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^[1][2].

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.

YO-2 (5 mg/kg; i.p.; daily; starting day 5 post-tumor inoculation) significantly reduces melanoma tumor weight and modulates key gene expression markers (increased TP53, p21, miR-103/107; decreased LRP1) in a murine subcutaneous melanoma model^[1].
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.

522.72

C₃₁H₄₆N₄O₃

288254-44-4

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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Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]