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.

Denintuzumab-MMAF, an ADC, combines a CD19-directed antibody with McMMAF and is utilized in researching acute lymphoblastic leukemia.

Anti-Human/Mouse CD95 Antibody (HFE7A) is a monoclonal inhibitory antibody that recognizes both human and mouse CD95 (Fas) and induces apoptosis in thymocytes.

Anti-Human/Mouse LY6E Antibody (9B12) is a monoclonal inhibitory antibody against human and mouse LY6E, applicable to cancer research.

Anti-Human/Mouse/Monkey CLDN18.2 Antibody (25C7A5-HZ1) is an inhibitory antibody that targets Claudin-18.2 in humans, mice, and monkeys, and is suitable for use in cancer-related research.

Anti-Human/Mouse/Monkey TL1A Antibody (1D1) is a monoclonal inhibitory antibody that blocks the TL1A/DR3 pathway, inhibits abnormal PI3K/AKT activation, corrects Th1/Th17 imbalance, and reduces pulmonary granuloma formation.

Anti-Human/Rat VEGF Antibody (A.4.6.1) is a monoclonal inhibitory antibody targeting human and rat VEGF, applicable to angiogenesis research.

Anti-Mouse VEGF Antibody (G6-31) is a monoclonal inhibitory antibody targeting mouse VEGF, applicable to angiogenesis-related research.

Anti-Mouse DDR2 Antibody (DAB0065) is a monoclonal inhibitory antibody targeting mouse DDR2, applicable to tumor microenvironment-related research.

Anti-Human CD64 Antibody (H22) is a monoclonal inhibitory antibody targeting human CD64 protein, which can be used in immunology-related research.

ADC Control Human IgG1 kappa-vcMMAE is a human monoclonal antibody and an isotype control for Human IgG1 kappa-vcMMAE that inhibits tubulin polymerization.

Anti-Mouse CD37 Antibody (252-3) is a monoclonal inhibitory antibody against mouse CD37, suitable for use in life science research.

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.

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.

JP-2-196 functions as a molecular glue handle, engaging with E3 ubiquitin ligases such as RNF126, LRSAM1, RNF40, MID2, RNF219, and RNF14 in an immunoprecipitation (IP) assay at a concentration of 10 µM. Additionally, JP-2-196 is utilized in the creation of diverse molecular glue degraders.

Antibacterialagent 196 (compound 6b) is a coumarin derivative featuring an oxime ether structure, and it demonstrates notable antifungal activity, with an EC50 value of 0.46 μg/mL against Rhizoctonia solani.

JP-2-196 (TFA) is a molecular glue handle that binds in vitro with E3 ubiquitin ligases [RNF126, LRSAM1, RNF40, MID2, and RNF14]. It is applicable in the synthesis of molecular glue degraders.

JP-2-196 hydrochloride is a covalent molecular glue degrader that specifically targets RNF126. It facilitates the formation of a ternary complex between RNF126 and target proteins (e.g., BRD4, AR-V7), promoting their ubiquitination and proteasomal degradation. JP-2-196 hydrochloride is being explored for potential applications in cancer research, such as prostate cancer and leukemia.

Wee1/HDAC-IN-1 is a dual inhibitor targeting Wee1 and HDACs, exhibiting IC50 values of 1.2 nM for Wee1, 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. It shows potent antiproliferative activity against MV4-11 cells, with an IC50 of 0.076 μM. This compound selectively binds to the catalytic sites of Wee1 and HDACs, disrupting DNA damage repair pathways and inducing apoptosis in MV4-11 cells (apoptosis). Wee1/HDAC-IN-1 is applicable for studying acute myeloid leukemia.

CRBN ligand-196 is a ligand for the E3 ubiquitin ligase cereblon (CRBN) and is used to recruit cereblon proteins. This compound can be linked to a target protein ligand via a linker to form a PROTAC.

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.

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)