| DC70195 |
AMY-101 |
AMY-101 (Cp40) is a peptidic inhibitor of the central complement component C3 for the management of patients with ARDS caused by SARS-CoV-2 infection.AMY-101 is a novel complement C3-targeted therapeutic based on the 3 rd-generation compstatin analog Cp40. |
|
| DC70264 |
BMS-905 |
BMS-905 is a potent dual inhibitor of TLR7 and TLR8 with IC50 of 0.3 nM (TLR7, IL-6 inhibition in mouse blood), shows good selectivity against TLR9 and other TLR family members. |
|
| DC70280 |
C5 complement inhibitor 7 |
C5 complement inhibitor 7 (C5-IN-7) is a potent, small-molecule inhibitor of C5 complement protein with serum assay IC50 of <5 nM (2% human serum complement inhibition).C5-IN-7 demonstrated excellent potency and good aqueous solubility, inhibited MAC deposition with IC50 of 1 uM in a complement inhibition assay using 50% human whole blood.The C5 triple mutants (C704R, V705I and N707H) were not inhibited by C5 complement protein inhibitor 7 up to 100 uM.C5 complement protein inhibitor 7 binds within the predicted pocket between the C5a and MG8 domains in close proximity to the C5 convertase cleavage site (R751-L752). |
|
| DC70330 |
CU-72 |
CU-72 is a potent, selective TLR7/8 dual inhibitor with IC50 of 5.10 and 2.87 uM, respectively. |
|
| DC70332 |
CU-CPD107
Featured
|
CU-CPD107 is a TLR8-specific small molecule with unique synergistic agonist activities in the presence of ssRNA, but inactive without the aid of ssRNA.CU-CPD107 significantly inhibited of R848-induced signaling in HEK-Blue hTLR8 cells with an IC50 of 13.7 uM.CU-CPD107 only inhibited synthesized small-molecule agonist-induced TLR8 signaling without affecting other TLRs.CU-CPD107 synergistically increased IFN-β, TNF-α, IL-1β, IL-6, and IL-8 mRNA expression levels in the presence of 5 μg/ml ssRNA40 in HEK-Blue hTLR8 cells, whereas CU-CPD107 alone did not. CU-CPD107 only activated TLR8-mediated signaling in the presence of ssRNA.CU-CPD107 showed no pure agonistic activity, addressing a major challenge that has existed for previous TLR7 and TLR8 agonists as vaccine adjuvants or antiviral drugs. |
|
| DC70351 |
DF2593A |
DF2593A (DF 2593A) is a potent, selective, noncompetitive allosteric inhibitor of C5aR with IC50 of 5 nM (C5a-induced human PMN migration inhibition), and rat and mouse orthologs (IC50=6.0 nM and IC50=1.0 nM, respectively); dispalys >1,000-fold selective versus other chemoattractants, including CXCL8 and CXCL1 (CI50>10 uM), as well as on a panel of different GPCRs and ion channels; DF2593A demonstrated antinociceptive effects in several models of inflammatory pain and effectively inhibited articular hyperalgesia in CFA-induced mechanical and thermal hyperalgesia and arthritic nociception. |
|
| DC70395 |
Evixapodlin |
Evixapodlin is a highly potent, small molecule human PD-1/PD-L1 protein-protein interaction inhibitor with IC50 of 0.213 nM, exhibits potential anticancer and antiviral activities. |
|
| DC70435 |
GNE-2256 |
GNE-2256 (GNE2256) is a potent, selective inhibitor of IRAK4 with biochemical Ki of 1.4 nM.GNE-2256 displays high selectivity in the CEREP panel with off-targets with >50% inhibition are TACR1, HTR2B and ACHE.GNE-2256 is potent in the NanoBRET assay (IC50 = 3.3 nM), the IL-6 human whole blood assay (IC50=190 nM) and the IFNα human whole blood assay (IC50=290 nM). |
|
| DC70469 |
GSK669 |
GSK669 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor, inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling (IC50=0.5 uM), has an IC50 of 3.2 uM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.GSK669 specifically inhibits MDP-induced NOD2 activation, has no effect on IL-8 secretion induced by over-expression of NOD1.GSK669 significantly inhibits platelet proinflammatory cytokine release induced by muramyl dipeptide, platelet aggregation, ATP release, and ROS generation induced by collagen and collagen related peptide (CRP). GSK669 inhibits thrombosis and oxidative stress via targeting platelet glycoprotein VI (GPVI), decreases malonaldehyde (MDA) and increases superoxide dismutase (SOD) levels in mouse plasma |
|
| DC70493 |
HS-243 |
HS-243 (HS243) is a highly potent, super-selective IRAK-1/4 inhibitor with IC50 of 24/20 nM, respectively.HS-243 shows exquisite potency toward IRAK-1/4 over all other human kinases with only minimal TAK1-inhibiting activity (IC50=0.5 uM).HS-243 binds in the ATP-binding pocket of IRAK-4.HS-243 potently reduces the proinflammatory response of RA cells and macrophages, has distinct cytokine profile from TAK1.HS-243 reduces percentage of survival in pancreatic and breast cancer cell lines. |
|
| DC70527 |
JPE1375 |
JPE1375 is a potent, peptidomimetic C5a receptor antagonist with IC50 of 39 nM.JPE1375 inhibits neutrophil influx in the RPAR in mice. |
|
| DC70644 |
ND2158 |
ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM;
ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.
ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.
IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.
In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199. |
|
| DC70654 |
NLRP3-IN-3 |
NLRP3-IN-3 is a potent and selective inhibitor of NLRP3 inflammasome with IC50 of 1.26 nM in THP1 cells, showing good pharmacokinetic profiles with oral bioavailability. |
|
| DC70682 |
PD-L1 inhibitor 4 |
PD-L1 inhibitor 4 is a small molecule inhibitor of PD-1/PD-L1 with SPR KD of 0.079 nM.PD-L1 inhibitor 4 exhibited substantially increased binding affinity to hPD-L1, as well as PD-1/PD-L1 inhibitory activity in physiological conditions.PD-L1 inhibitor 4 also showed a dose-dependent increase in IFN-γ secretion levels in a mixed lymphocyte reaction assay. |
|
| DC70786 |
SM360320 |
SM360320 (CL-087, 1V136) is a potent, orally active and selective TLR7 agonist (ligand).SM360320 inhibited HCV replication in Huh-7 cells in a dose-dependent manner in the Huh-7 replicon system, reduced HCV mRNA and protein levels in isolated Huh-7 hepatocytes.SM360320 induced in vivo secretion of interferon alpha (IFNalpha) and exerted a significant antitumor effect in CEA.Tg mice challenged with a syngenic tumor cell line expressing CEA.SM360320 exerts significant antitumor effects and can act in association with DNA-EP for CEA-positive colon cancer and HER2-positive mammary carcinoma.Repeated low dose administration of SM360320 induced hyporesponsiveness or tolerance to TLR2, -7, and -9 activators and limited the course of neural inflammation in an experimental allergic encephalomyelitis model. |
|
| DC70810 |
STING agonist 22 |
STING agonist 22 is a novel, non-nucleotide specific small-molecule STING agonist with IC50 of 28, 11 uM for human STING isoforms WT and HAQ, respectively.STING agonist 22 did not show any cytotoxicity in an immune cell proliferation panel across a variety of immune cell types and also did not show any activity in a kinome panel.STING agonist 22 introduced higher levels of iFIT3 and MX1 mRNA across three different donors possessing different STING genotypes: WT/WT, WT/HAQ, and WT/R232H in human PBMCs (IC50=5-35 uM).STING agonist 22 demonstrated in vivo antitumor effect in an MC38 mice model, with STING pathway activation and production of type I IFNs and proinflammatory cytokines, serum levels of IL-6, G-SCF, and MIP-1β. |
|
| DC70845 |
THZ-2-118 |
THZ-2-118 is a potent selective inhibitor of IRAK1 with IC50 of 14.2 nM;
THZ-2-118 does not inhibitor IRAK4 at 10 uM, also potently inhibits JNK1/2/3 (IC50=1-2 nM). |
|
| DC70929 |
ZE132 |
ZE132 is a potent and selective small-molecule inhibitor of PD-1/PD-L1 interaction with IC50 of <0.1 nM.ZE132 effectively inhibits the PD-1/PD-L1 interactions in vitro, and has a potent affinity to PD-L1.ZE132 shows robust anti-tumour effects in vivo, better than anti-PD-1 antibody.ZE132 treatment promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression.ZE132 elicits strong inhibitory effects on the mRNA expression of TGF-β. |
|
| DC71002 |
AMT hydrochloride
Featured
|
AMT hydrochloride is a selective inhibitor of inducible NOS (iNOS) with Ki of 4.2 nM. |
|
| DC71008 |
Avatrombopag maleate
Featured
|
Avatrombopag maleate (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag maleate mimics the biological activities of TPO. Avatrombopag maleate increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag maleate is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A. |
|
| DC71014 |
C6 L-threo Ceramide |
C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. C6 L-threo Ceramide significantly inhibits IL-4 production in T cells. Anti-allergic agents. |
|
| DC71023 |
CP-424174 |
CP-424174 is a reversible inhibitor against IL-1β processing with an IC50 of 210 nM.CP-424174 indirectly inhibits NLRP3. |
|
| DC71038 |
EXP3179 |
EXP3179 is an important intermediate aldehyde metabolite of Losartan. EXP3179 has no AT1-R–blocking activity, but potently inhibits the expression of endothelial cyclooxygenase (COX)-2. EXP3179 exerts potent anti-inflammatory actions. |
|
| DC71063 |
Isofezolac |
Isofezolac (LM 22070) is a non-steroidal anti-inflammatory drug (NSAID) that inhibits prostaglandin-synthetase. Isofezolac anti-inflammatory, and antipyretic properties. |
|
| DC71090 |
N2S2-CBMBC |
N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method. |
|
| DC71106 |
Pyocyanin |
Pyocyanin (Pyocyanine) is a phenazine that is a toxic, quorum sensing (QS)-controlled metabolite produced by P. aeruginosa. Pyocyanin is a redox-active compound and promotes the generation of reactive oxygen species (ROS). Pyocyanin also possesses antibacterial properties and increases fitness in competition with other bacterial species. |
|
| DC71123 |
TFC 007
Featured
|
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon). |
|
| DC71126 |
TL8-506 |
TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 can be used for the research of tuberculosis and autoimmune diseases. |
|
| DC71134 |
Ulevostinag (isomer 1) |
Ulevostinag isomer 1 (MK-1454 isomer 1) is the isomer of Ulevostinag. Ulevostinag is a STING agonist. |
|
| DC71144 |
HE-S2 |
HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the PD-1/PD-L1 interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity. |
|
