STAT3-IN-13 (compound 6f) is a STAT3 inhibitor. It exhibits anti-proliferative activity and binds to the STAT3 SH2 domain with a KD of 0.46 μM. This compound inhibits STAT3 Y705 phosphorylation and downstream target gene expression. In vitro studies show STAT3-IN-13 induces apoptosis, while in vivo experiments demonstrate its ability to suppress tumor growth and metastasis. STAT3-IN-13 has potential applications in cancer research.

STAT3-IN-12 is a potent inhibitor of STAT3signaling, by effectively blocking IL-6-induced activation of the JAK/STAT3 pathway. STAT3-IN-12 suppresses cancer cell proliferation and migration, while promoting apoptosis and inducing cell cycle arrest.

YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer.

STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer.

SGK1-IN-9 (Compound 1) is a SGK1 inhibitor. SGK1-IN-9 can be used in cancer research.

S1PR1/S1PR5 agonist-1 (Compound 19) is an orally active S1PR1 and S1PR5 agonist with EC50 values of 40.0 and 22.9 nM, respectively. S1PR1/S1PR5 agonist-1 binds to key residues of S1PR1 to mediate agonistic activity. S1PR1/S1PR5 agonist-1 alleviates colitis pathological changes in DSS-induced mouse models and exerts minimal effects on mouse heart rate. S1PR1/S1PR5 agonist-1 can be used for the research of inflammatory bowel disease.

PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer. (Pink: EZH2 ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).

PARP1-IN-51 (P55 the second compound in the fifth row) is a PARP1 inhibitor. PARP1-IN-51 can be used for the research of cancer, such as breast cancer.

OT-7100 is an orally active analgesic agent. OT-7100 inhibits hyperalgesia possibly by enhancing adenosinergic neurotransmission in the dorsal horn. OT-7100 can be used for the researches of inflammation, neurological and metabolic disease such as diabetes2].

NIP 502 is a pyridazinone derivative with orally active anti-inflammation and anti-immunology effects. NIP 502 can be used for the research of asthma.

GRM1 modulator-1 is a GRM1 modulator.

Fmoc-Asp(OtBu)-OH-15N is the 15N-labeled Fmoc-Asp(OtBu)-OH. Fmoc-Asp(OtBu)-OH (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate) is an aspartate derivative containing amine protecting group Fmoc. Fmoc-Asp(OtBu)-OH can be used for peptide synthesis.

DNMT-IN-6 is a DNA methyltransferase inhibitor with activity against DNMT1, DNMT3A, and DNMT3B. DNMT-IN-6 drives demethylation, and restores TMS1 tumor suppressor gene expression. DNMT-IN-6 induces apoptosis, causes G2/M phase arrest, disrupts mitochondrial integrity, and activates the intrinsic caspase cascade (3/7/9). DNMT-IN-6 inhibits tumor growth, and improves survival in xenograft models. DNMT-IN-6 can be used for the research of cancer, such as diffuse large B-cell lymphoma.

DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia.

DHX9-IN-21 (Compound 635) is a DHX9 inhibitor with an IC50 of 2 nM; its EC50 at the cellular level is 19.1 nM. DHX9-IN-21 exhibits antiproliferative activity against LS411N (CRC-MSI-H), with an IC50 value of 79.2 nM. DHX9-IN-21 can be used for the research of microsatellite unstable colorectal cancer.

CTR/AMYR modulator-1 is a calcitonin receptor/amylin receptor modulator. CTR/AMYR modulator-1 can be used for the research of metabolic disease.

Cathepsin L-IN-6 (Compound 6a) is a selective cathepsin L inhibitor with an IC50 of 0.021 μM. Cathepsin L-IN-6 suppresses cathepsin L activity by directly binding to cathepsin L. Cathepsin L-IN-6 inhibits IL-6 and IL-8. Cathepsin L-IN-6 shows a high anti-inflammatory activity. Cathepsin L-IN-6 can be used in the research of acute lung injury.

Anti-MRSA agent 36 (Compound III13) is an antibacterial agent with strong anti MRSA activity (MIC = 1 μg/mL). Anti-MRSA agent 36 targets phosphatidylglycerol (PG) on bacterial membranes, disrupting membrane integrity, leading to DNA leakage and increased ROS. Anti-MRSA agent 36 has advantages such as low cytotoxicity, low hemolysis, difficulty in inducing drug resistance, and good plasma stability. Anti-MRSA agent 36 can be used for the study of skin abscess and systemic infection models.

ALX-5407 ((R)-NFPS) is a selective and orally active glycine transporter GlyT1 inhibitor with an IC50 value of 3 nM. ALX-5407 can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia.

JP-11646 is a novel potent, selective, non-ATP competitive Pim2 inhibitor with IC50 of 0.5/1/24 nM for Pim2/3/1, respectively; shows less potency for other kinases in a kinase selectivity panel; exhibits 4-760-fold greater suppression of MM proliferation and viability than ATP-competitive PIM inhibitors; significant reduces tumor burden and increases median survival in xenogeneic myeloma murine models.

Voderdeucitinib (Compoudn I) is a TYK2 inhibitor with an anti-inflammatory activity. Voderdeucitinib can be used for inflammatory and autoimmune disease research, such as rheumatoid arthritis (RA), multiple sclerosis and intestinal bowel disease (IBD).

Butyzamide (GMP) is Butyzamide) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of platelets in mouse xenotransplantation assay.

WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research.

YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer.

(Rac)-TUL01101 (Compound I) is a selective JAK kinase inhibitor. (Rac)-TUL01101 can be used in the research of various diseases such as rheumatoid arthritis, atopic dermatitis, and alopecia areata.

Quecitinib (QY201) is an orally active JAK1/TYK2 dual inhibitor. Quecitinib is also a substrate of cytochrome P450 3A and is mainly metabolized to mono-oxide and glucuronidation products. Quecitinib has favorable pharmacokinetic properties as well as safety. Quecitinib can be used in the research of atopic dermatitis and other autoimmune diseases.

Modzatinib (ITK kinase-IN-1) (compound I) is an inhibitor targeting ITK kinase (IC50=8 nM, Jurkat cells) and can be used to study inflammatory diseases. Modzatinib has an IC50 of 23 nM for JAK3 in hPBMC cells (based on IL-2/pSTAT5 levels), wihout inhibitory effect against JAK2.

Socrodeucitinib (Compound Example 58) is an orally active and selective tyrosine kinase 2 (TYK2) inhibitor with an IC50 value of 1.41 nM. Socrodeucitinib exerts anti-inflammatory activity by inhibiting TYK2-mediated cytokine signaling pathways and reducing the secretion of inflammatory factors. Socrodeucitinib is promising for research of autoimmune diseases such as psoriasis and inflammatory diseases.

DEL1187-126-28-16 is a JAK3 inhibitor with IC50s of 10 and 0.97 nM against JAK3 WT in 0 and 60 min. DEL1187-126-28-16 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-28-16 can be used for the study of immune-mediated diseases.

KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.