Notum-IN-1 (compound 6b) is an orally active, selective and brain penetrant inhibitor of Notum. Notum-IN-1 blocks the Wnt signaling in vivo in mouse[1].
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
Erucin (ERU) is an isothiocyanate particularly abundant in arugula. Erucin shows anticancer, neuroprotective, and anti-inflammatory activities[1][2][3][4].
4-Bromo A23187 is a halogenated analog of the highly selective calcium ionophore A-23187. 4-Bromo A23187，a calcium modulator, induces apoptosis in different cells, including HL-60 cells[1].
Z-Ile-Leu-aldehyde(Z-IL-CHO; GSI-XII) is a potent gamma-Secretase inhibitor; Notch signaling inhibitor.IC50 value:Target: gamma-Secretase inhibitorin vitro: GSI-XII induces apoptosis of murine MOPC315.BM myeloma cells with high Notch activity. GSI XII impairs murine osteoclast differentiation of receptor activator of NF-κB ligand (RANKL)-stimulated RAW264.7 cells in vitro [1]. Notch-signaling inhibition in HRS cells by the γ-secretase inhibitor (GSI) XII results in decreased alternative p52/RelB NF-κB signaling, interfering with processing of the NF-κB2 gene product p100 into its active form p52 [2]. GSI treatment induced morphologic erythroid differentiation and promoted hemoglobin production. GSI treatment suppressed short-term growth and colony formation, while treatment with GSI-XXI promoted the growth of AA cells [3].in vivo: In the murine MOPC315.BM myeloma model GSI XII has potent anti-MM activity and reduces osteolytic lesions as evidenced by diminished myeloma-specific monoclonal immunoglobulin (Ig)-A serum levels and quantitative assessment of bone structure changes via high-resolution microcomputed tomography scans [1].
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research[1].
Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
NMS-P515 is a potent and stereospecific PARP-1 inhibitor, with an IC50 of 27 nM in hela cells. Anti-tumor activity[1].
Crizotinib hydrochloride is a potent inhibitor of c-Met and ALK with IC50s of 11 nM and 24 nM in cell-based assays, respectively.
GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12F36V). FKBP12F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC)[1].
CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM[1].
NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways[1][2].
Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity[1].
THP-PEG8-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Laprituximab (J2898A) is a humanized IgG1 anti-EGFR antibody that can be used for the synthesis of ADC IMGN289[1].
2'-O-(2-Methoxyethyl)-cytidine is a synthetic oligonucleotide conversed from uridine. 2'-O-(2-Methoxyethyl)-uridine has the potential for chemotherapeutic agents development[1].
Piperkadsin A is a potent inhibitor of ROS. Piperkadsin inhibits PMA-induced ROS production in human polymorphonuclear neutrophils with an IC50 of 4.3 μM[1].
N4-Benzoyl-2'-deoxy-5'-O-DMT-2',2'-difluorocytidine 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].
TP3011 is a potent topoisomerase-1 inhibitor and is the active metabolite converted from TP3076 by aldehyde oxidase 1 (AOX1)[1]. TP3011 has robust anti-tumor activities against cancer cell lines[2].
PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions[1].
Cdc7-IN-13 (compound 84) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-13 has the potential for the research of cancer[1].
IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy[1].
Tezosentan-d4 (RO 610612-d4) is the deuterium labeled Tezosentan. Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively[1][2].
Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4+ T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice[1].
EGFR-IN-88 (Compound 4i) is an EGFR inhibitor (IC50: 87 nM). EGFR-IN-88 shows cytotoxicity against A549 cell with an IC50? of 3.902? μM. EGFR-IN-88 can induce cell apoptosis[1].
Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research[1].
A novel, spectfic c-Myc IRES (internal ribosome entry site) function inhibitor that prevents binding of hnRNP A1 to the Myc IRES and specifically inhibits Myc IRES activity in MM cells; shows no effect on BAG-1, XIAP and p53 IRESes, and has no significant effect on myc translation; significantly inhibits myc expression when combined with ER stress inducers, especially bortezomib; shows synergistic anti-MM cytotoxicity combined with ER stress inducers; also blocks cyclin D1 IRES-dependent initiation and demonstrates synergistic anti-GBM properties combined with PP242.