epigeneticreaderdomain

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.

ZEN-3862 (Willardiine) is an inhibitor of BET(IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively). ZEN-3862 can be used to form PROTACs to induce degradation of BRD4.

PROTAC BRD9 Degrader-6, with an IC50 value of 0.13 nM, is a potent degrader of BRD9 suitable for research on BAF complex-related disorders [1].

PROTAC BRD3 BRD4-L degrader-2, a PROTAC molecule, selectively degrades cellular BRD3 and BRD4-L with K i values of 16.91 and 2.8 nM, respectively, and exhibits robust antitumor activity in mouse xenograft models, serving as a research tool for cancer [1].

Tz-Thalidomide is a tetrazine-modified Thalidomide (E3 ligase ligand) with some affinity for BRD4.

GXF-111, a proteolysis targeting chimera (PROTAC) molecule, efficiently induces the selective degradation of the BRD3 and BRD4-L proteins. It exhibits high binding affinities to both BRD3 BD1 and BRD3 BD2, with K i values of 11.97 nM and 2.35 nM, respectively. This compound is utilized in cancer research [1].

MZP-54 is a selective degrader of BRD3 4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)

PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based degrader targeting BRD4, with a pDC50 of 9.2 in MOLT4 cells over 24 hours [1].

(S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).

WWL0245 is a potent and selective BRD4-targeting PROTAC that exhibits sub-nanomolar degradation efficiency (DC50 < 1 nM) for BRD4 over BRD2 3 and PLK1 (DC50 > 1 μM). It demonstrates pronounced selective cytotoxicity in BETi-sensitive cancer cell lines, particularly in AR-positive prostate cancer lines, making it a promising candidate for research in AR-positive prostate cancer and a valuable tool for the investigation of BRD4's biological function [1].

PROTAC BRD4 Degrader-21 (Comp 74), a potent BRD4 degrader, has shown significant inhibition of tumor growth in mouse xenograft models, indicating its potential for anticancer research [1].

FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader that targets FKBP12F36V with FKBP12F36V expressed in-frame with a protein of interest, and selectively degrades the BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to the E3 ubiquitin ligase CRBN.

SMD-3040 is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM), comprising an SMARCA2 4 ligand, a linker, and a VHL ligand. It exhibits excellent degradation selectivity for the SMARCA2 protein over the SMARCA4 protein and has demonstrated robust tumor growth inhibition in xenograft models [1].

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.

dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.

SJ46421, a PROTAC protein degrader derived from (+)-JQ-1, targets KLHDC2. It efficiently forms a stable ternary complex with KLHDC2, exhibiting an IC50 of 7.8 nM. Furthermore, SJ46421 promotes the polyubiquitination of the BD2 domain of BRD2, BRD3, or BRD4.

dBAZ2 is a pioneering PROTAC degrader targeting BAZ2A and BAZ2B, with DC50 values of 180 nM for BAZ2A and 250 nM for BAZ2B.

AB3067 is a PROTAC degrader targeting BET protein, efficiently recruiting two distinct E3 ligases, Cereblon and VHL, with strong affinity (demonstrated by IC50 values of 559 nM for VHL and 190 nM for CRBN in vivo HEK293). It degrades BRD2, BRD3, BRD4, and CRBN with DC50 values of 2.1~2.3, 1.6, 15, and 75 nM, respectively. Additionally, AB3067 inhibits the proliferation of RKO cells, with an EC50 of 111 nM. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL and CRBN)

PROTAC BRD4 Degrader-29 (compound 7a) is a potent BRD4 PROTAC degrader with a DC50 of 89.4 nM, playing a significant role in cancer research.

SJ44236 is a BET PROTAC degrader capable of degrading BRD2 (DC50 = 0.127 nM), BRD3, and BRD4. It shows cytotoxicity in MV4-11 and HD-MB03 cells with IC50 values of 0.12 nM and 0.92 nM, respectively. The compound downregulates c-Myc expression and upregulates p53 expression. In mice, SJ44236 demonstrates good oral bioavailability (45%). [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonE3ligaseLigand 54]

PROTACSMARCA2 4 degrader-36 (Compound 29) is a potent dual degrader targeting SMARCA2 and SMARCA4, exhibiting DC50 values of 0.22 nM and 0.85 nM, respectively. Additionally, PROTACSMARCA2 4 degrader-36 demonstrates antiproliferative activity.