AG-1557, compound 22 (T), is a ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with a pIC50 value of 8.194[1].
Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities. Butin significantly alleviates myocardial infarction and improves heart function, together with prevents diabetes-induced cardiac oxidative damage in rat[1][2].
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity[1].
3-Maleimidobenzoic acid N-hydroxysuccinimide ester is used as asymmetric spacers[1].
(Rac)-Azide-phenylalanine is a racemate of Azide-phenylalanine. Azide-phenylalanine is a phenylalanine derivative and a non-natural amino acid. Azide-phenylalanine can be site-specifically incorporated into proteins and used to label proteins[1].
DMX-129 is an ΙΚΚε and TBK-1 inhibitor with IC50 values of <30 nM for both TBK1 and IKKε[1].
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease[1][2][3].
Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis[1][2].
(R)-Rivastigmine D6 (tartrate) is the deuterium labeled (R)-Rivastigmine, which is an cholinesterase inhibitor.
QC6352 is a potent KDM4C inhibitor with an IC50 of 35 nM.
N2-(((9H-Fluoren-9-yl)methoxy)carbonyl)-Nw-((4-methoxy-2,3,6-trimethylphenyl)sulfonyl)-N2-methyl-L-arginine is an arginine derivative[1].
BAY-826 is a selective and potent TIE-2 inhibitor with Kd of 1.6 nM, respectively.
3-Hydroxypentan-2-one, natural product, can be isolated from Carambola (Averrhoa carambola L. )[1].
Keto Ziprasidone is an impurity of Ziprasidone[1]. Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist[2].
p38 Kinase inhibitor 4 (compound 135) is a potent p38 inhibitor[1].
Phloretin(NSC 407292; RJC 02792) is a dihydrochalcone, a type of natural phenols. Phloretin inhibits the active transport of glucose into cells by SGLT1 and SGLT2.IC50 Value: 49 +/- 12 microM [4]Target: SGLT1/2in vitro: Phlorizin blocks glucose transport across the renal tubule at concentrations in renal blood and tissue in the range of 10-5 to 10-7 M [1]. PT significantly enhanced glycerol release and inhibited the adipogenesis-related transcription factors. PT also promoted phosphorylation of AMP-activated protein kinase and increased activity of adipose triglyceride lipase and hormone-sensitive lipase in 3T3-L1 cells [2]. Phloretin induced obvious cytotoxicity against BEL-7402 cells with IC50 of 89.23 microg/mL. The growth curve demonstrated decreased growth of the cells as phloretin concentration increased [3]. D-glucose-transport activity was observed with a Km for D-glucose of 3.4 +/- 0.2 mM (mean +/- S.E.M.) and was inhibited by cytochalasin B (IC50= 0.44 +/- 0.03 microM), HgCl2 (IC50)= 3.5 +/- 0.5 microM), phloretin (IC50= 49 +/- 12 microM) and phloridzin (IC50= 355 +/- 67 microM) [4].in vivo: The effect of phloridzin orally doses 5, 10, 20 and 40 mg/kg body weight on diabetes was tested in a streptozotocin-induced rat model of diabetes type 1. From beneficial effect of this compound is significant reduction of blood glucose levels and improve dyslipidemia in diabetic rats [5].
Bromoacetamido-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CK2-IN-7 (compound 2) is an inhibitor of casein kinase 2 (CK2). CK2-IN-7 shows synergistic effect with structurally distinct CK2 chemical probe: SGC-CK2-1, against cancer[1].
LY3143921 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. LY3143921 hydrate shows broad in vitro anticancer activity[1].
MBM-17 (compound 42c) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice[1].
Vadimezan (ASA-404; DMXAA), the vascular disrupting agent, is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines.
Tamarixetin (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin, with anti-oxidative and anti-inflammatory effects. Tamarixetin protects against cardiac hypertrophy[1][2].
Hirsutine, an indole alkaloid of Uncaria rhynchophylla, exhibits anti-cancer activity. Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity[1][2][3].
Calcein Blue is a short-term, blue-fluorescent dye for labeling live cells.
Mal-PEG2-CH2COOH is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Ac-Lys-D-Ala-D-Ala-OH is an oligopeptide. Ac-Lys-D-Ala-D-Ala-OH can be used for the research of various biochemical[1].
Aneratrigine (hydrochloride) is a sodium channel protein type 9 subunit alpha blocker. Aneratrigine (hydrochloride) can be used for neuropathic pain diseases research[1].
Erastin2 is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter[1][2].
Dovitinib-D8 (CHIR-258-D8) is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively[1][2].
trans-1,4-Dihydroxycyclohexaneacetic acid is a cyclohexylacetic acid derivative, which can be isolated from the aerial parts of Emilia sonchifolia[1].