b cell

Dacarbazine (DTIC-Dome) is an antineoplastic agent. It has significant activity against melanomas.

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19 0.96 μM).

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM 6 nM 8 nM 0.5 nM and 32 nM for JAK1 JAK2 JAK3 TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory and immunosuppressive properties that induces autophagy and inhibits LPS-induced inflammatory responses in macrophages.

Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib is an effective and orally active Bruton tyrosine kinase inhibitor (IC50: 1 nM). Remibrutinib has the potential for Chronic urticaria (CU) treatment.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

Ixabepilone (Azaepothilone B) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.

Wighteone (Erythrinin B) is a small molecule compound derived from Genista ephedroides with potential antifungal and anticancer activity against EGFR L858R T790M mutant non-small cell lung cancer.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

Lagociclovir (MIV-210), a nucleoside analogue, is an antiviral compound available for the treatment of HBV82 that inhibits the replication of wild-type hepatitis B virus (HBV) in human hepatocellular carcinoma cell lines that permanently express HBV.

Mepazine (Pecazine) is a potent and selective inhibitor of MALT1, inhibiting GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 μM and 0.42 μM, respectively. Mepazine enhances apoptosis and impacts cell viability.

Calpain Inhibitor XII (Z-L-Nva-CONH-CH2-2-Py) is a selective and potent inhibitor of calpain I, inhibits calpain II and cathepsin B. Calpain Inhibitor XII shows antiviral activity against coronavirus in cell culture.

Eckol inhibits ultraviolet B-induced cell damage by a decrease in oxidative stress in human keratinocytes.This compound is unstable in powder form and other related salt forms are recommended.

CT-2584 is an anticancer agent that inhibits phospholipid signaling and kills tumor cells through the production of reactive oxygen intermediates. CT-2584 reduces NKEF-B expression in several tumor cell types. CT-2584 reduced tumor growth in SCID mice by causing shunting of ab initio phospholipid biosynthesis from phosphatidylcholine (PC) to phosphatidylinositol (PI) via PA.

HBF-0259 is an inhibitors of hepatitis B virus surface antigen (HBsAg) secretion with an EC50 of 11.3 μM and a CC50 value of >50 μM in HepG2.2.15 cells. HBF-0259 had a EC50 of approximately 1.5 microM in a secondary, HBV-expressing cell line, with a concentration that exhibited 50% cytotoxicity of >50 microM. The equilibrium concentration of HBF-0259 in aqueous solution at physiological pH was 15 to 16 microM; the selective index was thus >9.

BTK inhibitor 1 (Compound 27) is a BTK inhibitor (IC50: 0.11 nM) with an inhibitory effect on B-cell activation in hWB with an IC50 of 2 nM.

QL-X-138 is a potent and selective BTK and MNK dual kinase inhibitor that binds covalently to BTK and non-covalently to MNK. The IC50 values of QL-X-138 are 9.4 nM for BTK, 107.4 nM for MNK1, 26 nM for MNK2, and 3.5 μM against Dengue 2. QL-X-138 is used in the study of B-cell malignancies and B-cell malignant tumors.

BMS-903452 is a potent and selective GPR119 agonist with an EC50 of 14 nM, indicated for the treatment of acute and chronic rodent diabetes. GPR119 is mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. BMS-903452 shows no significant inhibitory effect on 9 cytochrome P450 enzymes (IC50 > 40 μM), does not activate PXR (EC50 > 50 μM), and is not toxic to liver (HEPG2) cell lines.

Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.

TCIP 1 is a small molecule in the category of transcriptional epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].