t-20

Antiparasitic Agent-20 (Compound 1p) exhibits broad-spectrum activity as a parasitic inhibitor, demonstrating efficacy against T. brucei and T. cruzi with EC50 values of 0.09 µM and 14.1 µM, respectively [1].

(Rac)-ABT-202 dihydrochloride is a racemate of ABT-202, a nicotinic acetylcholine receptor (nAChRs) agonist used as an analgesic.

SNT-207707 is a potent, selective and orally active antagonist of melanocortin MC-4 receptor(IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor).

SNT-207858 free base is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor(IC50 of 22 nM (binding) and 11 nM (function), on the MC-4 receptor).

SNT-207858 is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.

68Ga-DOTA-NT-20.3 is an analogue of neurotensin (NTS) and acts as a ligand for 68Ga ions. In PET imaging, it demonstrates rapid tumor uptake and high contrast between tumor and background, along with fast clearance from the blood and moderate accumulation in the kidneys. Its pharmacokinetic and biodistribution properties are advantageous, producing high-quality PET images in mice with subcutaneous or orthotopic human pancreatic cancer xenografts. 68Ga-DOTA-NT-20.3 specifically binds to NTSR1 on pancreatic cancer cells and outperforms 18F-FDG in PET detection of adenocarcinoma.

Antioxidant agent-20 (Compound 3d) exhibits potent anti-inflammatory and antioxidant activities. It reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 demonstrates photoprotective effects on UVB-exposed human skin keratinocytes (HaCaT) (IC50=5.13 µM) by activating Nrf2 HO-1 signaling and inhibiting the NF-κB pathway.

ACT-209905 is an agonist of S1P1 receptor.

ABT-202 is a drug developed by Abbott that acts as an agonist for the nerve's nicotinic acetylcholine receptor and has been studied as a painkiller.

Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. 20(S)-hydroxy Cholesterol (20(S)-OHC) is an oxysterol which binds SMO and activates hedgehog signaling (EC50 = 3 μM), and this activation is selective for the nat-20(S)-OHC enantiomer. Nat-20(S)-OHC synergizes with the SMO agonist SAG, suggesting an allosteric effect. Nat-20(S)-yne is a form of nat-20(S)-OHC with a terminal alkyne group, which can be used in linking reactions known as click chemistry. Click chemistry involves highly dependable and specific azide-alkyne bioconjugation reactions and can be used to capture or immobilize bioactive molecules. Thus, nat-20(S)-yne has been conjugated with magnetic beads to demonstrate that nat-20(S)-OHC directly binds SMO.

Antitubercular agent-20 is an orally active antitubercular agent. agent-20 showed low cytotoxicity and good tolerability in BALB c mice.

Antiproliferative Agent-20 is a potent, orally active anticancer compound exhibiting both antiproliferative and anti-angiogenic activities.

STING agonist-20, a potent agonist utilized in the synthesis of XMT-2056, serves as a vaccine adjuvant for cancer and various inflammatory immune diseases research.

STING agonist-20-Ala-amide-PEG2-C2-NH2, an active scaffolding molecule, engages the stimulator of interferon genes (STING) pathway and is used in the synthesis of immune-stimulating antibody conjugates (ISAC), particularly in cancer research [1].

STING Agonist-20-Ala-amide-PEG2-C2-NH2 (Compound 30b) TFA, an active compound that interacts with the stimulator of interferon genes (STING), is utilized in the synthesis of immune-stimulating antibody conjugates (ISAC). This compound is also employed in cancer research [1].

JET-209 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades CBP p300, exhibiting half-maximal degradation concentration (DC50) values of 0.05 nM for CBP and 0.2 nM for p300. The compound comprises lenalidomide (the cereblon ligand), a connecting linker, and GNE-207 (the bromodomain inhibitor). JET-209 is utilized in cancer research [1].

Antileishmanial agent-20 exhibits selectivity against the Leishmania parasite, with IC50 values of 2.8 μM for L. infantum and 0.2 μM for L. braziliensis. It is a potential research tool for studying these parasites [1].

Tet-20, a synthetic cathelicidin-derived peptide with biological activity, has been evaluated for its efficacy as an infection-resistant coating on medical devices. Upon surface tethering to implants, Tet-20 demonstrates broad-spectrum antimicrobial properties, inhibits biofilm formation, and maintains non-toxicity to eukaryotic cells both in vitro and in vivo.

MAIT-203, a cyclopentyalanin-derived peptidomimetic, effectively disrupts the interaction between adenomatous polyposis coli (APC) and Asef (RhoGEF4), without affecting APC-Sam68 or APC-striatin interactions. It binds to APC-ARM domains with a K i of 0.015 μM and a K d of 0.036 μM, notably inhibiting the migration and invasion of colorectal cancer cells.

3β-Hydroxytaraxast-20-en-16-one is a natural compound isolated from a eucalyptol alcohol extract [1].

OAT-2068 is a potent and selective inhibitor of mouse chitotriosidase (CHIT1) and displays a remarkable 143-fold mCHIT1 vs. mAMCase selectivity.

BisMalt-20 is a useful organic compound for research related to life sciences. The catalog number is TF0097 and the CAS number is 1423237-53-9.

MAIT-203 acetate is a cyclopentylglycine-derived peptidomimetic that effectively inhibits the interaction between adenomatous polyposis coli (APC) and Asef (RhoGEF4), while not affecting the APC-Sam68 or APC-striatin interactions. It binds to APC-ARM with a Ki of 0.015 μM and a Kd of 0.036 μM, significantly impeding the migration and invasion of colorectal cancer cells.

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).