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Cat. No. Name Size Price Add Cart
KI3565LLL12QuoteQuote

Chemical Characteristic

Product NameLLL12
CAS No.1260247-42-4
Molecular Weight 303.29
FormulaC14H9NO5S
Chemical Name5-hydroxy-9,10-dioxo-9,10-dihydroanthracene-1-sulfonamide
Smilesc1(cccc2C(=O)c3c(cccc3C(=O)c12)O)S(=O)(=O)N
Chemical Structure

Biological activities

LLL12 is a novel signal transducer and activator of transcription 3 (STAT3) inhibitor. LLL12 inhibits human breast cancer cell lines (MDA-MB-231 and SK-BR-3) viability with IC50s of 0.97, 3.09 µM, respectively. LLL12 inhibits human pancreatic cancer cell lines (PANC-1 and HPAC), and glioblastoma cell lines (U87 and U373) viability with IC50s of 0.29, 0.16, 0.21 and 0.86 µM, respectively. LLL12 inhibits STAT3 phosphorylation induced by interleukin-6 (IL-6) in MDA-MB-453 breast cancer cells and induces apoptosis in human breast and pancreatic cancer cells. LLL12 inhibits STAT3-dependent transcriptional activities and transcription of downstream targets of STAT3 in MDA-MB-231 breast cancer cloned cells. LLL12 inhibits colony formation and cell migration and works synergistically with doxorubicin and gemcitabine.[1] LLL12 inhibits the secretion of IL-6 and leukemia inhibitory factor (LIF) in medulloblastoma and glioblastoma cell lines. LLL12 induces cell apoptosis in medulloblastoma and glioblastoma cell lines.[2] LLL12 (100 nM) significantly inhibits VEGF-stimulated STAT3 phosphorylation in human umbilical cord vascular endothelial cells (HUVECs), reduces their proliferation/migration and inhibits VEGF-induced tube formation.[3] LLL12 significantly inhibits tumor growth in the MDAMB-231 and U87 xenografted mice.[1] In scid mice, LLL12 (5 mg/kg daily) reduces microvessel invasion into VEGF-infused Matrigel plugs by 90%.[3]

Protocols

In vitro, LLL12 is dissolved in sterile DMSO.[1]

References

[1] Lin L, et al. A novel small molecule, LLL12, inhibits STAT3 phosphorylation and activities and exhibits potent growth-suppressive activity in human cancer cells. Neoplasia. 2010, 12(1): 39-50.
[2] Ball S, et al. The small molecule, LLL12, inhibits STAT3 phosphorylation and induces apoptosis in medulloblastoma and glioblastoma cells. PLoS One. 2011, 6(4): e18820.
[3] Bid HK, et al. Anti-angiogenic activity of a small molecule STAT3 inhibitor LLL12. PLoS One. 2012, 7(4): e35513.

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Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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