Monoethyl phthalate-d4 is the deuterium labeled Monoethyl phthalate[1]. Monoethyl phthalate is a metabolite of diethyl phthalate. Monoethyl phthalate acts as a urinary biomarker of phthalates exposure indicating the risks of thyroid cancer and benign nodule[2][3].
Menin-MLL inhibitor 24 (compound A) is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor. Menin-MLL inhibitor 24 can be used for the research of cancer[1].
Platycodin D2 is a saponin isolated from Platycodon grandiflorum, with anti-cancer activity[1].
NY2267 is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM. NY2267 inhibits Myc- and Jun-induced transcriptional activation[1].
Stauntosaponin A, a steroid glycoside, is a potent inhibitor of Na(+)/K(+)-ATPase with an IC50 value of 21 nM. Stauntosaponin A can be isolated from Carnation and has potential anti-cancer research value[1].
5’-Deoxy-5’-N,N-dimethylamino thymidine is a purine nucleoside analog. 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].
Napyradiomycin A1 is one enantioselective compound of napyradiomycins. napyradiomycins are an intriguing family of halogenated natural products with activity against several tumor cell lines as well as some bacterial strains[1].
Stearic acid-d5 is the deuterium labeled Stearic acid. Stearic acid is a long chain dietary saturated fatty acid which exists in many animal and vegetable fats and oils.
Evuzamitide is a diagnostic imaging agent. Evuzamitide as a pan-amyloid radiotracer binding to amyloid deposits from multiple amyloidogenic proteins. Evuzamitide can be used for the research of early diagnosis of amyloid cardiomyopathy (CMP) and monitoring[1][2].
IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1)[1].
Isorhamnetin 3-glucuronide is a potent anticancer agent. Isorhamnetin 3-glucuronide shows anti-proliferative activity. Isorhamnetin 3-glucuronide induces Apoptosis and cell cycle arrest at S-phase[1].
CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.
3',5'-Bis-O-benzoyl-2'-deoxy-2'-fluoro-beta-D-arabino-6-azidouridine is a purine nucleoside analog. 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].
Dehydrobruceine B, a quassinoid, can be isolated from Brucea javanica. Dehydrobruceine B shows a synergistic effect with Cisplatin (HY-17394) to induce apoptosis via mitochondrial method. Dehydrobruceine B increases apoptosis-inducing factor (AIF) and Bax expression and suppresses Keap1-Nrf2[1].
MCC-DM1 is a drug-Linker Conjugates for ADC such ad Anti-CD22-MCC-DM1[1].
UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs.IC50 value: 0.06 μM (HDAC3), 0.1 μM (HDAC2), 0.5 μM (HDAC1), 1.5 μM(HDAC 8)Target: HDACin vitro: UF010 is a competitive inhibitor with a fast-on/slow-off HDAC-binding mechanism. UF010 induces accumulation of acetylated histones in HCT116 cells in vitro, arrests cells at G1/S transition. It inhibits proliferation of a range of cancer cell lines. UF010 activates tumor suppression mechanisms while inhibiting oncogenic pathways.
POP-3MB (compound 1b) is an ICMT inhibitor (IC50: 2.5 μM). POP-3MB changes the subcellular localization of K-Ras and inhibits Ras activation. POP-3MB also inhibits Erk phosphorylation[1].
HMN-154 is a novel benzenesulfonamide anticancer compound; inhibits KB and colon38 cells with IC50 values of 0.0026 and 0.003 μg/mL, respectively.
Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC50 value of 3.2 μM. Anti-tumor agent[1].
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells[1].
AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells[1].
PSI-697is a P-selectin inhibitor.In vivo: 30 mg/kg; oral gavage daily. Animals treaed with PSI-697 shows a significantly decreased intimal thickness score when compared with vehicle control IVCs. PSI-697 significantly decreased vein wall levels of platelet-derived growth factor . d PSI-697 inhibits vein wall injury independently of thrombus mass. P-selectin inhibition seemed superior to LMWH in measured parameters of injury and mediator inhibition. PSI-697 inhibit vein wall injury independently of thrombus size in a rodent model of DVT. [1] PSI-697 (50 mg/kg p.o.) significantly reduced the number of rolling leukocytes by 39% (P < 0.05) versus vehicle control. In a rat venous thrombosis model, PSI-697 (100 mg/kg p.o.) reduced thrombus weight by 18% (P < 0.05) relative to vehicle, without prolonging bleeding time. [2] Animals receiving PSI-697 demonstrated significantly increased plasma D-dimer levels versus LMWH and control animals six hours post thrombus induction.[3]
FGFR-IN-1 is a potent FGFR inhibitor with an IC50 of <100 nM for FGFR1, FGFR2, and FGFR3, respectively (patent US20130338134A1, example 219)[1].
Tos-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity[1].
D-Glucose-13C2,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
Prostaglandin A2 (PGA2), a human endogenous metabolite of PGE2, is an antitumor agent. Prostaglandin A2 induces p53-dependent Apoptosis. Prostaglandin A2 also has antiviral activity[1][2][3].
Bufalin a major digoxin-like immunoreactive component of the Chinese medicine Chan Su; has been shown to exert a potential for anticancer activity against various human cancer cell lines in vitro.IC50 value:Target: Anticaner natural compoundin vitro: bufalin remarkably inhibited growth in human gallbladder cancer cells by decreasing cell proliferation, inducing cell cycle arrest and apoptosis in a dose-dependent manner. Bufalin also disrupted the mitochondrial membrane potential (ΔΨm) and regulated the expression of cell cycle and apoptosis regulatory molecules. Activation of caspase-9 and the subsequent activation of caspase-3 indicated that bufalin may be inducing mitochondria apoptosis pathways [1]. bufalin suppressed the protein levels associated with DNA damage and repair, such as a DNA dependent serine/threonine protein kinase (DNA-PK), DNA repair proteins breast cancer 1, early onset (BRCA1), 14-3-3 σ (an important checkpoint keeper of DDR), mediator of DNA damage checkpoint 1 (MDC1), O6-ethylguanine-DNA methyltransferase (MGMT) and p53 (tumor suppressor protein) [2]. TNF-α significantly increased p65 translocation into nucleus (P < 0.01) and enhanced NF-κB DNA-binding activity, which were dose-dependently inhibited by bufalin. Furthermore, bufalin attenuated the TNF-α-induced interleukin-1beta (IL-1β), IL-6, and IL-8 production in RAFLSs in a concentration-dependent manner [3]. bufalin enhanced TRAIL-induced apoptosis in MCF-7 and MDA-MB-231 breast cancer cells by activating the extrinsic apoptotic pathway. Bufalin also promoted the clustering of death receptor 4 (DR4) and DR5 in aggregated lipid rafts [4].in vivo: bufalin (0.3 and 0.6 mg/kg, i.p.) potently decreased carrageenan-induced paw edema. Bufalin down regulated the expression levels of nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) during these treatments [5].
Tivozanib hydrochloride hydrate is a potent and selective and orally active VEGFR tyrosine kinase inhibitor with IC50是of 0.21, 0.16, 0.24 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. Tivozanib hydrochloride hydrate inhibits angiogenesis and vascular permeability in tumor tissues and shows antitumor activity. Tivozanib hydrochloride hydrate has the potential for the research of metastatic renal cell carcinoma (RCC) [1][2][3].