insertion

Sunvozertinib (DZD9008) is a potent ErbBs and BTK inhibitor with inhibitory effects on EGFR, Her2, and mutant epidermal growth factor. It inhibits EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutation, and Her2 exon 20 YVMA and EGFR WT A431, with IC50 values of 20.4, 20.4, 1.1, 7.5, and 80.4 nM, respectively.

EGFR-IN-99 (JBJ-03-142-02) is an EGFR and HER2 Exon 20 insertion mutation inhibitor with antiproliferative activity for the study of non-small cell lung cancer (NSCLC).

GJ071 oxalate 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.

CLIP 86-100 acetate(648881-58-7 free base) 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 acetate(648881-58-7 free base) is accomplished by the molecule DM, which is shown to increase the dissociation rate of a CLIP peptide from class II.

Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, with KDs of 0.2, 0.76, 13, and 1.2 nM for EGFR, HER2, BLK, and RIPK2, respectively, and exhibits anticancer activity.

Coralyne chloride is a protoberberine with strong anticancer activity. It can be used to prepare Coralyne derivatives, a fluorescent DNA-based molecular rectifier built into DNA duplexes through site-specific insertion. It acts as a topoisomerase I toxic molecule, inducing topoisomerase I-mediated DNA cleavage.

WF-47-JS03 is a selective and potent inhibitor of RET kinase that crosses the blood-brain barrier and is more than 500-fold more selective for the kinase insertion domain receptor (KDR).WF-47-JS03 acts on Ba/F3 cells transfected with KIF5B-RET (IC50: 1.7 nM) and LC-2/ad lung cancer cells transfected with CCDC6-RET (IC50: 5.3 nM). cells (IC50: 5.3 nM).

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.

LDC0496 is a potent inhibitor of EGFR. LDC0496 significantly inhibits EGFR and Her2 exon 20 insertion mutations, and is selective for wild-type EGFR and kinase within the kinome.

GL0388 is a Bax activator and leads to Bax insertion into mitochondrial membrane that induce Bax-mediated apoptosis. GL0388 inhibits tumor growth of breast cancer xenograft in vivo which also exhibits antiproliferative activities against a variety of cancer cells with IC50 values of 0.299-1.57 μM [1].

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.

Cotransin, a Sec61 translocation inhibitor, selectively prevents the stable insertion of certain nascent chains into the Sec61 translocation channel, exhibiting signal-sequence discrimination. This compound also inhibits the expression of VCAM-1 and p-selectin proteins by blocking their co-translational translocation across endoplasmic reticulum (ER) membranes (IC 50 =0.5-5 µM). Cotransin's role extends to potential applications in inflammation and immunity research [1] [2].

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).

(S)-Sunvozertinib (DZD9008) is a rationally designed selective, irreversible EGFR/HER2 inhibitor.

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).

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.

CLIP (86-100) is an amino acids 86 to 100 fragment of the class II-associated invariant chain peptide called CLIP. The major histocompatibility complex class II molecule displays peptide fragments of foreign proteins to trigger an immune response. Before foreign peptides bind, a place-holding CLIP peptide is removed by the molecule DM, which increases the dissociation rate of CLIP from class II.