α-Obscurine derivative-1 (Compound 7) is a α-Obscurine derivative. α-Obscurine derivative-1 inhibits CaV3.1 ion channel current with an IC50 of 0.19 μM. α-Obscurine derivative-1 can be used in the research of neurological disorders.

α-Glucosidase-IN-113 is an α-glucosidase inhibitor with an IC50 of 17.52 μM. α-Glucosidase-IN-113 shows antiglycating activity and inhibits advanced glycation end-product formation. α-Glucosidase-IN-113 can be used for the research of type 2 diabetes.

Xanthine oxidase-IN-22 is an orally active inhibitor of xanthine oxidase (XO) (IC50: 0.0034 μM). Xanthine oxidase-IN-22 exhibits a mixed-type inhibition mode against XO. Xanthine oxidase-IN-22 reduces serum uric acid levels in mice. Xanthine oxidase-IN-22 can be used in research related to hyperuricemia and gout.

WIN 64338 is a non-peptide bradykinin B2 receptor antagonist. WIN 64338 can inhibit bradykinin-evoked trigeminal nerve stimulation.

Valyllysine (Val-Lys) is a renoprotective peptide. Valyllysine can be found in G. chorda soluble proteins following hydrolysis by thermolysin. Valyllysine effectively ameliorates pathological renal injury.

Tyk2-IN-23 is a potent, orally active, selective TYK2 inhibitor (IC50 = 18 nM), exhibiting more than > 70-fold selectivity over JAK1/2/3 isoforms. Tyk2-IN-23 potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α and IL-10. Tyk2-IN-23 potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells. Tyk2-IN-23 can be used for the study of alopecia areata and allergic Rhinitis.

Topoisomerase ll/ME-1-IN-1 (Compound 7a) is a Topoisomerase ll and ME-1 inhibitor with an IC50 of 5.03 μM against Topoisomerase ll. Topoisomerase ll/ME-1-IN-1 functionally inhibits the activity of Topoisomerase II and functionally blocks the activity of ME-1. Topoisomerase ll/ME-1-IN-1 induces Autophagy by upregulating the expression of Beclin-1 and LC3-II. Topoisomerase ll/ME-1-IN-1 promotes Apoptosis. Topoisomerase ll/ME-1-IN-1 exhibits antiproliferative activity against breast cancer cells and shows no toxicity to normal mammary epithelial cells. Topoisomerase ll/ME-1-IN-1 can be used in studies related to breast cancer (including triple-negative breast cancer).

TIPARP-IN-1 (Compound 15) is a selective PARP7 (TIPARP) (2,3,7,8-Tetrachlorodiben-zo-p-dioxin(TCDD)-inducible PARP) inhibitor with an IC50 of 2.15 nM. TIPARP-IN-1 can restore IFN signaling pathway in tumors by inhibiting TIPARP. TIPARP-IN-1 selectively activates the anti-tumor immune response in the tumor microenvironment and avoids the production of systemic cytokines. TIPARP-IN-1 can be used for research of head and neck squamous cell carcinoma.

TBC-4746 is a α4β1/α4β7 integrin antagonist. TBC-4746 can be used in the research of asthma and multiple sclerosis.

T3SS-IN-6 is a thiazolidin-2-cyanamide derivative and type III secretion system (T3SS) inhibitor targeting Xanthomonas oryzae pv. oryzae (Xoo). T3SS-IN-6 exhibits no effect on Xoo growth. T3SS-IN-6 shows no measurable acute toxicity to silkworms and earthworms.

STAT6 degrader-1 (Compound 21) is a bifunctional molecular glue degrader of STAT6 that recruits E3 ubiquitin ligase. STAT6 degrader-1 induces proteasomal degradation of STAT6. STAT6 degrader-1 is applicable to the research of cancer, inflammatory diseases and colorectal cancer.

SM-11044 is a β-adrenoceptor agonist with Ki values of 18.1 μM (β1), 4.1 μM (β2) and 1.3 μM (β3), showing higher binding selectivity for the β3-adrenoceptor. SM-11044 stimulates cAMP accumulation in cells expressing this receptor. SM-11044 mediates ileal relaxation, tracheal relaxation, pulmonary parenchymal relaxation, increased right atrial heart rate and adipocyte lipolysis.

SK-129 is a blood-brain barrier-permeable inhibitor of α-synuclein (αS) oligomers with a Kd of 221 nM. SK-129 preferentially binds to neurotoxic αS oligomers over physiological αS monomers, inhibits αS aggregation, blocks the interaction and co-aggregation of αS with tau protein, and prevents the maturation of αS-tau condensates into amyloid aggregates. SK-129 reduces ROS production, rescues dopaminergic neuron degeneration, improves motor function, restores endogenous dopamine synthesis, increases the number of Tyrosine Hydroxylase-positive neurons, prevents brain histopathological changes, alleviates neuroinflammation, and improves survival rates in relevant models. SK-129 can be used in research related to Parkinson's disease (PD) and Lewy body dementia (LBD).

SCH-720881 is the active metabolite of Rolapitant. Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model.

PROTAC SARS-CoV-2 Mpro degrader-8 is an antiviral PROTAC degrader targeting the SARS-CoV-2 main protease (Mpro), with weak direct binding affinity to Mpro (Kd=80.5 μM). PROTAC SARS-CoV-2 Mpro degrader-8 exhibits broad-spectrum antiviral activity against SARS-CoV-2 and the human endemic coronavirus HCoV-OC43. It can be used for research on coronavirus infections. (Pink: SARS-CoV Target protein ligand; Blue: VHL ligand ; Black: ).

PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-14 is an EZH2 PROTAC degrader, with an IC50 of 18.21 μM against diffuse large B-cell lymphoma cells, and exhibits no antiproliferative activity against non-target cells at concentrations up to 30.00 μM. PROTAC EZH2 Degrader-14 can be used in studies related to diffuse large B-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).

PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research. (Pink: CDK2 and CDK4 and CDK6 ligand ; Blue: Cereblon ligand ; Black: linker).

PPARγ agonist-22 is a PPARγ agonist. PPARγ agonist-22 promotes cellular glucose uptake. PPARγ agonist-22 reduces lipid accumulation in adipocytes. PPARγ agonist-22 can be used in the research of type 2 diabetes.

PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies.

Parsalmide is an orally active non-steroidal anti-inflammatory drug and gastroprotective agent, with an IC50 of 9.92 μM against COX-1 and 155 μM against COX-2. Parsalmide prevents gastric injury and reduces edema. Parsalmide can be used in the research of arthritis.

Pantothenate kinase-IN-3 is a PANK3-selective binder and CoA biosynthesis activator with a human PANK3 Ki of 9.1 nM, human PANK3 Ka of 1.8 nM, human PANK1β Ki of 113 nM, human PANK1β Ka of 23.4 nM, and oral effectiveness.Pantothenate kinase-IN-3 binds PANK3 via a water-mediated interaction between its sulfonamide NH and Gly193, elevates cellular, hepatic, and forebrain CoA levels, and shows improved metabolic stability in mouse and human microsomes.Pantothenate kinase-IN-3 has solubility properties favorable at pH 7.Pantothenate kinase-IN-3 can be used for the research of hepatic metabolic CoA deficiencies (acidemias).

OCA 983 is an orally active tetrahydrofuranyl 1β-methylcarbapenem antibiotic. OCA 983 exhibits potent inhibitory activity against class A and class C β-lactamases. OCA 983 possesses a broad antibacterial spectrum, and can be used in the research of infectious diseases.

N-Phosphotaurocyamine (Taurocyamine phosphate) is a phosphagen in Arenicola, the stores of phosphotaurocyamine are an energy source which can be used for rapid regeneration of ATP.

Neoambrosin is a sesquiterpene lactone. Neoambrosin acts as a partial agonist of PPARγ and TRPA1 receptors, with no carbonic anhydrase inhibitory activity. Neoambrosin can be used in research on hypoglycemia, analgesia, anti-inflammation and anticancer effects.

NecroX-5 free base is a derivative of the NecroX, reduces intracellular calcium concentration, and possesses anti-inflammatory and anti-cancer activity.

Necopidem (Compound 6) is a GABA A receptor modulator. Necopidem can be used in research on neurological disorders such as anxiety.

MS8815N is a negative control of EZH2 PROTAC degrader MS8815. MS8815N is incapable of recruiting the VHL E3 ligase but retains the same EZH2 binding moiety and linker. MS8815N can be used for triple-negative breast cancer (TNBC) research.

MS6178 is a MS5105-based CFTR deubiquitinase-targeted chimera (DUBTAC) that recruits OTUB1 to stabilize ΔF508-CFTR mutant protein in a concentration- and time-dependent manner, with an OTUB1-dependent effect and no impact on CFTR mRNA level. MS6178 can be used for the research of cancer.

MPAM-15 is a blood-brain barrier-penetrant pan-orthosteric allosteric modulator (PAM) of opioid receptors, with ≥16-fold selectivity for μOR over δOR and κOR. MPAM-15 acts as an anti-nociceptive potentiator and analgesic, and its activity is observed in mouse models via both intracerebroventricular and intraperitoneal administration. MPAM-15 is applicable for pain-related research.