Formosanin C is a diosgenin saponin isolated from Paris formosana Hayata and an immunomodulator with antitumor activity. Formosanin C induces apoptosis[1][2].
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.
Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitory activity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM[1][2].
LYG-202, a flavonoid, has potent anti-angiogenic and antitumor activity. LYG-202 inhibits VEGF-stimulated HUVEC migration and tube formation. LYG-202 induces cancer cell apoptosis[1][2].
A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively.
Laprituximab emtansine (IMGN-289) is an immunotoxin targeting HER1. Laprituximab emtansine is an EGFR antibody-drug conjugate (ADC) consisting of the J2898A antibody, DM1 (anti-microtubule agent) and the SMCC thioether linker. Laprituximab emtansine can be used for cancer research[1][2][3].
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].
(±)-Equol is the racemate of equol. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.
PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC50 of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) [1].
GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
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]
Aminooxy-PEG3-C2-NH-Boc is a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively[1].
10-Deacetyltaxol (10-Deacetylpaclitaxel) is a taxane derivative isolated from Taxus wallichiana Zucc[1]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) promotes the polymerization of tubulin and to inhibit the depolymerization of microtubules induced by cold or by calcium ions in vitro[2]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) exhibits cytotoxicity in human glial and neuroblastoma cell-lines[3].
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].
FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
Thalidomide-5-O-C3-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
Proglumide is a known cholecystokinin (CCK) antagonist.
Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs.IC50 value: 150 nM (HDAC1), 370 nM (HDAC3), 760nM(HDAC2)Target: HDAC in vitro: Pimelic diphenylamide 106 has preference toward HDAC3 with Ki of 14 nM, 15 times lower than the Ki for HDAC1.Pimelic diphenylamide 106 exhibits weaker inhibitory activities against HDAC 8 with IC50 of 5 μM after a 3-h preincubation with HDAC8.
Trijuganone C, a natural product extracted from Salvia miltiorrhiza, inhibits the proliferation of cancer cells through induction of apoptosis mediated by mitochondrial dysfunction and caspase activation[1].
OSBP-IN-1(compound 12) is a Schweinfurthins analogues targeted of oxysterol-binding protein (OSBP). OSBP-IN-1 has antitumor activity[1].
YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
Ivospemin is an antineoplastic spermine analog[1].
1-(2'-Deoxy-5'-O-DMT-2'-fluoro-b-D-arabinofuranosyl)thymine 3'-CE phosphoramidite is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
E3 ligase Ligand-Linker Conjugates 30 incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 30 can be used to design PROTAC MDM2 degrader[1].
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity[1].
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1].