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Chemical Structure : SJ432
Catalog No.: PC-72187Not For Human Use, Lab Use Only.
SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.
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SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.
SJ432 is more water soluble than SJ018 (40 uM vs <0.1 uM).
SJ432 potently inhibits MV4-11 cell growth with GI50 of 8 nM, is more effective than JQ1 at reducing levels of MYC protein in NB cell lines, upregulated p21& GADD45H and downregulated CCND2 & ODC1, C-MYC target genes.
SJ432 (15 mg/kg, i.p.) significantluy reduced tumor volumes in pediatric NB xenograft SK-N-AS, with essentially no loss in body weight.
| M.Wt | 371.444 | |
| Formula | C22H21N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. P Jake Slavish, et al. Cancer Res. 2020 Sep 1;80(17):3507-3518.
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