bet proteins

Molibresib (GSK525762) 是一种 BET 溴结构域抑制剂，IC50为32.5在42.5 nM 之间。

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。

ZEN-3411 是一种可口服且具有高效性的 BET 抑制剂，抑制 BRD4(BD1)，BRD4(BD2) 和BRD4(BD1BD2)，抑制过度产生 BET 蛋白的肿瘤细胞的生长。

Hexamethylene bisacetamide 抑制 BET Bromodomain 蛋白。

BET-BAY 002 S enantiomer为BET-BAY 002的S型对映异构体，属于BET小分子抑制剂。

Molibresib besylate (GSK 525762C) 是一种具有选择性和高效性的溴结构域和末端外 （BET） 蛋白家族抑制剂，具有潜在的抗癌活性，可用于研究难治性血液系统恶性肿瘤疾病。Molibresib besylate 产生活性氧 （ROS），增强 ATM 激活。

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins, with an IC50 of 9.6 nM.

(R)-BAY1238097是BAY1238097的R-异构体，其活性相对较低。BAY1238097 是一种针对 BET 蛋白与组蛋白结合的高效选择性抑制剂，在各种急性髓性白血病（AML）和多发性骨髓瘤（MM）模型中显示出显著的抗增殖作用。其高活性是通过下调 c-Myc 水平并随后调节其下游转录组实现的。

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound utilized in the synthesis of ARV-771. ARV-771, a BET PROTAC degrader relying on von Hippel-Landau (VHL) E3 ligase, demonstrates potent degradation of BET protein in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound serves as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, that facilitates the recruitment of von Hippel-Lindau (VHL) protein.

PROTAC BET Degrader-3 is a potent degrader of BET proteins based on the PROTAC (PROteolysis TArgeting Chimera) technology.

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].

Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate consisting of an E3 ligase ligand-linker, incorporating the Thalidomide-based cereblon ligand and a linker moiety. This compound, Thalidomide-NH-C4-NH2 TFA, is utilized as a component in PROTAC BRD2/BRD4 degrader-1, which is a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1].

BET-IN-28 (Compound 44) 是一种强效的溴结构域和末端外结构域 (BET) 抑制剂，对 BRD4-BD1 的 IC50 值为 4.47 nM。BET-IN-28 能够阻止 BET 蛋白与组蛋白尾部 N-乙酰化赖氨酸残基的相互作用，从而下调特定基因的表达。BET-IN-28 适用于血液系统恶性肿瘤和实体瘤的研究。

BTR2004 是一种专门作用于 BET 家族 (BRD2/3/4) 蛋白的 PROTAC 降解剂。该化合物通过与 BRD 蛋白和 KLHL20 结合形成三元复合物，利用 UPS 路径引发泛素化及蛋白酶体降解。这使 BTR2004 在 PC3 前列腺癌和 MDA-MB-231 乳腺癌细胞系研究中具有潜力。

K2-B4-5e 是一种以 KLHDC2 为基础的 E3 连接酶BRD4和雄激素受体 (AR) 降解的PROTAC，能够快速高效地在细胞中降解BET家族和AR蛋白。

IBG3 是一种含有双 JQ1 的 BET 分子胶降解剂，其目标是通过分子内二价胶降解蛋白质。IBG3 可降解 BRD2 和 BRD4，DC50值分别为 8.6 pM 和 6.7 pM。

Progranulin modulator-2 (compound 18A) 是一种创新的 bromodomain and extra-terminal domain (BET) 抑制剂。它通过靶向BET蛋白家族成员来提升PGRN的表达水平。Progranulin modulator-2 在研究BET蛋白对神经发育、神经可塑性及神经退行性变中的作用时，可以被广泛应用。

PROTACBET Degrader-12 (Compound 8b) 是一种靶向含溴结构域和额外末端结构域 (BET) 蛋白的PROTAC降解剂，通过DCAF11依赖机制降解BRD3和BRD4。它能够抑制KBM7细胞的活力，DC50值为305.2 nM。

GSK2820151 is an orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins with potential antineoplastic activity.

RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell

EN219 是一种 E3 泛素连接酶 RNF114 招募剂，特异性结合其本质无序区域的 C8 半胱氨酸，IC50 为 470 nM。EN219 可在体外实验中抑制 RNF114 介导的自泛素化和 p21 泛素化（50 μM）。在 1 μM 条件下，EN219 可与包括微管 β1 链（TUBB1）、热休克蛋白 60（Hsp60/HspD1）及组蛋白 H3.1 (HIST1H3A) 在内的多种蛋白相互作用（231MFP 乳腺癌细胞）。此外，EN219 可与溴结构域抑制剂 (+)-JQ1 偶联，构建可降解 BRD4 的 PROTAC。

Mivebresib (ABBV-075) 是一种有效的，口服活性的溴结构域和末端结构域 (BET) 抑制剂，结合BRD4的Ki 值是 1.5 nM。

GSK097 is a highly potent and selective inhibitor of the second bromodomain (BD2) found in bromodomain and extra-terminal domain (BET) proteins. It exhibits a remarkable 2000-fold selectivity for BD2 over BD1, as indicated by BRD4 data. Additionally, GSK097 demonstrates solubility of over 1 mg/mL in FaSSIF media.

BET bromodomain inhibitor 1 is an orally active, selective inhibitor of bromodomain and extra-terminal (BET) proteins. It specifically inhibits BRD4 with an IC50 of 2.6 nM. Additionally, BET bromodomain inhibitor 1 demonstrates high affinities towards BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, and 2.1 nM, respectively. This compound exhibits anti-cancer activity.