at 56

AT56, a specific inhibitor of prostaglandin D2 synthase enzymatic activity, blunted adipogenic aldosterone effects.

NF-56-EJ40 hydrochloride is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 hydrochloride has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.

Rac1 Inhibitor W56 acetate(1095179-01-3 free base) is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 acetate(1095179-01-3 free base) selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

26RFa acetate is a hypothalamic neuropeptide with orexigenic activity in mammals[1].

Compound 6317-56-2, with CAS No. 6317-56-2, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound 6317-56-2 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

Compound 63089-56-5, with CAS No. 63089-56-5, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound 63089-56-5 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

Compound 622864-56-6, with CAS No. 622864-56-6, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound 622864-56-6 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor, with an IC50 of 1-5 μM for PAD4. Compared with Cl-amidine, YW3-56 shows >60-fold increase in cell growth inhibition efficacy (IC50 about 2.5 μM) but only 5-fold increase in PAD4 inhibition (IC sub>50 about 1-5 μM). At 2-4 μM concentrations, YW3-56 displays mainly cytostatic effects by slowing cell division, whereas at higher concentrations, it exerts cytotoxic effects by altering cell morphology and killing cells[1]. [1]. Wang Y, et al. Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and t he mammalian target of rapamycin complex 1 activity. J Biol Chem. 2012 Jul 27;287(31):25941-53.

Anticancer agent 56 (compound 4d) is a powerful anti-cancer compound with favorable drug-like properties, showing significant anticancer activity against multiple cancer cell lines with an IC50 value of less than 3 μM. It exerts its effects by causing cell cycle arrest at the G2/M phase and activating the mitochondrial apoptosis pathway, inducing the accumulation of reactive oxygen species (ROS), upregulating BAX, downregulating Bcl-2, and triggering the activation of caspases 3, 7, and 9 [1].

Klotho-derived peptide 1 (KP1) (56-87), a peptide originating from the human Klotho protein, disrupts TGF-β signaling by binding to TGF-β receptor types 1 and 2 (TGFBR1 and TGFBR2; Kds = 1.41 and 14.6 µM, respectively). Preincubation with KP1 at a concentration of 10 µg/ml hinders the TGF-β-induced escalation of fibronectin and α-smooth muscle actin (α-SMA) levels in NRK-49F rat fibroblasts. Furthermore, in vivo studies reveal that KP1, administered at 1 mg/kg per day, preferentially accumulates in damaged kidneys, leading to significant reductions in serum creatinine and blood urea nitrogen levels, indicators of improved kidney function. Additionally, it decreases kidney fibrosis in mouse models of unilateral ureteral obstruction (UUO) and unilateral ischemia-reperfusion injury-induced renal fibrosis.

NF-56-EJ40 is an effective and highly selective antagonist of human SUCNR1 with an IC50 of 25 nM and a Ki of 33 nM.

UP202-56 is an adenosinergic agonist and is an adenosine analog.

Antiproliferative agent-56 (Compound 31) is an antimalarial agent that inhibits the Pf3D7 strain of the malaria parasite Plasmodium falciparum with an IC50 of >12.5 (48h) and 0.03 μM (98h), displaying slow-acting characteristics.

VEGFR-2-IN-56 (compound 12e) exhibits the strongest inhibition activity against VEGFR-2, with an IC50 value of 45.9 nM.

NLRP3-IN-56 (compound 062) is an inhibitor of NLRP3. It effectively suppresses the secretion of IL-1β in THP-1 cells, demonstrating an IC50 of 9.7 nM. NLRP3-IN-56 is useful for research into NLRP3-mediated symptoms and/or diseases.

HPK1-IN-56 (Compound A29) is an HPK1 inhibitor with an IC50 of 2.70 nM. It inhibits downstream p-SLP76 in Jurkat T cells with an IC50 of 8.1 nM. Additionally, HPK1-IN-56 induces IL-2 production in human PBMCs. This compound exhibits anticancer properties, enhancing T cell cytotoxicity and the antitumor efficacy of anti-PD-1 antibodies.

E3 Ligase Ligand 56 is a ligand for the E3 ligase Cereblon, and it can be utilized in the synthesis of [PROTACCDK9degrader-11].

PI3K-IN-56 (Compound 1) is an orally active, potent, and selective irreversible inhibitor of phosphoinositide 3-kinase (PI3K). It irreversibly blocks the production of phosphatidylinositol-3,4,5-trisphosphate (PIP3) and the downstream AKT signaling pathway. PI3K-IN-56 holds promise for research in PI3Kα-driven cancers, such as breast and ovarian cancer.

HDAC6-IN-56 (compound 18d) is an inhibitor of HDAC6, with an IC50 of 1.3 nM. This compound can inhibit the S phase and induce apoptosis in HCT-116 colon cancer cells.

AChe-IN-56 is an orally active acetylcholinesterase (AChE) inhibitor with neuroprotective properties.

COX-2-IN-56 (example 6) is a selective COX-2 inhibitor that shows no significant inhibitory effect on COX-1. It can be utilized in research on COX-2-dependent conditions such as inflammation.

ABD56 inhibits osteoclast formation and activity in vitro and in vivo.

EMI56, a derivative of EMI1, exhibits enhanced potency against mutant EGFR compared to EMI1. Additionally, EMI56 effectively inhibits EGFR triple mutants[1].

YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg/kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and the mammalian target of rapamycin complex 1 activityThe Journal of Biological Chemisty287(31)25941-25952(2012) 2.Wang, S., Chen, X.A., Hu, J., et al.ATF4 gene network mediates cellular response to the anticancer PAD inhibitor YW3-56 in triple-negative breast cancer cellsMol. Cancer Ther.14(4)877-888(2015)