications
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