KBU2046
CAS No. : 1143863-69-7
| Size | Price | Stock |
|---|---|---|
| 5mg | $57 | In-stock |
| 10mg | $80 | In-stock |
| 25mg | $170 | In-stock |
| 50mg | $267 | In-stock |
| 100mg | $405 | In-stock |
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| Cat. No. : | HY-120548 |
| M.Wt: | 242.25 |
| Formula: | C15H11FO2 |
| Purity: | >98 % |
| Solubility: | DMSO : 50 mg/mL (ultrasonic) |
KBU2046 is an orally active transforming growth factor-β (TGF-β1) inhibitor. KBU2046 reduces integrin family protein expression, decreases Raf, RIPK1 and ERK phosphorylation to deactivate the ERK signaling pathway, and down-regulates genes linked to TGF-β1 maturation. KBU2046 suppresses tumor cell motility, impedes cancer invasion and metastasis, and inhibits human ESCC growth and metastasis in a murine model. KBU2046 can be used for the researches of triple-negative breast cancer and esophageal squamous cell carcinoma[1][2].
In Vitro:KBU2046 (1-10 μM; 24-48 h) does not significantly alter the proliferation of MDA-MB-231 or BT-549 TNBC cells[1].
KBU2046 (1-10 μM; 24 h) dose-dependently inhibits TGF-β1-induced motility of MDA-MB-231 and BT-549 TNBC cells, with maximum inhibition at 10 μM, reducing motility to 50.77% and 36.09% of control levels, respectively[1].
KBU2046 (10 μM; 24 h) significantly down-regulates the mRNA expression of LRRC8E, LTBP3, DNAL1, and MAFF in MDA-MB-231 and BT-549 TNBC cells[1].
KBU2046 (1-10 μM; 48 h) dose-dependently suppresses integrin αv and integrin α6 protein expression in MDA-MB-231 and BT-549 TNBC cells, and reverses TGF-β1-mediated up-regulation of these integrins[1].
KBU2046 (10 μM; 15-60 min) time-dependently inhibits phosphorylation of Raf1 and ERK1/2 in MDA-MB-231 and BT-549 TNBC cells, with significant suppression evident within 15 min of treatment[1].
KBU2046 (1-10 μM; 24-48 h) inhibits collective migration of KYSE-30 and KYSE-410 ESCC cells in a time- and concentration-dependent manner[2].
KBU2046 (10 μM; 72 h) inhibits EGF and TGF-β-stimulated single-cell migration and invasion of KYSE-30 and KYSE-410 ESCC cells[2].
KBU2046 (1-10 μM; 72 h) does not inhibit proliferation of KYSE-30 or KYSE-410 ESCC cells after 72-hour incubation[2].
KBU2046 (10 μM; 30 min) inhibits EGF-stimulated phosphorylation of RIPK1 at Ser166 in KYSE-30 and KYSE-410 ESCC cells[2].
KBU2046 (1-10 μM) downregulates ITGA3, ITGA6, and ITGAV expression in KYSE-30 and KYSE-410 ESCC cells in a concentration-dependent manner[2].
KBU2046 (10 μM) selectively modulates expression of motility-related proteins in KYSE-30 ESCC cells, with significant downregulation of integrin family members and other ECM-adhesion proteins that are overexpressed in human ESCC[2].
In Vivo:KBU2046 (80 mg/kg; i.g.; every other day; 12 total doses) completely inhibits pulmonary metastasis of ESCC cells in male NOD-SCID mice[2].
KBU2046 (80 mg/kg; i.g.; every 2 days; 12 total doses) reduces mean ESCC tumor volume to 62% of control levels in male athymic nude mice, without causing significant systemic toxicity[2].
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