AMPA-IN-1 is a potent inhibitor of AMPA receptor. AMPA receptors are receptors that are widely expressed in the brain, and play a central role in the regulation of fast excitatory synaptic transmission and synaptic plasticity. AMPA-IN-1 has the potential for the research of various central diseases including epilepsy (extracted from patent WO2017082288A1, compound 14).

(R)-CPP is a highly potent NMDA receptor antagonist.

epi-Aszonalenin A is a benzodiazepine fungal metabolite originally isolated from Aspergillus novofumigatus. epi-Aszonalenin A can be used as a psychoactive agent.

TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats.

3α,21-Dihydroxy-5α-pregnan-20-one-d3 (THDOC-d3) is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity.

TTA-P1 is a potent state-independent compound inhibiting human T-type calcium channel. T-type calcium channels play a role in diverse physiological responses including neuronal burst firing, hormone secretion, and cell growth. TTA-P1 has the potential for the research of absence epilepsy.

2-NP is a selective enhancer of STAT1 transcription. 2-NP can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells.

STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182).

5,15-Diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist (IC50s of 0.28 µM and 10 µM for STAT3 and STAT1, respectively).

Danvatirsen is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth.

Tofacitinib Prodrug-1 is an effective and oral active prodrug to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib Prodrug-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib Prodrug-1 is a potential drug candidate for the treatment of ulcerative colitis.

JAK-IN-19 is a potent JAK inhibitor (PBMC IFNγ pIC50=7.2 and HLF Eotaxin pIC50=7.7). JAK-IN-19 has good retentive properties in the lung via mitigating being metabolized by Aldehyde Oxidase (AO), with diminished VEGFR2 selectivity (VEGFR2 pIC50=7.0, Aurora B pIC50=5.8).

JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.

JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity.

Hydroxyphenyl fluorescein (HPF) is the reagent that can directly detect highly reactive oxygen species (hROS). Hydroxyphenyl fluorescein selectively and dose-dependently reacts with hROS, such as the hydroxyl radical and peroxynitrite, which exhibit strong fluorescence.

RIDR-PI-103 is a reactive oxygen species (ROS)-induced drug release prodrug with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103).

L-Ascorbic acid-13C (L-Ascorbate-13C) is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

L-Ascorbic acid-13C6 (L-Ascorbate-13C6) is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC50s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders.

TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.

DB-3-291 is potent and selective CSK degrader, with a Kd of 1 nM.

SM-360320 (CL-087) is a potent, oral actively TLR7 agonist. SM-360320 is a mmuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.

TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders.

STING agonist-8 is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells (WO2021239068A1, compound 5-AB).

IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma.

[D-Leu-4]-OB3 inhibits expressions of pro-inflammatory, proliferative and metastatic genes and PD-L1 expression. [D-Leu-4]-OB3 stimulates expression of pro-apoptotic genes.

PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC50 of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1.

NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body's intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3).

IRAK4-IN-8 (VI-177) is a potent IRAK4 inhibitor.