protac brd-9-binding moiety 1 hydrochloride

PROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.

PROTAC BRD4 ligand-1 是 PROTAC GNE-987 靶向 BRD4 蛋白的配体，也是一种 BET 的抑制剂。

SMARCA-BD ligand 1 for Protac 能够与 BAF ATPase 亚基 SMARCA2 结合，可用于 PROTAC 技术，用于降解 SMARCA2。

Homo-PROTAC cereblon degrader 1 (compound 15a) 是一种高效 cereblon 降解剂，对 IKZF1 和 IKZF3 的影响很小。

SMARCA-BD ligand 1 for Protac dihydrochloride 是一种能够与 BAF ATPase 亚基 SMARCA2 结合的化合物，基于 PROTAC 技术，使 SMARCA2 降解。

Homo-PROTAC pVHL30 degrader 1 是一种基于 PROTAC 的 pVHL30 降解剂。

PROTAC ERRα ligand 1 是一种雌激素相关受体 α (ERRα) 拮抗剂，能够作用于 ERRα (IC50:0.04 μM)和 ERRγ (IC50:2.8 μM)。

PROTAC BRAF-V600E degrader-1 (Compound 23) 选择性地诱导 BRAF-V600E 的降解，而不是野生型 BRAF。

PROTACSOS1 degrader-8 (Compd 10) 是SOS1的PROTAC降解剂，其中包含SOS1配体（红色）、连接子（黑色）和E3连接酶配体（蓝色）。

PROTACeDHFR Degrader-1是一种高效的PROTAC，针对eDHFR-YFP和多种POI（如YFP、荧光素酶）具有显著的降解作用。

PROTAC CDK9 Degrader-1 是一种选择性 CDK9 降解剂，是由Cereblon 配体和CDK 配体相连的PROTAC。

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1 Sirt3 (IC50s > 100 μM)[1].

PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) with an IC50 of 6.5 nM.

9-Decyn-1-ol is an alkyl ether-based PROTAC linker suitable for synthesizing PROTACs. It serves as a conjugation agent to combine GDC-0068 and Lenalidomide, resulting in the formation of INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that operates through the PROTAC mechanism. It effectively inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1].

PROTACTYK2 degrader-1 (CPD-155), 作为TYK2的PROTAC靶向降解剂，其Dmax超过60%。 (Srtucture Note: PINK, TYK2 ligand 1; Blue, VHL ligand Thalidomide; Black, linker)

PROTACpan-IAP degrader-1 (Compound 9) 是一种 pan-IAPPROTAC 降解剂。PROTACpan-IAP degrader-1 在 MM.1S 细胞中降解 XIAP、cIAP1 和 cIAP2 的 DC50分别为 0.7、2.4 和 6.2 nM。

PROTACAR-NTD antagonist 1 (compound 18) 是一款针对雄激素受体AR-V7变体的PROTACs，它特异性地拮抗AR的N末端结构域 (AR-NTD)，能有效诱导前列腺癌细胞凋亡，并在VCaP细胞中以1 μM 和 5 μM的浓度分别实现了62.2%和71.1%的AR-V7蛋白降解率。

PROTAC tubulin-Degrader-1（化合物 W13）作为PROTAC tubulin的抑制剂，展示了对人类肺癌的抗肿瘤活性。

PROTACGDI2 Degrader-1（化合物 21）为高效的PROTACGDI2降解剂，在GDI2过表达的胰腺异种移植模型中展现出显著的体内抗肿瘤活性。

PROTACNSD3 degrader-1 (compound 56)，是一种定向作用于NSD3蛋白的PROTAC。在NCI-H1703和A549肺癌细胞系中，该化合物能特异性诱导NSD3的降解，其DC50值分别为1.43 μM和0.94 μM。PROTACNSD3 degrader-1能够抑制H3K36的甲基化，触发细胞凋亡以及细胞周期阻滞，同时降低包括CDC25A、ALDH1A1和IGFBP在内的NSD3相关基因的表达水平。

PROTAC CBP P300 Degrader-1 is an effective compound that degrades CBP P300 in a potent manner. It significantly reduces cell viability in various cancer cell lines.

PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1]. PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng mL) are incubated with HeLa cells for 24 h, and a significant dose-dependent degradation is observed. PROTAC IDO1 Degrader-1 combined with chimeric antigen receptor-modified T (CAR-T) cells can improve the tumor-killing activity of HER-2 CAR-T cells[1].PROTAC IDO1 Degrader-1 induces significant and persistent degradation of IDO1 with maximum degradation (dmax) of 93% in HeLa cells[1]. [1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.

PROTACHDAC6 degrader (Compound A6) 为有效且选择性的PROTACHDAC6降解剂，具有3.5 nM的DC50。在髓系白血病细胞系中，通过诱导凋亡（apoptosis）表现出抗增殖活性。

PROTACBRD9-binding moiety 5 是一种选择性 BRD9结合剂，IC50为 4.20 μM，可用于合成 PROTACs。PROTACBRD9-binding moiety 5 对癌细胞具有抗增殖活性。

PROTAC BRD4 Degrader-9 (compound 8a) is a novel chemical compound consisting of ligands for von Hippel-Lindau and BRD4, connected by a PROTAC moiety. This compound can effectively degrade the BRD4 protein in PC3 prostate cancer cells. When conjugated with STEAP1 and CLL1 antibodies, PROTAC BRD4 Degrader-9 exhibits potent activity, with respective DC50 values of 0.86 nM and 7.6 nM.

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 是一种靶向 SGK3 且与 VH032 VHL 结合配体的 PROTAC 偶联物，可诱导内源性 SGK3 降解。PROTAC SGK3 degrader-1 可抑制GDC0941诱导的癌细胞增殖。

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

Halo PROTAC 1 is a PROTAC, which is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker[1].

(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1, which is an estrogen-related receptor alpha (ERRa) degrader. PROTAC ERRα Degrader-1 consists of an MDM2 ligand binding moiety, a linker and an ERRa binding moiety [1].

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.

PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.

PROTACSOS1 Degrader-1为一种高效PROTACSOS1降解剂，DC50值为98.4 nM。此化合物在含有各类KRAS突变的癌细胞中展现出了抗增殖活性，证明了其抗肿瘤作用及低毒性特性。

PROTACPTK6 ligand-1是用于合成BTK激酶抑制剂的中间体，也可作为ARD-61合成的原料。

SMARCA-BD ligand 1 hydrochloride forProtac是一种基于PROTAC技术的化合物，能够与BAF ATPase亚基SMARCA2结合，用于降解SMARCA2。

PROTAC CDK4 6 degrader 1（Compound 7f）作为一种针对CDK4和CDK6的双重降解剂, 其DC50值分别为10.5 nM和2.5 nM。该化合物能显著抑制Jurkat细胞的增殖，其中IC50为0.18 μM，能够在G1期阻断细胞周期，并引发细胞凋亡（apoptosis）。此外，化合物的结构中包括三种配体，分别用不同颜色标记：靶蛋白配体YY173（Pink），连接子（Black），以及E3 ligase配体（Blue）。

PROTACAR AR-V7 degrader-1 (27c) 作为AR与AR-V7的双效PROTAC降解剂，显示出DC50值为2.67 μM和2.64 μM。此外，该化合物具备诱导凋亡的功能 (Red: AR拮抗剂; Blue: E3 连接酶配体; Black: linker)。

PROTACATR degrader-1 (compound ZS-7) 作为一种针对共济失调毛细血管扩张症和Rad3相关 (ATR) 的有效PROTAC降解剂，展现出了DC50为0.53μM的强效活性。此化合物在癌症研究领域扮演着关键角色。

PROTACBcI-2 BcI-xI Degrader-1 (15) 是一种用于降解BcI-2 BcI-xI的PROTAC降解剂 (Red: BcI-2 BcI-xI inhibitor, black: linker, Blue: E3 ligase ligand)。

PROTACHsp90α degrader 1 (Compound X10g) 是一款选择性的PROTACHsp90α降解剂，专用于乳腺癌细胞研究。它对MDA-MB-231、MDA-MB-468、MCF-7、及MX-1等乳腺癌细胞系表现出显著的增殖抑制作用，其IC50s值分别为51.48 μM、16.46 μM、8.93 μM、和11.95 μM。

BCL6PROTAC1 是一种选择性的 B 细胞淋巴瘤 6 (BCL6)PROTAC。BCL6PROTAC1 抑制 BCL6 细胞报告，IC50值为 8.8 µM。BCL6PROTAC1 在弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞系中显著降解 BCL6。BCL6PROTAC1 可用于肿瘤相关研究。

PROTACSTINGDegrader-1 (Compound SP23) 是一种STINGPROTAC 降解剂，其DC50为 3.2 μM。PROTACSTINGDegrader-1 具有抗炎活性。

PROTACEZH2 Degrader-1 (Compound 150d)是高效的PROTACEZH2降解剂，能够抑制EZH2甲基转移酶的活性，其IC50值为2.7 nM。由于EZH2在许多肿瘤的发生及进展中具有关键作用，这种化合物的研发具有重要意义。

PROTACAxl Degrader 1 是一种有效的选择性PROTACAxl 降解剂，IC50为 0.92 µM。PROTACAxl Degrader 1 显示出体外抗增殖活性、抗迁移活性。PROTACAxl Degrader 1 诱导巨泡式细胞死亡。

PROTACPARP EGFR ligand 1 是一种活性化合物，可通过蛋白水解靶向嵌合体（PROTAC）技术用于合成双 PARPEGFR 降解剂的合成。