thp1

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.

THP104c is an inhibitor of mitochondrial fission.

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).

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.

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.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.

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

RU.521 (RU3205217) is a potent dsDNA inhibitor (IC50 : 700 nM), inhibition of the dsDNA pathway by RU.521 requires the presence of cGAS.

VAS 3947 is a specific inhibitor of NADPH oxidase (NOX).VAS 3947 has a potent anti-platelet effect, inducing apoptosis through UPR activation, mainly due to protein aggregation and misfolding, independent of anti-NOX activity.

ML390 exerts its potent differentiation effect on multiple leukemia models.

SR-717 free acid is a stable cGAMP mimetic and non-nucleotide STING agonist, demonstrating antitumor activity with EC50 values of 2.1 μM in ISG-THP1 (WT) and 2.2 μM in ISG-THP1 cGAS KO (cGAS KO) cell lines.

Cynanoside J, a C21 steroidal glycoside derived from Cynanchum taihangense, exhibits IC50 values of 6.38, 5.82, and 6.76 μM against HL-60, THP1, and Caco2 cell lines, respectively. This compound can be utilized in cancer research [1].

Bepafant is a platelet activating factor (PAF) antagonist. Bepafant may produce significant anti-inflammatory effects. Bepafant triggered apoptosis in NB4, KG1, and NB4-MR4 cells where PTEN was expressed, but not in THP1 and U937 cells where PTEN was abse

BCL6-IN-10 (Compound WK499) is an inhibitor of BCL6 that disrupts its interaction with the SMRT protein, promoting apoptosis, cell cycle arrest, and DNA damage. It effectively hampers the proliferation of various AML cell lines, with IC50 values of 0.91, 1.63, 1.026, 7.42, 0.87, and 0.85 μM for OCI-AML3, THP1, MOLM13, HL60, KG1, and NB4 cells, respectively [1].

IQ3 is a selective inhibitor of JNK3(JNK3, JNK1 and JNK2 with Kd of 66 nM, 240 nM and 290 nM, respectively). IQ 3 inhibits NF-κB AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM, also inhibits TNF-α and IL-6 production in vitro.

NLRP3 agonist 2 (compound 22) is an orally active agent that activates Caspase-1 in THP1 cells [1].

SW2_110A acetate is a selective, cell-permeable chromobox inhibitor of homologue CBX8 (Kd = 800 nM) bound to CBX8 N-terminal color gamut (ChD). SW2_110A acetate has a high affinity for CBX8N, inhibits the association between CBX8 and cell chromatin, and inhibits the proliferation of ML-AF9-induced THP1 leukemia cells.

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.

DY-46-2 is a selective non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor (IC50: 0.39 ± 0.23 μM) with anticancer activity for the study of cancer and tumors.

STING Agonist-8 Dihydrochloride (Compound 5-AB) is a highly effective STING agonist, exhibiting an EC50 value of 27 nM in THP1-Dual KI-hSTING-R232 cells.

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).