XMD8-92, via inhibition of BMK1 activation, significantly induces p21 expression in cells, and mediates suppression of cancer cell proliferation. XMD8-92 markedly abrogates the inhibitive effects of hydroxysafflor yellow A (HSYA) on hepatic stellate cell (HSC) activation, and blockes the HSYA-mediated MEF2C down-regulation.
|Cell lines||A549 cell lines|
|Preparation method||Control and shBNIP3/shBNIP3L A549 sphere cells were treated with/without 4 μmol/L XMD8-92 for 36 hrs, and collected by trypsinization and centrifugation at 300 G for 5 mins. The resultant cells were washed twice with cold PBS and resuspended in 100 μL Annexin-binding buffer.|
|Incubation time||36 h|
|Animal models||Nod/Scid mice bearing HeLa xenograft, C57Bl/6 mice bearing LL/2 xenograft|
|Dosages||~50 mg/kg twice a day|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||73 mg/mL warmed in DMSO|
BIX02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor.
Park SJ, et al. Cancer Lett. 2016 Oct 28;381(2):314-22. PMID: 27543359.
Inhibition of BMK1 pathway suppresses cancer stem cells through BNIP3 and BNIP3L.
Song C, et al. Oncotarget. 2015 Oct 20;6(32):33279-89. PMID: 26432836.
XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism.
Sureban SM, et al. Cancer Lett. 2014 Aug 28;351(1):151-61. PMID: 24880079.
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