AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC50 of 7 nM.
Pildralazine (Propyldazine) is a hydralazinelike antihypertensive vasodilator containing a free hydrazine group. Pildralazine is orally active, has no significant carcinogenicity in mice model[1][2].
Rosmarinic acid (RA) is a widespread phenolic ester compound in the plants. Rosmarinic acid inhibits MAO-A, MAO-B and COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.
DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes[1][2].
Ganoderic acid S is a positional isomer of ganoderic acids, that can be isolated from the fermented mycelia of Ganoderma lucidum. Ganoderic acid S can induce apoptosis in HeLa cells through the mitochondria pathway[1].
H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).
SR 16832 is a dual-site, covalent and allosteric antagonist of PPARγ, inhibits cellular allosteric activation of PPARγ by rosiglitazone; a useful, complementary chemical tools for researchers to use to simultaneously inhibit both orthosteric and allosteric ligand-induced cellular activation of PPARγ.
Labetuzumab is a humanised anti-carcinoembryonic antigen (CEA) monoclonal antibody that inhibits tumour growth and sensitises human medullary thyroid cancer xenografts to Dacarbazine chemotherapy[1].
KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na+ channels. KB130015 opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle[1][2][3].
Succinate/succinate receptor antagonist 1 (compound 7a) is a succinate/succinate receptor antagonist. Succinate/succinate receptor antagonist 1 blocks succinate signaling in gingival tissue. Succinate/succinate receptor antagonist 1 inhibits the activation of succinate receptor 1 (SucnRl) with an IC50 value of 20 μΜ. Succinate/succinate receptor antagonist 1 can be used for the research of periodontal disease[1].
Erlotinib mesylate inhibits purified EGFR kinase with an IC50 of 2 nM.
Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate drug. Tacrine exhibits certain hepatotoxicity in some individuals. Tacrine can be used for researching Alzheimer's disease (AD)[1][2][3].
Lathyrol is a natural product, and is used for cancer treatment.
Cefditoren pivoxil is a new-third generation cephalosporin antibiotic that has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including common respiratory and skin pathogens.Target: AntibacterialCefditoren pivoxil, a new-third generation cephalosporin antibiotic that has recently been granted approval in Spain, shows important activity over a large part of the pathogens causing skin, soft tissue and respiratory tract infections, including Gram-negative and Gram-positive bacteria. Cefditoren is also marketed under the name Meiact. Cefditoren has a broad spectrum of activity and has been used to treat bacterial infections of the skin and respiratory tract including bronchitis, pneumonia, and tonsillitis. The following represents MIC susceptibility data for a few medically significant microorganisms.Cefditoren has shown excellent in vitro activity against the Gram-positive pathogens penicillin-susceptible and -intermediate Streptococcus pneumoniae, S. pyogenes and methicillin-susceptible Staphylococcus aureus. Cefditoren was inactive against methicillin-resistant S. aureus. Of the important Gram-negative pathogens, cefditoren had potent antibacterial effects against beta-lactamase-positive and -negative Haemophilus influenzae, H. parainfluenzae and beta-lactamase-positive and -negative Moraxella catarrhalis.
VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC50 of 4.6 μM[1].
BI-1950 is a potent, selective LFA-1 antagonist that inhibits the binding of LFA-1 to ICAM-1 with Kd value of 9 nM; displays >1,000 fold selectivity against the most closely related b2-integrin Mac-1 and b1-integrin function; inhibits the production of IL-2 in human PBMC and whole blood with IC50 value of 3 nM and 120 nM, respectively; exhibits an attractive DMPK profile, BI-1950 is a excellent molecule for testing pharmacological hypotheses in vitro and in vivo.
alpha-Man-TEG-N3 is a click chemistry reagent containing an azide group[1].
Gumokimab (AK 111) is a monoclonal antibody targeting IL-17A, which can be used in the study of psoriasis, ankylosing spondylitis. Gumokimab competitively blocks the binding of human IL-17A to IL-17R.
Boc-D-Pen(Mob)-OH is a phenylalanine derivative[1].
Thymosin β10Arg is a thymosin β4-like peptide that contains an additional amino acid, arginine, inserted following lysine-38[1].
Eleutheroside E, a principal component of Eleutherococcus enticosus, has anti-inflammatory and protective effects in ischemia heart. IC50 value:Target:In vitro: Treatment of 10 μM Eleutheroside E (EE) for 24 h increased basal glucose uptake as well as improved TNF-α-mediated suppression of glucose uptake. [2]In vivo: To investigate the effect of Eleutheroside E (EE) on arthritis, the CIA model in DBA/1 mice was used. Compared to vehicle-treated CIA mice, 15 mg/kg TG treatment and 30 and 60 mg/kg EE treatment obviously decreased the arthritis scores and body weight loss in CIA mice (P<0.01) [1].
[Tyr12] Somatostatin 28 (1-14) is an analogue of Somatostatin-28 (1-14) (HY-P1499). Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28[1].
ARQ 531 is a reversible non-covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively[1].
5,6-Didehydroginsenoside Rd is a dammarane-type saponin isolated from the dried roots of Panax notoginseng[1].
L-Methionine hydrochloride is a Methionine (HY-13694) derivative[1].
Bevemipretide is a biodegradable silica hydrogel composite. Bevemipretide can be used for ocular indication[1].
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent[1].
Aucubin is an iridoid glycoside with a wide range of biological activities, including anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.IC50 value:Target:In vitro: Aucubin promotes neuronal differentiation and neurite outgrowth in neural stem cells cultured primarily from the rat embryonic hippocampus [1]. Aucubin significantly reversed the elevated gene and protein expression of MMP-3, MMP-9, MMP-13, iNOS, COX-2 and the production of NO induced by IL-1β challenge in rat chondrocytes [2]. In vivo:
7-O-Geranylscopoletin is a coumarin from the root of Atalantia monophylla. Various parts of this plant have been used for folk medicine for several purposes such as the treatment of chronic rheumatism, paralysis, antispasmodic, stimulant and hemiplegia[1].