insertion

Tuxobertinib (BDTX-189) 是一种高效可口服的选择性 EGFR 和 HER2变构突变抑制剂，具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的 KD 值分别为 0.2、0.76、13 和 1.2 nM。

Sunvozertinib (DZD9008) 是一种有效的 ErbBs 和 BTK 抑制剂，对EGFR、Her2和突变型表皮生长因子有抑制作用。 Sunvozertinib (DZD9008) 显示 EGFR 外显子 20 NPH 插入、EGFR 外显子 20 ASV 插入、EGFR L858R 和 T790M 突变以及 Her2 外显子 20 YVMA 和 EGFR WT A431 有抑制作用， IC50 分别为 20.4、20.4、1.1、7.5 和 80.4 nM 。

(S)-Sunvozertinib (DZD9008) 是 Sunvozertinib 的 S-对映体，能够抑制EGFR 外显子 20 NPH 和 ASV 插入、EGFR L858R/T790M 突变及 Her2 外显子 20 YVMA 插入，也能够抑制BTK。

GJ071 oxalate 是一种无义抑制剂。无义抑制剂（NonSups）诱导“读出”，即在提前终止密码子处选择近同源tRNA，并将相应的氨基酸插入新生多肽中。

Coralyne chloride 是一种具有强抗癌活性的原小檗碱。它可用于制备 Coralyne 衍生物，是一种基于荧光 DNA 的分子整流剂，通过位点特异性插入构建成 DNA 双链体。它可作为一种拓扑异构酶 I 毒性分子，诱导拓扑异构酶 I 介导 DNA 裂解。

CLIP 86-100 acetate(648881-58-7 free base) 这是称为 CLIP 的 II 类相关不变链肽的氨基酸 86 至 100 片段。主要组织相容性复合物 II 类分子显示外源蛋白的肽片段，以触发免疫系统的防御反应。在将外源肽插入结合槽之前，去除一个占位肽 CLIP。这是通过分子 DM 实现的，它被证明可以增加 CLIP 肽与 II 类的解离速率。

Ir(III) Octaethylporphine chloride作为一种合成卟啉，主要用途包括作为内分子C-H插入的强效催化剂。此外，Ir(III) Octaethylporphine chloride还参与初级醇的C-O键断裂反应。当与组氨酸功能化肽结合时，该化合物还能渗透细胞并感应细胞内O2浓度。

GJ-072 is a Nonsense suppressor. Nonsense suppressors (NonSups) induce “readthrough”, i.e., the selection of near cognate tRNAs at premature termination codons and insertion of the corresponding amino acid into nascent polypeptide.

EGFR-IN-99 (JBJ-03-142-02) 是一种 EGFR 和 HER2 Exon 20 插入突变抑制剂，具有抗增殖活性，可用于研究非小细胞肺癌 (NSCLC) 。

9(R)-HODE is one of several monohydroxylated products of linoleic acid. All known mammalian lipoxygenases appear to catalyze the oxygenation of arachidonic and linoleic acid to give products having strictly the (S) configuration at the site of oxygen insertion. However, both human umbilical vein endothelial cells and bovine aorta endothelial cells have been shown to produce 9(R)-HODE when incubated with linoleic acid. The physiological function of 9(R)-HODE and the enzyme that catalyzes its formation have not been determined.

1,2-Dipalmitoyl-13C-sn-glycero-3-PC is intended for use as an internal standard for the quantification of 1,2-dipalmitoyl-sn-glycero-3-PC by GC- or LC-MS. 1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.1,2,3,4 It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.3 Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.4 |1. Ege, C., and Lee, K.Y.C. Insertion of Alzheimer's Aβ40 peptide into lipid monolayers. Biophys. J. 87(3), 1732-1740 (2004).|2. Leekumjorn, S., and Sum, A.K. Molecular simulation study of structural and dynamic properties of mixed DPPC/DPPE bilayers. Biophys. J. 90(11), 3951-3965 (2006).|3. Kalra, V.K., Sikka, S.C., and Sethi, G.S. Transport of amino acids in γ-glutamyl transpeptidase-implanted human erythrocytes. J. Biol. Chem. 256(11), 5567-5571 (1981).|4. Uemura, A., Watarai, S., Iwasaki, T., et al. Induction of immune responses against glycosphingolipid antigens: Comparison of antibody responses in mice immunized with antigen associated with liposomes prepared from various phospholipids. J. Vet. Med. Sci. 67(12), 1197-1201 (2005).

GL0388 是一种Bax 激活剂，可导致 Bax 插入线粒体膜，从而诱导 Bax 介导的细胞凋亡。GL0388 在体内抑制乳腺癌异种移植的肿瘤生长，并且对多种癌细胞表现出抗增殖活性，IC50值为 0.299-1.57 μM。

WF-47-JS03 是选择性的、有效的、能够透过血脑屏障的 RET 激酶抑制剂，比对激酶插入域受体 (KDR) 的选择性高 500 多倍。WF-47-JS03 作用于转染 KIF5B-RET 的 Ba F3 细胞 (IC50: 1.7 nM) 和转染 CCDC6-RET 的 LC-2 ad 肺癌细胞 (IC50: 5.3 nM)。

LDC0496 是 EGFR 的有效抑制剂。LDC0496 能够显著抑制 EGFR 和 Her2 外显子 20 插入突变，并对野生型 EGFR 和激酶组内的选择性。

DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112 not only displayed a potent inhibitory activity against EGFRL858R T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib,against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate optimization yielded fourfold oral AUC better that afatinib along with F = 41.5%, an encouraging safety profile, and significant antitumor efficacy in in vivo xenograft models.

PUN-96956 is a novel BAM complex inhibitor, interfering with BamA-related processes and affect folding and insertion of OMPs. This product has no formal name. For the convenience of scientific communication, we named it by combining its InChi Key (3 letters from the first letter of each section) with the last 5 digit of its CAS#) according to MedKoo Chemical Nomenclature (https: www.medkoo.com page naming).

Biotin-TEG-ATFBA 作为点击化学试剂,具备全氟苯基叠氮基团.该化合物在光解后生成高度稳定的氮烯中间体,可通过中等至良好的产率进行插入和加成反应(非分子间重排).

CLIP (86-100) is amino acids 86 to 100 fragment of class II-associated invariant chain peptide called CLIP. The major histocompatibility complex class II molecule displays peptide fragments of foreign proteins to trigger a defensive reaction from the immune system. Before insertion of the foreign peptides into the binding groove, a place-holding peptide CLIP is removed. CLIP (86-100) is accomplished by the molecule DM, which is shown to increase the dissociation rate of a CLIP peptide from class II.

Cotransin 是一种 Sec61 易位抑制剂，能以信号序列辨别的方式阻止新生链插入 Sec61 易位通道中，通过抑制 VCAM-1 和 p-selectin 蛋白跨内质网 (ER) 膜的共翻译易位 (IC50=0.5-5 µM) 来选择性抑制这些蛋白的表达，有用于研究炎症及免疫的潜力。

3'-Amino-3'-dGTP tetrasodium 是一种 GTP 的变体，其结构在 GTP 的 C3 位置插入氨基酸。