PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549[1].
NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
Guaiacin is a arylnaphthalene type lignin isolated from the barks of Machilus thunbergii SIEB. et ZUCC (Lauraceae). Guaiacin significantly increases alkaline phosphatase activity and osteoblast differentiation[1].
Z-Tyr(tBu)-OH.DCHA is a tyrosine derivative[1].
Bersanlimab (BI-505) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anticancer effects[1].
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising drug candidate for the research of KRAS-driven cancer[1].
Isosativan is a natural product that can be found in Trifolium hybridum. Isosativan shows antifungal activity[1].
Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.
N-Demethyl Ivabradine Hcl is a metabolite of Ivabradine, which is a specific inhibitor of the funny channel.
AAF-CMK is a TPPII (tripeptidylpeptidase II) inhibitor, shows anti-tumor activity and induces apoptosis. AAF-CMK can be used in leukemia research[1].
L-Psicose-13C is the 13C labeled L-Psicose[1].
JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.IC50 value: 4 nM [1]Target: c-Metin vitro: JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. [1] In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth [2]. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells [3]. in vivo: In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose [3].
TP-0903 is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
SU 5616 is an organic compound. SU 5616 potentially modulates tyrosine kinase signal transduction, and regulates abnormal cell proliferation[1].
CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection[1].
CBQCA is a fluorescencent dye for quantitation of protein (Ex=488nm, Em=530 nm)[1].
Norfloxacin nicotinate (MK-0366 nicotinate) is a fluoroquinolones antibiotic, an adduct of Norfloxacin (NOR) and nicotinic acid. Norfloxacin nicotinate has been widely used for replacing NOR in animal husbandry and fishery industry. Norfloxacin nicotinate can induce innate immune response at a high concentration[1].
N-(Azido-PEG3)-NH-PEG3-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α.target: p38α;R1487 (Hydrochloride) potently inhibits cytokine production in a variety of in vitro and in vivo models.[1]R1487 (Hydrochloride) inhibits production of TNFR by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS.[1]
LY3143921 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. LY3143921 shows broad in vitro anticancer activity[1].
5-HT2 agonist-1 (Compound 24) is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders[1].
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect[1].
NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM[1][3][4].
Norverapamil is a calcium channel blocker， it is the main active metabolite of verapamil.In vitro: Norverapamil is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs. norverapamil, also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil.[1] Norverapamil (NOR) is the major metabolite and shows approximately 20% of the efficacy of VER with regard to the vasodilation effect, but shows no antiarrhythmic activity. [2] Verapamil and its major metabolite norverapamil were identified to be both mechanism-based inhibitors and substrates of CYP3A and reported to have non-linear pharmacokinetics in clinic. [3]
9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-phenylpurine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound that inhibits stress-induced ulcer and low toxicity, and can maintain the content of phospholipase A2 and prostaglandin E2 in ulcerated rats induced by water immersed restrained stress.
Gomisin D, a lignan compound isolated from Fructus Schisandra, is a potential antidiabetic and anti-Alzheimer’s agent. Gomisin D inhibits UDP-Glucuronosyltransferases activity and scavenges ABTS(+) radicals. Gomisin D is used as a quality marker of Shengmai San and shenqi Jiangtang Granule[1].
9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal. 9-cis-β-Carotene inhibits photoreceptor degeneration and restores retinal function in vivo. 9-cis-β-Carotene has the potential for the study of congenital stationary night blindness and fundus albipunctatus[1].
Colistimethate is a polymyxin with cytotoxicity to renal tubular cells. Colistimethate has poorly inactive in vivo. Colistimethate shows seldomly detectable activity against 6 strains of P. aeruginosa[1][2].
KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.IC50 value: 15, 43, and 5.9 nM (mouse, rat, and human brain proteomes)Target: MAGLin vitro: KML29 potently and selectively inhibits MAGL with minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.[1]in vivo: KML29 a potentially very useful tool to explore the consequences of inhibiting MAGL in the whole animal and in multiple species, and provides greater selectivity than JZL184 in inhibiting MAGL. [2]