Corynoxine is an enantiomer of Corynoxine B; induces autophagy in different neuronal cell lines, including N2a and SHSY-5Y cells.IC50 value:Tareget: Autophagy inducerIn vivo, Cory promotes the formation of autophagosomes in the fat bodies of Drosophila. By inducing autophagy, Cory promotes the clearance of wild-type and A53T α-syn in inducible PC12 cells. Interestingly, different from its enantiomer Cory B, Cory induces autophagy through the Akt/mTOR pathway as evidenced by the reduction in the levels of phospho-Akt, phospho-mTOR and phospho-p70 S6 Kinase [1]. Corynoxine significantly decreased locomotor activity after oral administration to mice [2].
FGFR3-IN-7 is a potent and selective FGFR3 inhibitor with IC50 value less than 350 nM. FGFR3-IN-7 can be used in research of cancer[1].
(Rac)-Hesperetin-13C,d3 is the 13C- and deuterium labeled. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
Momelotinib-3,3,5,5-d4 (CYT387-3,3,5,5-d4) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
Naratuximab (Anti-TSPAN26/CD37 Reference Antibody (naratuximab)) is a humanized monoclonal antibody that binds CD37 (TSPAN26). Naratuximab can be used to synthesize an ADC compound, Naratuximab emtansine[1].
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
2-Chloroinosine 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].
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer[1].
FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.
PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects[1].
Methyl 2,3,5-tri-O-benzyl-D-ribofuranoside 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].
Debio 0123 (Debio0123) is a potent, orally available, and highly selective Wee1 kinase inhibitor with IC50 of 0.8 nM, Ki of 0.1 nM.Debio 0123 is highly selective to Wee1 on 465 selected kinases in a cellfree system, does not inhibit Plk1 and Plk2, as also reported in recent publications for AZD1775.Debio 0123 exhibits in vitro growth inhibition activity in a broad number of human cancer cell lines (IC50= 0.109 to 7.08 uM).Debio 0123 prevent CDC2 / Cdk1 phosphorylation, induces γH2AX and enhances phosphorylation of histone H3.Debio 0123 induces apoptosis through mitotic catastrophe following cell cycle progression despite accumulation of unrepaired DNA damage both in vitro and in vivo.
α-Thevetin B（Compound 24） is a cardiac glycoside that can be isolated from Thevetia peruviana. α-Thevetin B（Compound 24） can be used in lung cancer, gastric cancer and pancreatic cancer research[1].
Azido-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways[1].
NH-bis(C1-Boc)is a uncleavable linker used for antibody-drug conjugates (ADC).
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary drug conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors[1][2][3].
C-11 is a tubulysin-based antibody–drug conjugates (ADCs), displays cytotoxicity for carcinoma cell lines[1].
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity[1].
GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
2-Amino-2’,3’-bis-O-(2-methoxyethyl) adenosine 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].
Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.
Methyl 2-deoxy-3,5-di-O-toluoyl-D-ribofuranoside 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].
Monomethyl auristatin E intermediate-14 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].
λ-Carrageenan is a seaweed polysaccharide which has been generally used as proinflammatory agent in the basic research. λ-Carrageenan is a potent antitumor agent[1].
VEGFR-2-IN-21 (Compound 5d) is a potent VEGFR-2 inhibitor with an IC50 of 0.10 μM. VEGFR-2-IN-21 shows anticancer activity[1].
Izeltabart (IMGC-936) is a Maytansinoid-based ADC targeting ADAM9. Izeltabart is comprised of a high-affinity humanized antibody site-specifically conjugated to DM21-C, a linker-payload that combines a Maytansinoid microtubule-disrupting payload with a stable tripeptide linker, at a drug antibody ratio of approximately 2.0. Izeltabart exhibits cytotoxicity toward ADAM9-positive human tumor cell lines and has potent antitumor activity in xenograft tumor models[1].
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc[1].
1,2-Di-O-isopropylidene-3-O-methyl-D-ribofuranose 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].
Isogambogenic acid is a natural product that can be isolated from Resina Garciniae. Isogambogenic acid has cytotoxicity to cancer cell lines with IC50 values of 0.4327-5.942 μmol/L[1].