STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.IC50 value:Target: NAMPT inhibitorin vitro: improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and targets leukemia stem cells. STF-118804 displays distinctive cytotoxicity by inducing apoptosis without causing a phase-specific cell cycle arrest. Over-expression of NAMPT rendered 293T cells more resistant to STF-118804 resulting in a higher IC50 (106 nM, 95% CI 74–151 nM) compared to control cells (17 nM, 95% CI 13–23 nM), further confirming that NAMPT protein levels dictate sensitivity to STF-118804 [1].in vivo: STF-118804 displayed high efficacy in a xenograft model of ALL. Mice treated with STF-118804 over a 20-day period survived an average of 34 days longer than vehicle-treated animals. During treatment, bioimaging showed regression of tumor followed by suppression of disease. STF-118804 was tolerated in the efficacious dose range, and the absence of adverse physical or pathological effects indicated that toxicity was not limiting in a 20-day study of mock transplanted mice [1].
19-Oxocinobufotalin is capable of suppressing EMT (Epithelial-mesenchymal transition) and weakening the migratory and invasive potential of PC3 cells[1].
Ublituximab (LFB-R603; TG-1101; TGTX-1101) is a next-generation, type 1 chimeric monoclonal antibody targeting a unique epitope on the CD20 antigen. Ublituximab has anticancer effects[1].
BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells[1][2].
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer[1].
PMEDAP is a potent inhibitor of human immunodeficiency virus (HIV) replication. PMEDAP has anti-murine cytomegalovirus (MCMV) activity. PMEDAP is a very potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and associated mortality[1][2].
Adrixetinib is an inhibitor of protein tyrosine kinase with antineoplastic activity[1][2].
BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM[1].
Monomethyl auristatin E intermediate-6 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
HO-1-IN-1 hydrochloride (Compound 2) is a heme oxygenase 1 (HO-1) inhibitor with an IC50 of 250 nM[1].
Gefitinib (ZD1839) is a EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer[1].
Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent depositiontarget: AβIn vitro: Tramiprosate provides neuroprotection against Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors. Tramiprosate dose-dependently provides neuroprotection against ischemic stroke.In vivo: Tramiprosate produced dose-dependent reductions of Aβ in the brain of transgenic mice (hAPP-TgCRND8). Clinical studies show that tramiprosate was safe and tolerable. In mild-to-moderate AD patients tramiprosate also reduced Aβ42 levels in CSF.The reference for animal administration is 50 mg/kg.
Heptadecanoic-d33 acid is the deuterium labeled Heptadecanoic acid. Heptadecanoic acid is an odd chain saturated fatty acid (OCS-FA). Heptadecanoic acid is associated with several diseases, including the incidence of coronary heart disease, prediabetes and type 2 diabetes as well as multiple sclerosis[1].
AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.
Dovitinib (dilactic acid) is an orally active inhibitor of VEGF kinase. Dovitinib (dilactic acid) inhibits receptor tyrosine kinases (RTKs) involved in solid and hematologic cancers and tumor angiogenesis[1].
CPT2 (Carnitine palmitoyltransferase 2), an enzyme that participates in fatty acid oxidation, also is a colorectal cancer (CRC) prognostic biomarker. CPT2 overexpression can activate p-p53 to increase p53 expression, thereby inhibiting tumor proliferation and promoting apoptosis. CPT2 deficiency results in the most common inherited disorder of long-chain fatty acid oxidation affecting skeletal muscle. Downregulation of CPT2 is also highly correlated with the progression of various cancers and has potential for cancer research[1][2].
Malonylginsenoside Rc is a natural active compound with anti-proliferative activity[1].
SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation[1]. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis [2].
Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells[1].
(rel)-BMS-641988 is a relative configuration of BMS-641988. BMS-641988 is a potent nonsteroidal androgen receptor antagonist. BMS-641988 has the potential for the research of prostate cancer[1].
Ganoderic acid AM1 (GAAM1) is a natural product that can be found in ganoderma lucidum. Ganoderic acid AM1 shows cytotoxicity with an IC50 value of 19.8 µM for HeLa cells[1].
Juncuenin D induces caspase-3-mediated cytotoxicity in HT22 cells. Juncuenin D also has anti-bacterial activity against MRSA strains. Juncuenin D can be isolated from J. effusus[1].
MC 1046(Impurity A of Calcipotriol) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors. IC50 value:Target: Vitamin D3 analog that displays minimal effects on calcium homeostasis. Regulates cell differentiation and proliferation; Calcipotriol (MC 903; Calcipotriene) exhibits antiproliferative activity against human HL-60, HL60/MX2, MCF-7, T47D, SCC-25 and mouse WEHI-3 cancer cell lines.
Azido-PEG6-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG6-amine is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Propargyl-PEG2-NHBoc is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-NHBoc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Azetidine-3-carboxylic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azetidine-3-carboxylic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2
Isoeugenol acetate, an essential oil constituent of nutmeg, clove, and cinnamon, shows excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes (IC50=77 nM; Ki=16 nM), α-glycosidase (IC50=19.25 nM; Ki=21 nM), and α-amylase (IC50=411.5 nM). Isoeugenol acetate is used medical and cosmetics industries for its antioxidant, anticancer, antimicrobial and anti-inflammatory properties[1][2].
Procyanidin B2 is a natural flavonoid, with anti-cancer, antioxidant activities.
SN05 is a potent amino acid transport (AAT) inhibitor with Kis of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used for researching anticancer[1].