ap1

AP-1 NF-κB activation inhibitor 1 是一种有效的 AP-1和 NF-κB 介导的转录激活抑制剂(IC50=1 μM)，不阻断 β-actin 启动子驱动的基础转录。AP-1 NF-κB activation inhibitor 1 对受刺激细胞中 IL-2和 IL-8的产生水平有相似的抑制作用。

AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.

B-AP15 (NSC-687852) 是 26S 蛋白酶体的去泛素化酶 Usp14 和 UCHL5 的选择性抑制剂。 它阻断 26S 蛋白酶体的去泛素化活性。

TAT-Gap19 acetate 是 connexin43 hemichannel (Cx43 HC) 的特异性抑制剂。 它穿过血脑屏障并减轻小鼠的肝纤维化。它不抑制相应的 Cx43 GJC。

AP1189 acetate 是黑皮质素 1 和黑皮质素 3 受体的偏向激动剂。

ERAP1-IN-2 (compound 3f) 作为endoplasmic reticulum aminopeptidase 1（ERAP1）的抑制剂，对hERAP1展示了1.72 μM的IC50值。

cIAP1 Ligand-Linker Conjugates 3 are chemical compounds comprising an IAP ligand designed specifically for the E3 ubiquitin ligase and a PROTAC linker. These conjugates, denoted as cIAP1 Ligand-Linker Conjugates 3, find utility in the design of SNIPERs, short for Specific and Non-genetic IAP-dependent Protein Erasers [1].

cIAP1 Ligand-Linker Conjugates 16 refers to a specific type of ligase ligand-linker conjugate, possessing the ability to engage with E3 ligases, which finds application in the synthesis of PROTACs.

CAP18 (rabbit) is a 37 amino acid antimicrobial peptide derived from rabbit granulocytes. It exhibits extensive antimicrobial activity against both Gram-positive (IC50, 130-200 nM) and Gram-negative (IC50, 20-100 nM) bacteria. Thus, CAP18 (rabbit) holds promise for the study and advancement of bacterial sepsis research.

cIAP1 Ligand-Linker Conjugates 11 Hydrochloride is a chemical compound consisting of an IAP ligand that targets the E3 ubiquitin ligase, along with a PROTAC linker. It is primarily utilized in the development of SNIPERs, a molecular tool for targeted protein degradation[1].

Gap19 TFA is a peptide derived from nine amino acids of Cx43 cytoplasmic ring (CL), an effective, selective connexin 43 (Cx43) half-channel blocker.

cIAP1 ligand 2, a derivative of LCL161, is an IAP ligand that can be connected to the ABL ligand for protein via a linker, resulting in the formation of SNIPER.

cIAP1 Ligand-Linker Conjugates 15 hydrochloride is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is useful in the development of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 7 is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker. It is utilized in the design of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 1 is composed of an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 1, is particularly useful in the development of SNIPERs[1].

TRAP1-IN-1（化合物35）是一种高效、具有高选择性的TRAP1抑制剂，其中TRAP1为Hsp90蛋白质家族中的一种线粒体同源体。该抑制剂对TRAP1的选择性优于Grp94超过250倍，能够破坏TRAP1四聚体的稳定性，并诱导下游蛋白质的降解。此外，TRAP1-IN-1能够抑制线粒体氧化磷酸化复合体（OXPHOS），破坏线粒体膜电位，并促进糖酵解过程。

TAT-Gap19 TFA为Cx模拟肽，特异性抑制connexin43半通道(Cx43 HC)，但不影响相应的Cx43 GJC。该化合物具备透过血脑屏障功能，能够减轻小鼠肝纤维化。

XIAP cIAP1 antagonist-1 是一种有效的、口服具有活力的 XIAP cIAP1 拮抗剂，能够作用于 XIAP (EC50: 5.1 nM) 和 cIAP1 (EC50: 0.32 nM)。XIAP cIAP1 antagonist-1 能够剂量依赖性地抑制体内肿瘤生长。

Keap1-Nrf2-IN-23（compound 56）作为Keap1–Nrf2 PPI的抑制剂表现出色，具体抑制浓度为IC50=16.0 nM。该化合物与Keap1的结合亲和力强，Kd值仅为3.07 nM。此外，Keap1-Nrf2-IN-23还具备良好的口服活性。

Keap1-Nrf2-IN-25 (Compound 19) 是一种强效的Keap1-Nrf2抑制剂，IC50值为0.55 μM，并展现出与Keap1的结合亲和力，Kd为0.50 μM。Keap1-Nrf2-IN-25 能激活Nrf2，降低ROS及促炎细胞因子如IL-1β和IL-6的水平，对DSS诱导的结肠炎具有保护作用。

cIAP1 Ligand-Linker Conjugates 9 feature an IAP ligand specifically targeting the E3 ubiquitin ligase, along with a PROTAC linker. It is valuable tools for developing SNIPERs[1].

Cx43 hemichannel blocker (IC50 ~7 μM). No significant affinity for gap junctions or Panx1 channels. N-terminal transactivator of transcription (TAT) motif promotes membrane permeability and increases inhibitory effect of Gap19. Active in vivo. Brain penet

ERAP1-in-1 是一种内质网氨基肽酶 1 (ERAP1) 抑制剂，能竞争性地抑制 ERAP1 对代表性生物底物九聚物肽的作用。

Gap19 是一种衍生自 Cx43 细胞质环九个氨基酸的肽，是选择性连接蛋白 43 半通道阻滞剂。它可以防止 C 末端与 CL 的分子内相互作用，具有保护心肌作用。