homology-2

Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and exhibit synergy with the anti-cancer drug doxorubicin against breast cancer cells.

SMIFH2 is formin homology 2 (FH2) domains inhibitor.

2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor that covalently blocks the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with a Ki value of 43 μM and PTP1B with a Ki value of 42 μM [1]. SHP-1 and PTP1B both have known roles in regulating insulin signaling as well as myeloid and lymphoid cell differentiation, making inhibitors of these phosphatases of interest in diabetes, cancer, allergy, and inflammation research [2].

PTP inhibitor 1 is an inhibitor of cell-permeable protein tyrosine phosphatase (PTP) that covalently binds the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)),with Ki of128 μM.

NSC117079 is a novel PHLPP1/2 (Pleckstrin homology domain and leucine rich repeat protein phosphatase) inhibitor that activates neuronal AKT and ameliorates staurosporine-induced cell death in neurons.

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

Bragsin2 (6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one) is a hydration-resistant cell penetrant, selective and non-competitive inhibitor of Afr guanine nucleotide exchange factor BRAG2 that inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin2 binds at the interface between the pleckstrin homology domain of BRAG2 and the lipid bilayer, leading BRAG2 unable to activate lipidated Arf GTPase.

YTHDF2-IN-1 (Compound CK-75) is an inhibitor of YT521-B homology domain family 2 (YTHDF2) with a dissociation constant (Kd) of 26.2 μM, and it effectively blocks the interaction between YTHDF2 and m6A RNA. It suppresses colony formation in JAR cells and exhibits antiproliferative activity in various cancer cell lines, with an IC50 in the micromolar range. Additionally, YTHDF2-IN-1 induces apoptosis in K562 cells and causes cell cycle arrest at the G0/G1 phase.

SHP2-IN-28 (Compound 7188-0011) is an inhibitor of Src homology 2-containing protein tyrosine phosphatase 2 (SHP2) with an IC50 of 54.31 μM. It exerts its inhibitory effect by binding to the allosteric site of SHP2, displaying high selectivity.

SHP2-IN-42 is an inhibitor of the phosphatase containing the Src homology 2 domain (SHP2), with an IC50 of 15 nM. It inhibits cell proliferation, induces apoptosis, and causes G1 phase cell cycle arrest. SHP2-IN-42 is applicable in cancer research, including studies on acute myeloid leukemia (AML).

CHS-111 is a benzyl indazole compound that inhibits superoxide anion (O(2)(-)) generation and reduces fMLP-stimulated PLD activity (IC(50) 3.9±1.2μM). It inhibits the interaction of PLD1 with ADP-ribosylation factor (Arf) 6 and Ras homology (Rho) A, and reduces the membrane recruitment of RhoA in fMLP-stimulated cells.

1-O-Octadecyl-2-O-methyl-sn-glycerol is a metabolite of a phosphotidylinositol ether lipid analog (PIA). PIAs are known to target the pleckstrin homology domain of the serine/threonine kinase Akt and to induce apoptosis in cancer cell lines with high levels of endogenous Akt activity.

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3, also known as PIP3, is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. PIP3 can serve as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking. PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) is a synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacylglycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog give it different physical properties from naturally-occurring PIP3, including higher solubility in aqueous media.

EPQpYEEIPIYL, a phosphopeptide, is a ligand for the Src homology 2 (SH2) domain, activating Src family members such as Lck, Hck, and Fyn through binding interactions with SH2 domains.

Migoprotafib (GDC-1971) is a potent and highly selective SHP2 (Src Homology-2 Domain-Containing Phosphatase 2) inhibitor for the study of advanced solid tumours.

Beinaglutide, a recombinant human GLP-1 (rhGLP-1) polypeptide, exhibits nearly complete homology with human GLP-1 (7–36). It demonstrates dose-dependent effects in improving glycemic control, reducing food intake, delaying gastric emptying, and promoting weight loss. This compound shows promise for research into overweight/obesity and nonalcoholic steatohepatitis (NASH) [1] [2].

Neuropeptide Y (2-36) (porcine) is a pig-sourced peptide closely resembling its rat and human counterparts with 97.14% homology. It acts as an agonist for rat neuropeptide receptors Y5, Y2, and Y1, with EC50 values of 1.2, 1.6, and 3.4 nM, respectively. This compound is utilized in research on obesity and eating disorders [1].

STAT6-IN-3 (Compound 18a) is an inhibitor of STAT6, targeting the Src Homology 2 (SH2) domain with an IC50 value of 44 nM. It is used in research on inflammatory disorders, such as asthma [1].

Sydowimide A is an effective inhibitor of phosphatase 1 containing the Src homology 2 domain (SHP1), T cell protein tyrosine phosphatase (TCPTP), and leukocyte common antigen (CD45) with IC50 values of 1.5, 2.4, and 18.83 μM, respectively.