a-196

A-196 is a potent and selective inhibitor of SUV420h1 and SUV420h2, with IC50 values of 0.025 μM and 0.144 μM, respectively; it is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.

Surfactant protein A (SP-A) (196-215) is a synthetic peptide derived from the C-terminal carbohydrate recognition domain of human SP-A, specifically amino acids 196-215. This peptide suppresses LPS-induced TNF-α release in JAWSII mouse dendritic cells at 1 and 10 µM concentrations and promotes phagocytosis of P. aeruginosa at a 75 µM concentration. Furthermore, intratracheal administration of SP-A (196-215) at a dose of 50 µg per animal reduces disease severity and lung colony-forming units in mice infected with P. aeruginosa.

Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor, suppressing the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM, a hDHFR IC50 of 308 ± 71 nM, and a hDHFR to TgDHFR selectivity ratio of 196.

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker [IC50: 196 nM].

EM12-FS is a cereblon (CRBN) ligand that binds to CRBN at His353 and acts as a molecular glue degrader of NTAQ1. It has a half-life of 196 minutes in human plasma.

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

D-threo-PPMP is a glucosylceramide (GlyCer) synthetase inhibitor.1,2It is the active enanantiomer and enzymatic inhibitory component of the racemic DL-threo-PPMP . In MDCK kidney epithelial cells, D-threo-PPMP induces a 70% reduction in cell growthin vitroat 20 μM and significantly inhibits DNA synthesis at 3 μM.3[Matreya, LLC. Catalog No. 1865] 1.Shen, W., Henry, A.G., Paumier, K.L., et al.Inhibition of glucosylceramide synthase stimulates autophagy flux in neuronsJ. Neurochem.129(5)884-894(2014) 2.Lee, L., Abe, A., and Shayman, J.A.Improved inhibitors of glucosylceramide synthaseJ. Biol. Chem.274(21)14662-14669(1999) 3.Abe, A., Inokuchi, J.-i., Jimbo, M., et al.Improved inhibitors of glucosylceramide synthaseJ. Biochem.111(2)191-196(1992)

ICRF-196 is a Topoisomerase II Inhibitor and antineoplastic agent.

Amubarvimab (BRII-196) is a humanized recombinant antibody targeting the spike protein of SARS-CoV-2, with antiviral activity, used in studies of COVID-19 infection.

5-HT2A&5-HT2C agonist-1 (Example 2) is a dual-acting agent targeting 5-HT2A and 5-HT2C receptors with IC50 values of 196 nM and 0.9 nM, respectively. It is applicable in studying central nervous system disorders, including depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, post-traumatic stress disorder (PTSD), and seizure disorders [1].

Colestilan (MCI-196), a non-absorbable, non-calcium-based phosphate binder and anion exchange resin, exhibits oral activity and is utilized in the study of hypercholesterolemia [1] [2].

VHL Ligand 14 (Compound 11), a VHL ligand engineered for creating PROTAC estrogen receptor α (ERα) degraders, exhibits a binding affinity with an IC50 of 196 nM [1].

Acalabrutinib-d4 is a deuterated compound of Acalabrutinib. Acalabrutinib has a CAS number of 1420477-60-6. Acalabrutinib, also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.