I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation[1].
WHI-P97 is a rationally designed potent inhibitor of JAK-3.IC50 value:Target: JAK3Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal. WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose.
MK-0429 is a potent integrin antagonist with IC50s of 12.2 nM (α5β1 integrin) and 2.8 nM (αvβ3 integrin), respectively.
Epimedin K (Korepimedoside B), a flavonol glycoside, is isolated from the aerial parts of Epimedium koreanum Nakai. Epimedium koreanum Nakai is a famous Chinese herbal medicine for the research of impotence, osteoporosis, immune suppression and cardiovascular diseases[1][2].
MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.IC50 value: 0.11 uM [1]Target: MAPKAPK2(MK2) inhibitorMK2-IN-1 was profiled for kinase selectivity by screening against a broad panel of 150 protein kinases at a concentration of 10 μM, and only CK1γ3 was significantly inhibited at greater than 50%. MK2-IN-1 inhibited pro-inflammatory cytokine secretion from the human THP1 acute monocytic leukemia cell line, causing dose-dependent inhibition of LPS-stimulated TNFα and IL6 secretion. MK2-IN-1 also dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion from the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures. Of note, given its high degree of selectivity, our data suggest that MK2-IN-1 may be an excellent pharmacologic tool for specifically exploring and validating MK2 biology [3].
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2].
Flurandrenolone Acetate is a derivative of Flurandrenolide (HY-B1013). Flurandrenolone Acetate is a synthetic glucocorticoid steroid, can be used for the research of skin disorders such as eczema and psoriasis[1].
HPK1-IN-13 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-13 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 64) [1].
GW311616A(GW311616 Hcl) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.IC50 value: 22 nM [1]Target: neutrophil elastaseThe HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic.
MC-Val-D-Cit-PAB-PNP is a drug-linker-ligand conjugates. MC-Val-D-Cit-PAB-PNP can be used for researching cancer, autoimmune diseases and infectious diseases[1].
JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model[1].
Lanraplenib (GS-9876) is a highly selective and oral SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3].
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19[1][2][3][4][5].
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes[1]. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities[2].
AJ2-30 is a SLCl5A4 inhibitor. AJ2-30 inhibits TLR9-mediated B cell activation. AJ2-30 block endogenous NOD signaling in human and mouse macrophages. AJ2-30 can be used for research of inflammation[1].
6-trans-leukotriene B4 is a neutrophil chemotaxin in the guinea pig dermis[1].
DHODH-IN-14 (Compound 7l) is a hydroxyfurazan analog of A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for rat liver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis[1].
Bellidifolin is a xanthone isolated from the stems of Swertia punicea, with hepatoprotective, hypoglycemic, anti-oxidation, anti-inflammatory and antitumor activities[1][2][3]. Bellidifolin also acts as a viral protein R (Vpr) inhibitor[4].
Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
MLKL-IN-2 is a MLKL inhibitor extracted from patent WO2021224505A1, compound (i)[1].
Methylophiopogonone A, a homoisoflavonoid isolated from the tuberous roots of Ophiopogon japonicas, shows anti-inflammatory activity[1].
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor[1]. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies[2][3][4].
α-CGRP, rat, a neuropeptide (calcitonin gene-related peptide (CGRP)), is a potent vasodilator, with the potential in cardiovascular, pro-inflammatory and metabolic studies[1].
Dovramilast (CC-11050) is an oral phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast (CC-11050), as an adjunct, is used for the research of tuberculosis (TB)[1].
Wittifuran X is a 2-arylbenzofuran derivative, which can be isolated from the stem bark of Morus wittiorum[1].
FCPR03 is a novel potent, selective PDE4 inhibitor with IC50 of 60, 31 and 47 nM for PDE4CAT (PDE4 catalytic domain), PDE4B1 and PDE4D7, respectively; displays >2,000-fold selectivity over other PDEs; effectively increases the production of cAMP, promotes CREB phosphorylation, and inhibits NF-κB activation both in vitro and in vivo; displays anti-neuroinflammation potential, promising antidepressant-like effects in vivo.
Maraviroc-d6 (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].
LTD4 antagonist 1 is a potent, orally active antagonist of leukotriene D4 (LTD4) with a Ki of 0.57 nM.