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].

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 (56-87) (human) TFA, a peptide derived from the human Klotho protein, disrupts TGF-β signaling through binding interactions with TGF-β receptor type 1 (TGFBR1) and TGF-β receptor type 2 (TGFBR2), with Kd values of 1.41 and 14.6 µM, respectively. Preincubation with Klotho-derived Peptide 1 (56-87) (human) TFA at 10 µg/mL inhibits TGF-β-induced increases in fibronectin and α-smooth muscle actin (α-SMA) expression in NRK-49F rat fibroblasts. In vivo investigations demonstrate that Klotho-derived Peptide 1 (56-87) (human) TFA, administered at 1 mg/kg per day, preferentially accumulates in damaged kidneys and significantly reduces serum creatinine and blood urea nitrogen levels while decreasing renal fibrosis in mouse models of unilateral ureteral obstruction (UUO) and unilateral ischemia-reperfusion injury-induced renal fibrosis. Klotho-derived Peptide 1 (56-87) (human) TFA is therefore valuable for investigations involving renal fibrosis, TGF-β signaling modulation, and kidney injury-associated molecular pathways.

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.

Tubulin-IN-56 is a tubulin inhibitor with cytotoxic effects on colon cancer cell lines (LS180, HCT116, SW620, LoVo). It downregulates βIII-tubulin expression and upregulates βIVa-tubulin expression within these cell lines. Additionally, Tubulin-IN-56 inhibits cell invasiveness and elevates intracellular ROS levels in colon cancer cell lines. This compound is applicable in colon cancer research.

Z56-L23 is a drug-linker conjugate used in antibody-drug conjugates (ADC), comprised of a linker and a Ras inhibitor. It is applicable in cancer research, including studies on pancreatic cancer.

Z56 is a Ras protein inhibitor that can be utilized in cancer research, including studies on pancreatic cancer.

Mel56 is a melanin precursor analogue that enhances melanin production in human melanoma cells. It exhibits cytotoxicity towards cancer cells and induces apoptosis (apoptosis) in melanoma cells. Mel56 is valuable for melanoma research.

Antitubercular agent-56, a derivative of Questiomycin A, is a potent antitubercular compound effective when taken orally. By inhibiting FabD (Kd = 9.39 μM; IC50 = 49.60 μM), it compromises the cell membrane integrity of Mycobacterium tuberculosis. Antitubercular agent-56 demonstrates significant intracellular antimycobacterial activity against Mycobacterium tuberculosis (MTB) and drug-resistant MTB both in vitro and in vivo, making it valuable for tuberculosis (TB) research.

Apoptosis inducer56 is an apoptosis inducer that binds to DNA minor grooves, causing DNA damage through the upregulation of γH2AX and p-ATM expression. This compound induces endogenous apoptosis by causing S phase cell cycle arrest and increasing the p53 and Bax/Bcl-2 ratios, as well as promoting caspase-7 cleavage. It demonstrates higher selectivity for cancer cells compared to normal breast epithelial cells and is useful in breast cancer research.