Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent. Ceratamine A exhibits cytotoxicity against human cancer cell lines[1][2][3].
ASP3026 is a novel and selective inhibitor for ALK (anaplastic lymphoma kinase) with IC50 of 3.5 nM.
EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM.
PPA is an ADC linker (US20060073528A1). PPA can be used for making antibody-drug conjugate[1].
(R)-FL118 (10,11-(Methylenedioxy)-20(R)-camptothecin) is the R-enantiomer of FL118 (HY-12486). (R)-FL118 shows anticancer activity[1].
Glucose-6-phosphate dehydrogenase is the rate-limiting enzyme of the pentose phosphate pathway. Glucose-6-phosphate dehydrogenase is a major source of NADPH that is required by many essential cellular systems including the antioxidant pathways, nitric oxide synthase, NADPH oxidase, cytochrome p450 system, and others. Glucose-6-phosphate dehydrogenase can be used for the research of diabetes, aldosterone-induced endothelial dysfunction, and cancer[1].
Pegdinetanib (BMS-844203; CT-322) is a selective VEGFR-2 (VEGFR) inhibitor with Kds of 11 nM and 250 nM and IC50s of 16 nM and 240 nM for human and murine VEGFR-2, respectively. Pegdinetanib does not bind to VEGFR-1 or VEGFR-3. Pegdinetanib has antitumor activity[1].
A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
PX-478 is an antitumor inhibitor of hypoxia-inducible factor-1α (HIF-1α).
Tridecanoic acid-d25 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation[1].
Propargyl-C2-NHS ester is a nonclaevable linker for antibody-drug-conjugation (ADC).
MAC glucuronide linker-1 is a nonclaevable ADC linker for antibody-drug-conjugations (ADCs)[1].
2-Chloro-N6-furfuryladenine is a Kinetin riboside derivative[1].
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity[3]. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively[1]. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation[3].
Bis-propargyl-PEG8 (compound 16e) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
BAN ORL 24 free base is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 free base has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 free base can be used for the research of cancer and analgesic[1].
HG106 is a potent SLC7A11 inhibitor. HG106 markedly decreased cystine uptake and intracellular glutathione biosynthesis. HG106 can be used for the research of KRAS-mutant lung adenocarcinoma[1].
Uridine 13C-2 is the 13C labeled Uridine[1].
Aminomalonic acid is an amino endogenous metabolite, acts as a strong inhibitor of L-asparagine synthetase from Leukemia 5178Y/AR (Ki= 0.0023 M) and mouse pancreas (Ki= 0.0015 M) in vitro. Aminomalonic acid is a potential biomarker to discriminate between different stages of melanoma metastasis[1][2][3].
Nicotinamide Hydrochloride is a form of vitamin B3 or niacin that inhibits sirtuin 2 (SIRT2) activity in vitro, with an EC50 of 2 μM. Nicotinamide Hydrochloride inhibits up to 90% melanoma cell number and increases cellular NAD+, ATP, ROS levels. Nicotinamide Hydrochloride inhibts tumor growth in vivo and improves survival of melanoma-bearing mice, which can be used for the research of skin cancers such as melanoma[1].
Dehydroeffusol is a phenanthrene from medicinal herb Juncus effuses. Dehydroeffusol inhibits gastric cancer cell growth and tumorigenicity by selectively inducing tumor-suppressive endoplasmic reticulum stress and a moderate apoptosis. It shows very low toxicity[1][2].
Isobutyl-deoxynyboquinone (IB-DNQ) is a selective substrate for NAD(P)H:quinone oxidoreductase (NQO1), produces ROS, and induces cytotoxicity in cancer cells in an NQO1-dependent manner; has improved solubility and biocompatibility in comparison with DNQ; a superior drug candidate for evaluating anticancer activities and tolerability in vivo.
PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.IC50 value: 9 nMTarget: c-Metin vitro: PHA-665752 significantly inhibits c-Met kinase activity with Ki of 4 nM, and exhibits >50-fold selectivity for c-Met compared with various tyrosine and serine-threonine kinases. PHA-665752 potently inhibits the HGF-stimulated c-Met autophosphorylation with IC50 of 25-50 nM. PHA-665752 also significantly blocks HGF- and c-Met-dependent functions such as cell motility and cell proliferation with IC50 of 40-50 nM and 18-42 nM, respectively. In addition, PHA-665752 potently inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines [1]. PHA-665752 inhibits cell growth in TPR-MET-transformed BaF3 cells with IC50 of <60 nM, and inhibits constitutive cell motility and migration by 92.5% at 0.2 μM. Inhibition of c-Met by PHA665752 (0.2 μM) also induces cell apoptosis of 33.1% and G1 cell cycle arrest with cells in G1 phase increasing from 42.4% to 77.0%. PHA665752 can cooperate with rapamycin to inhibit cell growth of TPR-MET-transformed BaF3 cells and non-small cell lung cancer H441 cells [2].in vivo: Administration of PHA-665752 induces a dose-dependent tumor growth inhibition of S114 xenografts by 20 %, 39% and 68%, at dose of 7.5, 15, and 30 mg/kg/day, respectively [1]. PHA665752 treatment significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively. PHA665752 also significantly inhibits angiogenesis by >85%, due to decreasing the production of vascular endothelial growth factor and increasing the production of the angiogenesis inhibitor thrombospondin-1 [3].
S65487 (VOB560) hydrochloride is a potent and selective Bcl-2 inhibitor. S65487 hydrochloride is also active on BCL-2 mutations, such as G101V and D103Y. S65487 hydrochloride has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 hydrochloride induces apoptosis and has anticaner activities[1][2].
EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases[1].
YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis[1].
DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM[1][2].
Boc-Aminooxy-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
1-(β-D-Xylofuranosyl)uracil is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].