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Cat. No. Product Name CAS No. Information
PC-35172

ABBV-744

2138861-99-9

ABBV-744 (ABBV744) is a potent, BDII-selective BET bromodomain inhibitor, ABBV-744 is a potent, selective inhibitor of the AR transcription activity; induces tumor growth inhibition in LNCaP and MDA-Pca-2b xenograft models.

Prostate Cancer

Phase 1 Clinical

PC-35097

ZL0454

2229042-77-5

ZL0454 is a potent, highly selective small-molecule BRD4 inhibitor with IC50 of 49 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively; displays selectivity over BRD2, BRD3, and BRDT( BRD2-BD1 and BRD2-BD2, IC50=772 and 1836 nM); disrupts the BRD4 complex with Pol II and histones, inhibits poly(I:C)-induced expression of innate immune genes IL6 and CIG5 in human small airway epithelial cells (hSAECs) (IC50=0.62 and 0.57 uM); blocks Poly(I:C)-induced inflammation and neutrophilia in vivo.

PC-35096

ZL0420

2229039-45-4

ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively; displays selectivity over BRD2, BRD3, and BRDT (BRD2-BD1 and BRD2-BD2, IC50=803 and 1736 nM); disrupts the BRD4 complex with Pol II and histones, inhibits poly(I:C)-induced expression of innate immune genes IL6 and CIG5 in human small airway epithelial cells (hSAECs) (IC50=0.54 and 0.51 uM); blocks Poly(I:C)-induced inflammation and neutrophilia in vivo.

PC-63255

SJ830599

2215098-23-8

SJ830599 is a modest selective BRD2-BD2 inhibitor with IC50 of 0.61 uM, 3.3-fold selectivity over BRD2-BD1; demonstrates cytotoxicity against several pediatric cancer cell lines with EC50 values (HD-MB03 EC50=480 nM) comparable to BET inhibitor (BETi) clinical candidates.

PC-63245

Y08060

2222565-19-5

Y08060 is a potent and selective BET inhibitor with Kd of 306 nM for BRD4 BD1, displays excellent selectivity for BET subfamily over other non-BET family with the exception of moderate inhibition of CBP/EP300; esuppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC in prostate cancer cell lines. such as C4-2B, LNCaP, and 22Rv1; demonstrates good PK profile with high oral bioavailability (61.54%).

PC-43338

JQ1

1268524-70-4

(+)-JQ-1 (JQ1) is a potent, selective, cell-permeable BET bromodomain inhibitor with IC50 of 77 nM/33 nM for BRD4 BD1 and BD2, respectively; induces rapid expression of keratin in treated NMC 797 cells, displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models.

PC-62636

FL-411

2118944-88-8

FL-411 is a novel small-molecule inhibitor of BRD4, induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction and activating AMPK-mTOR-ULK1-modulated autophagic pathway in breast cancer cells; induces ACD pathways involved in HMGB1, VDAC1/2, and eEF2, displays a therapeutic potential on both breast cancer xenograft mouse and zebrafish models.

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