BV6 TFA

BV6 TFA is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis ( IAP ) family. BV6 TFA shows an IC₅₀ of 7.2 μM in MTS assays in HCC193 cells. BV6 TFA can be used in the research of endometrial cancer and endometriosis ^{[1] [2]}.

In Vivo, BV6 TFA (10 mg/kg, twice weekly for 4 weeks, i.p.) attenuates the intensity of IAPs expression^[2]. BV6 TFA (10 mg/kg, twice weekly for 4 weeks, i.p.) reduces the total number of lesions and the percentage of Ki67-positive cells compared to the control^[2].

In Vitro, BV6 TFA (250 nM-30 μM, 24 h) induces apoptosis in HCC193 and H460 lung cancer cell lines in a concentration- and time-dependent manner. BV6 TFA (250 nM-30 μM, 24 h) can also enhance the sensitivity of HCC193 and H460 cell lines to radiation^[1]. BV6 TFA (1μM 24 h; 5 μM, 48 h) significantly sensitizes the cell to radiation (HCC193-DER=1.38, at 1μM BV6; H460-DER=1.42, at 5μM BV6)^[1].

References:
[1]. Li W, et al. BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro. J Thorac Oncol. 2011 Nov;6(11):1801-9.
[2]. Uegaki T, et al. Inhibitor of apoptosis proteins (IAPs) may be effective therapeutic targets for treating endometriosis. Hum Reprod. 2015 Jan;30(1):149-58.