Catalog No.
Product Name
Application
Product Information
Citations
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TYROSINE 3-MONOOXYGENASE inhibitor
Metyrosine is an inhibitor of the enzyme TYROSINE 3-MONOOXYGENASE. -
H-PGDS inhibitor
HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM. -
PD-1/PD-L1 interaction inhibitor
PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM. -
MD2-TLR4 inhibitor
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. -
glucocorticoid receptor agonist
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent. -
CCR4 antagonist
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. -
Gal-3 inhibitor
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model.- Jiten R Sharma, .et al. , Life Sci, 2023, Apr 1;318:121480 PMID: 36775116
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STING ligand
STING ligand-1 is a lead STING ligand with an IC50 of 68 nM for HAQ STING. -
CCR2 /CCR5 dual antagonist
PF-04634817 is an orally administered CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema. -
NOS inhibitor
Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a number of pathological states.- Raul Salinas, .et al. , PLoS One, 2023, Mar 2;18(3):e0282155 PMID: 36862634
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cGAS inhibitor
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. -
SIK inhibitor
YKL-06-061 is a potent and selective SIK (salt-inducible kinase) inhibitor. -
C5 inhibitor
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). -
Factor B inhibitor
LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM).- Wenbin Yang, .et al. , J Clin Invest, 2022, Oct 17;132(20):e157975 PMID: 36250462
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FKBP Dimerizer
Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis. -
COX/LOX inhibitor
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 ?M?? -
CD38 inhibitor
CD38 inhibitor 1 (compound 78c) is a potent CD38 inhibitor with IC50s of 7.3 nM and 1.9 nM for hCD38 and mouse CD38. -
STING receptor agonist
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. -
heterobifunctional degrader
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. -
Keap1-Nrf2 inhibitor
Keap1-CNrf2-IN-1 (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. - Pyropheophorbide-a (Ppa) is a promising photosensitizer for tumor photodynamic therapy (PDT).
- Purpurin 18, a derivative of chlorophyll, is an interesting dihydroporphyrin for generating photosensitizers.
- Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1.
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nitric oxide synthases inhibitor
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively. -
FKBP ligand
AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules. -
TLR7 agonist
TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM. -
CCR2 antagonist
CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM. -
CRBN degrader
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3. -
drug-linker conjugate for ADC
AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.
