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.

MMP-9-IN-13 (Example 1) is a selective inhibitor of human MMP9 with an IC50 value of 0.02 nM. MMP-9-IN-13 can be used in the research of ocular surface.

Man-GIcNAc-oxazoline (compound 6) is an N-acetylglucosamine (GlcNAc) and azide-modified disaccharide that can be used to label antibodies. Man-GIcNAc-oxazoline can be synthesized as an ADC via click chemistry.

LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto. (Pink: CCR2 ligand ; Blue: Cereblon ligand ; Black: linker).

Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

Largazole thiol, the active form of Largazole, is a potent, selective and brain-penetrant class I HDAC inhibitor. Largazole thiol. Largazole thiol exerts antitumor and neuroprotective effects. Largazole thiol can be used for research of Glioblastoma.

IDH1 ligand 1 (Compound 18) can serve as a negative control for the IDH1 target, with no detectable affinity for wild-type IDH1 and an IC50 >10,000 nM.

HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.

GSPT2 degrader-1 (compound 619) is a selective molecular glue GSPT2 degrader targeting GSPT2. GSPT2 degrader-1 contains Thalidomide and the linker of MDEG-541. GSPT2 degrader-1 induces the degradation, but not GSPT1 or myelocytomatosis oncogene (MYC). GSPT2 degrader-1 can be used for research of gastrointestinal cancer.

GSK190937 is a type II platelet-derived growth factor receptor alpha (PDGFRA) human kinase inhibitor with antimalarial activity. GSK190937 can inhibit the formation of hemozoin in the malaria parasite, resulting in the accumulation of free hemoglobin within the malaria parasite. GSK190937 shows IC50 values of 0.22, 0.59 and 0.25 μM against P. falciparum NF54, K1 and Dd2 parasite. GSK190937 shows an IC50 of 25 μM for CHO cells. GSK190937 can be used for research of malaria.

GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a KD of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer.

FXR agonist 16 is a FXR agonist with an EC50 of 2.2 μM. FXR agonist 16 activates FXR transcriptional activity, upregulates SHP and BSEP, and downregulates Cyp7a1. FXR agonist 16 exhibits hepatoprotective activity and reduces AST and ALT levels in free fatty acid-induced hepatocellular injury models. FXR agonist 16 can be used for the research of liver injury.

Feruloyl-CoA (Feruloyl-coenzyme A) is a cinnamoyl-CoA ester substrate involved in the biosynthesis of lignin and coumarin in plants. Feruloyl-CoA acts as a substrate for cinnamoyl-CoA reductase 1-dependent reduction reaction with NADPH to produce cinnamaldehyde. Feruloyl-CoA is a precursor that generates Scopoletin via spontaneous trans/cis isomerization and lactonization of its side chain.

FBPase-IN-6 (Compound 96) is an orally active FBPase inhibitor with an IC50 value of 1.769 μM. FBPase-IN-6 modulates AMPK/mTORC1/S6K signaling pathways. FBPase-IN-6 improves glucose tolerance, enhances insulin sensitivity, and promotes insulin secretion in type 2 diabetic mice.

Farabursen (RGLS8429; RG1015) is a blood-brain barrier-permeable miR-17 inhibitor. Farabursen derepresses Pkd1 and Pkd2, the target genes of miR-17, increases the levels of PC1 and PC2, and reduces cyst growth. Farabursen decreases renal cyst growth, kidney weight-to-body weight ratio, cyst index, proliferation index, and blood urea nitrogen levels in mouse models. Farabursen is applicable to research related to autosomal dominant polycystic kidney disease.

Dotarizine is a novel Piperazine derivative and antimigraine agent. Dotarizine exhibits Ca2+ channel blocking properties. Dotarizine decreases the release of lactate dehydrogenase. Dotarizine shows 5-HT receptor blocking effect.

DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA. DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure.

DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells, with no activation of EPAC2 or PKA. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts.