σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1R Ki of 8.8 nM and an H3R Ki of 31.2 nM. Through the dual action of simultaneously antagonizing σ1R and H3R, σ1R/H3R ligand-1 exhibits potent dose-dependent analgesic activity in mouse models of visceral pain and neuropathic pain. σ1R/H3R ligand-1 can be used for the research of visceral pain and neuropathic pain.

Topoisomerase IV-IN-3 is a Staphylococcus aureus Topoisomerase IV inhibitor, DNA gyrase inhibitor and antibacterial agent. Topoisomerase IV-IN-3 has IC50 values of 1.32 μM and 0.48 μM against topoisomerase IV, and 0.88 μM and 0.54 μM against DNA gyrase. Topoisomerase IV-IN-3 inhibits decatenation, ATPase, and supercoiling activities of its target enzymes. Topoisomerase IV-IN-3 exerts antibacterial activity against Gram-positive and Gram-negative bacterial strains. Topoisomerase IV-IN-3 exhibits low cytotoxicity toward human fibroblast cells. Topoisomerase IV-IN-3 can be used for the research of bacterial infections.

TLR2/9 antagonist 1 (Compound 24) is a reversible covalent TLR2 (IC₅₀ = 0.5 μM (TLR2/TLR6); IC₅₀ = 0.6 μM (TLR2/TLR1)) and TLR9 (IC₅₀ = 0.32 μM) antagonist. TLR2/9 antagonist 1 has no significant effect on other TLR subtypes. TLR2/9 antagonist 1 can be used for studying central nervous system diseases and malignant tumors caused by inflammation.

Palmitoyl glutathione is a palmitoylated peptide derivative and a liver-targeted liposome-forming agent. Palmitoyl glutathione can form liposome-like vesicles with cholesterol, which can encapsulate water-soluble solutes and remain stable in fresh Rattus norvegicus (rat) plasma at 37°C. Palmitoyl glutathione can be used in studies related to acetaminophen-induced liver necrosis.

NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD).

NHWL071065 is a IKZF1/IKZF3 degrader. NHWL071065 selectively degrades IKZF1 and IKZF3 in lymphoma cells via the ubiquitin-proteasome pathway. NHWL071065 inhibits the proliferation of lymphoma cells. NHWL071065 downregulates proteins involved in cytoskeleton assembly, cell adhesion and immune regulation in cells, while upregulating proteins related to the type I IFN signaling pathway. NHWL071065 can be used in the research of lymphoma.

ND-654 is a highly selective acetyl-CoA carboxylase (ACC) inhibitor (IC50: ACC1=3 nM, ACC2=8 nM). ND-654 reduces hepatic lipogenesis, decreases neutrophil recruitment and promotes anti-inflammatory M2 macrophage polarization. ND-654 is promising for research of nonalcoholic steatohepatitis and hepatocellular carcinoma.

MLS-2384 free base is a dual JAK/Src kinase inhibitor. MLS-2384 free base downregulates STAT3 downstream proteins c-Myc and Mcl-1. MLS-2384 free base induces Apoptosis. MLS-2384 free base exhibits anticancer activity against prostate cancer, breast cancer, skin cancer, ovarian cancer, lung cancer, and liver cancer.

KTT-1 is a kinetically selective and orally active HDAC2 inhibitor. KTT-1 exhibits high HDAC2-selectivity over HDAC1. KTT-1 inhibits osteoclast differentiation at an early stage by downregulating c-Fos expression. KTT-1 effectively suppresses arthritis symptoms in the collagen-induced arthritis (CIA) mouse model. KTT-1 can be used for the research of rheumatoid arthritis and neurodegenerative diseases.

KRP-203 monophosphate is a monophosphate of KRP-203. KRP-203 is an orally active sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs.

JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease.

IHCH-3185 is an orally active class I HDAC inhibitor (HDAC1 IC50 =102.9 nM) and A2AR antagonist (A2AR Ki =7.6 nM). IHCH-3185 reverses immune gene silencing by inducing histone acetylation and blocks the adenosine signaling pathway to relieve T-cell suppression. IHCH-3185 exhibits antiproliferative activity, induces cell cycle arrest, and significantly improves the tumor microenvironment. IHCH-3185 reduces the proportion of regulatory T cells, increases the CD8+/Treg ratio, and upregulates the expression of key factors such as H2-K1, Cxcl9 and Cxcl10. IHCH-3185 shows significant antitumor potential in CT26 and MC38 mouse tumor models and is suitable for related cancer research.

Dihydro-α-ionone is a volatile compound found in the essential oil of Persicaria hydropiper L. leaves. The essential oil can inhibit α-glucosidase and α-amylase activities.

Cryptophycin 52 (LY355703) is a synthesized 16-membered cyclic ester peptide compound and is a derivative of marine natural product cryptophycin 1 with antitumor activity. Cryptophycin 52 can induce cells G2/M phase arrest. Cryptophycin 52 is also effective for solid tumors that are resistant to Paclitaxel and Doxorubicin. Cryptophycin 52 can be used for the research of cancer, such as multidrug-resistant tumor.

COX-2/Aromatase-IN-2 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-2 can simultaneously inhibit COX-2 and aromatase, suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-2 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-2 can be used for the study of inflammation and breast cancer.

BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC).

1,3-Palmitin-2-laurin is an acylglycerol.

ISM5939 is an orally active and selective ENPP1 inhibitor with an IC50 of 0.63 nM for 2,3-cGAMP degradation and 9.28 nM for ATP hydrolysis. ISM5939 has antitumor activity.

ORG-20241 is a PDE3/PDE4 dual inhibitor. ORG-20241 has a significant bronchodilator effect and completely prevents allergen induced airway hyperresponsiveness. ORG-20241 can significantly inhibit eosinophil infiltration at high concentrations. ORG-20241 can be used for research on asthma.

Vizenpistat is an ENPP1 inhibitor that can be used in the study of cancer.

CK-2289 is an inhibitor of type III cyclic 3'5'-adenosine monophosphate phosphodiesterase (PDE). CK-2289 can inhibit platelet aggregation and decreases mean arterial blood pressure. CK-2289 can be used for the research of cardiovascular disease, such as congestive heart failure.

BMY 20844 is an orally active platelet cAMP phosphodiesterase inhibitor with anti-thrombosis activity. BMY 20844 can elevate cAMP levels and activate protein kinase in platelets. BMY 20844 can be used for the research of cardiovascular disease.

UK-371800 is a highly selective PDE5 inhibitor (IC50 = 4.2 nM). UK-371800 has good permeability and is not affected by the efflux of P-glycoprotein.

KF-17625 is an orally active bronchodilator. KF-17625 can inhibit bronchoconstriction induced by Carbachol, Histamine, or Leukotriene D4. KF-17625 can inhibit canine tracheal phosphodiesterase (PDE) IV (IC50 = 12 μM) and Concanavalin-A-induced histamine release from rat mast cells (44% inhibition at 10 mM). KF-17625 can be used for the researches of immunology and inflammation.

OPC-33540 is a highly selective and competitive PDE3 inhibitor with IC50 values of 0.32 nM (PDE3A) and 1.5 nM (PDE3B). OPC-33540 exhibits IC50s against PDE1, PDE2, PDE4, PDE5, and PDE7 of 42.9, 52.3, 100.8, 2.5, and 51.3 μM, respectively. OPC-33540 significantly enhances cAMP accumulation in platelets and effectively inhibits thrombin-induced platelet aggregation. OPC-33540 can be used in antithrombotic studies.

(R)-Xanthoanthrafil is a phosphodiesterase-5 (PDE5) inhibitor. (R)-Xanthoanthrafil selectively inhibits PDE5, increasing cyclic guanosine monophosphate (cGMP) levels, leading to smooth muscle relaxation and promoting penile erection. (R)-Xanthoanthrafil can be used to study erectile dysfunction.

KD-027 (SLx-2101) is a Phosphodiesterase 5 (PDE5) inhibitor. KD-027 can be used for endothelial dysfunction, and hypertension research.

CC-3052 is a phosphodiesterase 4 (PDE4) inhibitor with immunomodulatory activities. CC-3052 reduces neutrophil apoptosis in HIV⁺. CC-3052 is promising for research of HIV-related diseases.

FR-181074 is a selective and orally active PDE V inhibitor. FR-181074 can specifically block PDE V to inhibit the degradation of cyclic guanosine monophosphate (cGMP) in order to relax smooth muscle. FR-181074 can be used for the research of cardiovascular disease and endocrinology, such as hypertension and erectile dysfunction.

BL-122 is a selective phosphodiesterase-5 (PDE-5) inhibitor. BL-122 can increase the level of cGMP in the tissue, promote the expression of nitric oxide (NO), and mediate the relaxation of smooth muscle. BL-122 can be used for the researches of inflammation, immunology and cardiovascular disease, such as asthma and hypertension.