BRDT
BRDT (bromodomain testis-specific protein) is a testis-specific member of the BET (bromodomain and extra-terminal) family that functions as an epigenetic reader of acetylated histones and regulates transcriptional programs required for male germ-cell differentiation[1][2]. BRDT contains two bromodomains, and its first bromodomain (BD1) recognizes hyperacetylated histone H4, enabling stable chromatin association and directing chromatin remodeling during spermatogenesis[1][2]. Mechanistically, BRDT coordinates stage-specific gene expression from meiosis through post-meiotic differentiation and links histone acetylation signals to large-scale genome reorganization in developing male germ cells[2]. During spermiogenesis, BRDT promotes genome-wide histone replacement and chromatin compaction, processes required for proper sperm maturation and male fertility[2]. Experimental studies further demonstrated that BRDT is essential for meiotic chromatin organization, meiotic sex chromosome inactivation, and epigenetic reprogramming during prophase I, indicating a broader role in maintaining germ-cell genome integrity[3]. In mouse models, loss of BD1 causes severe spermiogenic defects and impaired chromatin organization, whereas complete BRDT deficiency arrests spermatogenesis before the first meiotic division and results in male sterility[1][3]. Compared with other BET family members, BRDT displays highly restricted testicular expression, making it a distinctive regulator of spermatogenesis and an attractive experimental target for reproductive biology research[2][3]. For experimental applications, the BET bromodomain inhibitor JQ1 suppresses BRDT-dependent chromatin binding and produces a reversible contraceptive effect in mice, establishing BRDT inhibition as a valuable model for studying non-hormonal male contraception and epigenetic regulation of germ-cell development[4].
References:
- [1]. Shang E, et al. The first bromodomain of Brdt, a testis-specific member of the BET sub-family of double-bromodomain-containing proteins, is essential for male germ cell differentiation. Development. 2007 Oct;134(19):3507-15. [Content Brief]
- [2]. Gaucher J, et al. Bromodomain-dependent stage-specific male genome programming by Brdt. EMBO J. 2012;31(19):3809-3820.
- [3]. Manterola M, et al. BRDT is an essential epigenetic regulator for proper chromatin organization, silencing of sex chromosomes and crossover formation in male meiosis. PLoS Genet. 2018 Mar 7;14(3):e1007209. [Content Brief]
- [4]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84. [Content Brief]
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BRDT Related Products (26)
Related Products (26)
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ABBV-744
0 ImagesABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.
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GSK778
0 ImagesSynonyms: iBET-BD1GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
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GSK046
0 ImagesSynonyms: iBET-BD2GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.
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GSK973
0 ImagesGSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
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BRDT-IN-2
0 ImagesCat. No.: HY-183248BRDT-IN-2 is a BRDT-BD1-preferring inhibitor (Ki=10 μM) with higher affinity for BRDT-BD1 than BRD4-BD1. BRDT-IN-2 preferentially binds BRDT-BD1 without direct interaction with BRDT-BD1’s Arg54 residue. BRDT-IN-2 binds BRD4-BD1 with lower affinity via structured water molecule displacement in its binding pocket. BRDT-IN-2 can be used for the research of multiple myeloma.
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BRDT-IN-1
0 ImagesCat. No.: HY-183247BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma.
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LT052
0 ImagesLT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research.
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(S)-JQ-35
0 ImagesSynonyms: TEN-010(S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma.
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RVX-297
0 ImagesCat. No.: HY-114504CAS No.: 1044871-04-6RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
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CF53
0 ImagesCF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
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BET bromodomain inhibitor 1
0 ImagesBET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
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PLK1/BRD4-IN-3
0 ImagesPLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively.
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BY27
0 ImagesCat. No.: HY-126325CAS No.: 2247236-59-3BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity.
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GXH-II-052
0 ImagesCat. No.: HY-150684CAS No.: 3031654-49-3GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc.
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NC-III-49-1
0 ImagesCat. No.: HY-150683CAS No.: 3031654-46-0NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc.
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BET-IN-13
0 ImagesCat. No.: HY-152213CAS No.: 2506823-08-9
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BET BD2-IN-1
0 ImagesCat. No.: HY-155680CAS No.: 2677039-24-4
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SB-284851-BT
0 ImagesCat. No.: HY-136794CAS No.: 219769-23-0SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET).
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