brd4 in 2

BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC 50 value of 9.9 nM.

PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718.

BRD4 D1-IN-2 (compound 26) 是一种选择性的、有效的 BRD4 D1 抑制剂，其 IC50 值小于 0.092 μM。BRD4 D1-IN-2 对 BRD4 D1 具有 15 nM 亲和力，对 BRD2 D1 和 BRD4 D2 具有 500 倍以上的选择性。

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

PROTAC BRD2 BRD4 degrader-1 (compound 15) serves as a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination of BRD4 and BRD2 compared to BRD3. Its efficacy in suppressing solid tumors manifest with minimal cytotoxic effects. This compound comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN) cullin 4A[1].

BRD4 CK2-IN-1 是靶向 BRD4 和 CK2 的小分子抑制剂，对 BRD4 的 IC 50 值为 180nM，对 CK2 的IC 50 值为 230 nM。BRD4 CK2-IN-1 可抑制 MDA-MB-231 和 MDA-MB-468 细胞的增殖并诱导细胞凋亡和自噬相关细胞死亡，可用于研究三阴乳腺癌。

PROTACBRD4配体-2盐酸盐是一种专门针对BRD4蛋白的配体，主要用于PROTACCFT-2718的合成过程中。

PLK1 BRD4-IN-2 (compound 15) 作为一种BI-2536类似物，是PLK1和BRD4的双重抑制剂。它针对Polo样激酶1 (PLK1) 和 BRD4溴结构域 (BRD4-BD1，IC50=28 nM) 以及PLK1 (IC50=40 nM) 展示出高效的抑制活性。

CF53 是一种高效、选择性、可口服的 BET 抑制剂，对 BRD4 BD1 的 Ki 值为 <1 nM，Kd 值为 2.2 nM，IC50 值为 2 nM；CF53 对 BRD2，BRD3，BRD4 和 BRDT BET 蛋白的 BD1 和 BD2 两个结构域都有高亲和性，对其选择性远高于非含溴结构域 BET 蛋白。CF53 在体外和体内都具有显著的抗肿瘤活性。

BRD4-BD1-IN-2 是一种具有选择性和有效性的 BRD4-BD1 抑制剂，IC50 值为 2.51 µM ，是对 BRD4-BD2 抑制活性的 20 倍。BRD4-BD1-IN-2 可用于研究心血管疾病和癌症相关疾病。

BET-IN-2 is a BET inhibitor (IC50: 52 nM for BRD4-BD1).

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1].

(R)-(-)-JQ1 Enantiomer 是 (+)-JQ1 的立体异构体。 (+)-JQ1 是一种 BET 溴结构域抑制剂，对BRD4(1 2)的IC50 为 77 和 33 nM。

HDAC3 BRD4-IN-1 (compound 26n) 是一种HDAC3 BRD4的抑制剂，其针对HDAC3的IC50为8 nM，而对HDAC1和HDAC2的IC50分别为220 nM和120 nM。HDAC3 BRD4-IN-1 展现出抗肿瘤和抗增殖作用，并通过上调Ac-H3和下调c-Myc实现。该化合物在人肝脏微粒中的半衰期为29.36分钟 (t1 2=29.36 min)。

AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) 是 AZD5153的6-羟基-2-萘甲酸盐形式。AZD5153是一种有口服活性的选择性 BET BRD4溴结构域抑制剂，对BRD4的IC50值为1.7nM。

TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells. 1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020)

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC50 of 7.5 nM[1]. [1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020)

BRD4 Inhibitor-15 (compound 13) is a highly potent and specific inhibitor of BRD4, effectively inhibiting it with an IC50 of 18 nM. By regulating the Bcl-2 Bax proteins and activating the caspase-3 signaling pathway, BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells. Additionally, it effectively down-regulates the c-Myc level in 22RV1 cells. Due to its properties, BRD4 Inhibitor-15 is a valuable compound for research related to prostate cancer [1].

BRD4-BD1 2-IN-1 is a highly effective inhibitor of BRD4, specifically targeting the BRD4 BD-1 and BRD4 BD-2 domains with IC 50 values of <100 nM each (US20150148375A1, compound 5) [1].

PARP1 BRD4-IN-2 是一种有效的、选择性的 PARP1 (IC50: 197 nM) 和 BRD4 (IC50: 238 nM) 抑制剂。PARP1 BRD4-IN-2 能够抑制 DNA 损伤修复，阻滞 G0 G1 细胞周期转变，诱导细胞凋亡 (apoptosis)。PARP1 BRD4-IN-2 对 MDA-MB-468 小鼠异种移植瘤模型表现出抗肿瘤效果。PARP1 BRD4-IN-2 能够用于研究三阴性乳腺癌 (TNBC)。

BRD4-BD1 2-IN-2 是 BRD4-BD2 的有效抑制剂，能够作用于 BRD4 BD2 (IC50<0.5 nM) 和 BRD4 BD1 (IC50<300 nM)。

PROTACBRD3 BRD4-L degrader-2 是一款可以特异性地降解BRD3和BRD4-L的PROTAC分子，其对BRD3的Ki值为16.91 nM，对BRD4-L为2.8 nM。在小鼠异种移植模型中，该分子展示了卓越的抗肿瘤效果，可被应用于癌症相关研究。

Emetine hydrochloride (NSC 33669)，一种从ipecac根部提取的生物碱，用于临床上作为催吐及抗原生动物药物。它能够降低HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2)和BRD4，抑制细胞自噬，并展现抗疟疾、抗病毒、抗细菌及抗变形虫效果。