synergistic

Rufigallol (AI3-00865) is an electron-deficient disk-shaped molecule with six hydroxyl groups and is a good unit for inducing the formation of DLC from non-planar AIE molecules, an anthraquinone derivative.Rufigallol induces the acquisition of DLC properties, while the introduction of TPE groups gives the molecular structure good fluorescence in the aggregated state.The remarkable synergistic in vitro antimalarial effect, in vivo with vitamin C and ketones was synergistic and showed antimalarial activity.

PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.

JAK3 BTk-in-2 is a potent JAK3 BTK inhibitor. JAK3 BTk-in-2 inhibits both BTK and JAK3, which are two important targets IN autoimmune diseases. JAK3 BTk-in-2 simultaneously inhibits the BTK JAK3 signaling pathway, showing a synergistic effect. JAK3 BTk-in-2 has the potential to treat diseases associated with abnormal JAK3 and BTK activity.

JAK3 BTk-in-1 is a dual JAK3 BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3 BTk-in-1 simultaneously inhibited the BTK JAK3 signaling pathway, showing a synergistic effect. JAK3 BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.

trans-Cyclohexane-1,2-diol (trans-1,2-Cyclohexanediol) has a synergistic retardation effect on percutaneous absorption and penetration of metronidazole (MTZ).

2',3'-Dideoxyuridine is a purine nucleoside analog with potential antitumor activity. Purine nucleoside analogs such as 5-hydroxymethyl-2'-deoxyuridine have synergistic anticancer effects with 5-Fluorouracil in solid tumor cell lines.

QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor. Modulates ARF-GTP levels and synergizes with the Wnt β-catenin signaling pathway to upregulate β-catenin nuclear translocation. Also reduces in vitro migration of metastatic human breast cancer cells.

Brusatol (NSC-172924) is a natural product isolated from the Brucea javanica plant. It inhibits Nrf2.

WDR5-IN-6 is a WDR5 inhibitor targeting the WBM locus and is highly synergistic with OICR-9429, a WDR5 inhibitor that targets the WIN locus. It exhibits potent antitumor activity and inhibits cell proliferation in neuroblastoma cell lines, making WDR5-IN-6 suitable for neuroblastoma research.

BAY-8400 is a potent, selective, and orally active DNA-dependent protein kinase (DNA-PK) inhibitor (IC50 = 81 nM) that demonstrates synergistic efficacy when combined with targeted alpha therapies. BAY-8400 is applicable for cancer research [1].

ATN-161 acetate, a pentapeptide compound derived from the synergistic region of fibronectin, is a non-competitive integrin-alpha5 antagonist with antitumor activity that attenuates the pathology of caerulein-induced acute pancreatitis.

Dri-c21045 showed concentration-dependent inhibition of NF- B activation and all CD40L induced by B cell proliferation. IC50 was 17.1 M and 4.5 M, respectively.Dri-c21045 is an effective selective inhibitor of CD40-CD40L synergistic stimulator protein-pro

Duocarmycin SA is an extremely potent cytotoxic agent and antitumor antibiotic that induces sequence-selective alkylation of duplex DNA, with an IC50 of 10 pM. It demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells when combined with proton radiation in vitro.

INSR agonist 1, an insulin receptor (INSR) agonist, effectively elevates INSR pY1355 1361 levels and exhibits synergistic effects with insulin.

OES2-0017 exhibits strong synergistic effects and growth inhibition in collaboration with polyamines within a low micromolar range. At low concentrations, OES2-0017 inhibits spermidine spermine N1-acetyltransferase (SpeG) (IC50: 34.82 μM) and other polyamine detoxifying enzymes, while at higher concentrations, it disrupts bacterial membranes.

PRMT5-MTA-IN-2 (compound 1) is a synergistic inhibitor of PRMT5 with an IC50 of less than 1.5 nM.

MTI013 is a selective inhibitor of SARS-CoV-2 nsp14 Mtase (IC50: 2.98 µM) and an antiviral agent (IC50: 10.33 µM in HCoV-229E infected Huh7 cells). Additionally, MTI013 demonstrates synergistic antiviral effects when used in conjunction with the RdRp inhibitor SHEN26.

ZG-2033 (Compound 26) is an orally active HIF-2α agonist that exhibits nanomolar activity (EC50 = 490 nM) in a luciferase reporter assay. It demonstrates an anti-anemic effect and shows synergistic effects with AKB-6548 in anemia, making it useful for the study of renal anemia.

MC3343, a DNMT inhibitor with IC50 values of 5.7 μM for DNMT1 and 1.7 μM for DNMT3a, affects tumor proliferation by blocking osteosarcoma cells in the G1 or G2 M phase and induces osteogenic differentiation by specifically re-expressing genes that regulate this physiological process, and is able to show synergistic effects in combination with adriamycin and cisplatin (CDDP).

PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader specifically targeting PARP1, with a DC50 of 58.14 nM. It demonstrates cytotoxicity in SW-620 and LOVO cancer cells, with IC50 values of 1.63 μM and 2.84 μM, respectively. In BRCA-mutated colon cancer cells, PROTAC PARP1 degrader-3 exhibits synergistic effects with SN-38, with a combination index (CI) of 0.487.

HPK1-IN-54 (Compound 16) is a potent inhibitor of HPK1 (hematopoietic progenitor kinase 1), enhancing T cell activation and proliferation by blocking HPK1 activity to exert antitumor effects. It has an IC50 of 2.67 nM for HPK1, showing excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 exhibits moderate in vivo clearance and reasonable oral exposure in both mice and rats. Additionally, in the CT26 mouse colon cancer model, HPK1-IN-54 demonstrates significant antitumor activity and shows a synergistic effect when combined with anti-PD-1 therapy. HPK1-IN-54 holds promise for research in the field of immunology.

AKT-IN-24 (Compound M17) is an allosteric inhibitor of AKT exhibiting antitumor activity. In combination with Trametinib, it targets the AKT mTOR and MEK ERK signaling pathways while inhibiting epithelial-mesenchymal transition, resulting in a synergistic suppression effect on TNBC. This combination promotes apoptosis and inhibits cell proliferation and migration.

RdRP-IN-9 (Compound 6b) is a reversible covalent allosteric inhibitor of RdRp, demonstrating substantial anti-coronavirus activity with an EC50 of 0.68 μM against HCoV-OC43. By reversibly acylating the Cys12 in the NiRAN domain of non-structural protein 12 (nsp 12), it exerts prolonged antiviral effects and shows synergistic anti-coronavirus activity with Molnupiravir.

Conteltinibtetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride form of Conteltinib. It acts as an inhibitor for FAK (IC50=1.6 nM), ALK, and Pyk2. When used in combination with Cabozantinib, Conteltinib tetrahydrochloride exhibits a synergistic antitumor effect.