Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system[1].
TG 100801 Hydrochloride is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats[1].
Kaempferitrin is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway.
AcBut is a pH cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Azido-PEG8-NHS ester is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Azido-PEG8-NHS ester is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[2].
A novel potent and metabolically stable tubulin inhibitor that can circumvent the drug efflux pumps responsible for multidrug resistance of existing tubulin inhibitors; demonstrates cytotoxicty in a panel of human metastatic melanoma cell lines harboring major clinically relevant mutations with IC50 of 7-10 nM, disrupts microtubule networks, suppresses anchorage-dependent melanoma colony formation, and impaires cancer cell migration; inhibits tumor growth and reduced lung metastasis in melanoma-bearing mice, also completely inhibits tumor growth in a paclitaxel-resistant xenograft mouse model.
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRASG12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 has picomolar binding affinity, single digit nanomolar activity in cellular assays, and marked in vivo efficacy in tumor models harboring KRASG12D mutations[1].
Acetomycin is an antibiotic. Acetomycin inhibits the growth of CT-8 human colon adenocarcinoma cells (IC50: 1.5 μg/mL) and L1210 murine leukemia cells (IC50: 2.2 μg/mL). Acetomycin can be isolated from actinomycete WP-2661[1].
DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs)[1].
IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
3’-β-Amino-2’,3’-dideoxy-5’-O-methoxy trityluridine 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].
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].
Galectin-3 antagonist 1 (compound 15) is a potent and selective Galectin-3 (Gal-3) antagonist with Kd value of 5.3 μM. Meanwhile, Galectin-3 antagonist 1 binds to various Galectin with Kd values of 250 μM (Gal-4N), 18 μM (Gal-4C), 450 μM (Gal-8C), respectively[1].
B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM[1].
Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
Tenovin-1 is an inhibitor of sirtuin 1 and sirtuin 2, an activator of p53 and may have potential in the management of cancer.
Cabozantinib-d6 (XL184-d6) is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Clionamine B is an autophagy stimulating aminosteroid isolated from the sponge Cliona celata. Clionamine B strongly stimulates autophagy in human breast cancer MCF-7 cells[1].
TCO-PEG4-biotin is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe[1].
SHP2-IN-19 (compound 183) is a SHP2 inhibitor with an IC50 value of 3 nM. SHP2-IN-19 can be used for glioblastoma research[1].
Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities[1]. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway[2].
Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition[1].
2-Aminoadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
DT-6 is an effective TGF-β1 inhibitor. DT-6 inhibits M2 macrophage induced epithelial to mesenchymal transition and invasive migration of cancer cells. DT-6 can be used for cancer diseases research[1].
Alacizumab pegol (CDP-791) is a pegylated antibody fragment directed against KDR. Alacizumab pegol can be used for the research of cancer[1].
IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor, extracted from patent WO2014150677A1, Compound example 1 enantiomer 1.
Azo-resveratrol, an Azo compound, inhibits Mushroom tyrosinase (IC50=36.28 μM).