thp1

ML390 exerts its potent differentiation effect on multiple leukemia models.

G150 inhibited interferon expression triggered by DSDNA with IC50 of 10.2 nM.G150 is an effective and highly selective inhibitor of human cyclic GMP-AMP synthase (H-CGAS).

SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a "closed" activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens.

THP1 Lipid is an ionizable lipid utilized in the synthesis of lipid nanoparticles (LNPs) for mRNA delivery to muscle tissue, exhibiting extremely low toxicity. In tdTomato transgenic mice, it facilitates the editing of specific genes in liver tissue. Additionally, THP1 Lipid is employed in vaccine delivery and studies involving CRISPR/Cas9-mediated gene editing.

THP104c is an inhibitor of mitochondrial fission.

Damascenone is a mixture of E- and Z-isomer damascenones, characteristic compounds with anti-inflammatory properties derived from Epipremnum pinnatum.

Piribedil (Trivastan) is a dopamine D2 agonist, used in the treatment of Parkinson's disease.

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity, showing potential as a first-in-class candidate in AML [Acute Myeloid Leukemia].

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

R1487 Hydrochloride is an orally available, selective and potent inhibitor of mitogen-activated protein kinase (p38α) for the study of metabolic diseases.

m-3M3FBS is a phospholipase C (PLC) activator.

AI-10-47 (1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47) is a small molecule inhibitor of CBFβ-RUNX binding(IC50 : 3.2 μM).

Andrograpanin (19-HYDROXY-8(17),13-LABDADIEN-16,15-OLIDE) is a bioactive compound from Andrographis paniculata. Andrograpanin has anti-inflammatory and anti-infectious properties.

Adalimumab (anti-TNF-alpha) is the first fully human recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

Compound 3 (diABZI-V/C-DBCO) functions as an efficient STING agonist. This compound acts by releasing diABZI-amine under the action of cathepsin B to activate STING, thereby inducing the production of interferon and other immune-activating molecules, which enhances the immune system's response to tumors. In THP1-Dual cells, the EC50 values for STING activation by diABZI-V/C-DBCO and diABZI-amine are 1.47 nM and 0.144 nM, respectively, and in primary mouse splenic cells, the EC50 values are 7.7 µM and 0.17 µM, respectively. diABZI-V/C-DBCO is useful for research in the field of cancer immunotherapy.

STING-IN-12 (compound Y2) acts as an inhibitor of STING. It suppresses IFNβ gene expression induced by SR717 with an IC50 of 0.75 μM. Additionally, STING-IN-12 inhibits STING pathway activation induced by the STING agonist SR717 in THP1 cells and by MSA-2 in mice.

STING-IN-14 is a STING inhibitor with an IC50 of 0.6 nM. It effectively suppresses the activation of the IRF pathway in THP1-DualTM cells. This compound is applicable in research related to autoimmune diseases.

STINGagonist-42 (compound 8a) is a potent STING agonist. It activates STING in THP1 and RAW 264.7 cells, with EC50 values of 0.06 μM and 14.15 μM, respectively.

Antiparasitic agent-22 (Compound 24) is a broad-spectrum antiparasitic compound that inhibits the procyclic form of T. brucei, L. infantum, and L. tropica with IC50 values of 2.41, 5.95, and 8.98 μM, respectively, and the amastigote form of L. infantum with an IC50 of 8.18 μM. It also shows inhibitory activity against the P. falciparum W2 strain with an IC50 of 0.155 μM. Additionally, Antiparasitic agent-22 exhibits low cytotoxicity in THP1 cells, with a CC50 of 64.16 μM.

Cisplatin/Dasatinib prodrug-1 (Compound 3) is a precursor drug for Cisplatin and Dasatinib. It exhibits antiproliferative activity against tumor cell lines A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1, and HL60, with IC50 values of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3, and 0.25 μM, respectively.

Leuxinostat, an inhibitor of HDAC, exhibits an IC50 of 30 nM against hHDAC6. It suppresses the proliferation of THP1, K562, U937, and MEK1 cells, while also inducing apoptosis in leukemia cells NB4 and MOLT-4. Additionally, Leuxinostat inhibits the expansion of hematopoietic stem cells and demonstrates anti-leukemic activity in a zebrafish model.

STINGagonist-44 (Compound 4) is a potent and selective STING agonist with an EC50 value of 5.68 μM in THP1 cells and 2.212 μM in RAW cells for inducing IRF. It activates the STING pathway, leading to the production of type I interferons and pro-inflammatory cytokines (e.g., CXCL10, TNFα). STINGagonist-44 holds promise for cancer research.