Innate and adaptive immunity, inflammatory pathways and immune signaling.
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CAS 939681-36-4
JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2; demonstrates inhibitor of U87MG/EGFR and U87MG/EGFRvIII with IC50 of 0.75 and 1.0…
CAS 1557232-32-2
GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.
CAS 497223-25-3
Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
CAS 1672684-68-2
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in…
CAS 54447-84-6
Cyclic-di-AMP (c-di-AMP) is a second messenger molecule produced in bacteria but not in mammals; can induce a strong immune response in vitro and in vivo.
CAS 110078-46-1
Plerixafor is a selective CXCR4 antagonist with an IC50 of 44 nM.
CAS 2105904-82-1
AB-680 is highly potent, reversible and selective small molecule inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity[1].
CAS 510-30-5
Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties. In vitro: Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced…
CAS 206645-99-0
Compstatinis is a 13-residue cyclic peptide, and a potent inhibitor of the complement system.
CAS 878385-84-3
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
CAS 864249-60-5
AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)…
CAS 2650093-47-1
UNC10225387B is a multi-kinase inhibitor, cocktail of UNC10225387B, UNC10225263A and UNC10225761A, promotes stem-cell-like chimeric antigen receptor T cells (CAR T cells).
CAS 2138299-33-7
diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
CAS 75567-37-2
Ingenol 3-Angelate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
CAS 2272917-13-0
NT-0796 is a Brain-Penetrant and Highly Potent. NLRP3 Inflammasome Inhibitor (IC50 = 0.32 nM) for Neuroinflammatory Disorders.
CAS 281209-71-0
DMB(C-185) is a direct and selective GSDMD agonist that activates GSDMD pore formation and pyroptosis without cleaving GSDMD. DMB treatment synergizes with anti-PD-1 and does not alter circulating proinflammatory cytokine or leukocyte numbers or cause weight…
CAS 592517-80-1
11R-VIVIT is a potent NFAT inhibitor. 11R-VIVIT inhibits LPS or LPS plus IFN-γ-induced IL-12 p40, IL-12 p70, IL-23 and TNF secretion from bone marrow-derived macrophages (BMDMs). 11R-VIVIT also attenuates NO production and Nos2 mRNA expression in…
CAS 2101700-15-4
LOXO-305 is an investigational, novel, selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. LOXO-305 was designed to reversibly bind BTK, preserve activity in the presence of the acquired resistance, and avoid off-target kinases that have…
CAS 34031-32-8
Auranofin, also known as Ridaura and SKF-39162, is an oral chrysotherapeutic agent for the treatment of rheumatoid arthritis. Auranofin's exact mechanism of action is unknown, but it is believed to act via immunological mechanisms and alteration of lysosomal…
CAS 2244984-64-1
CSLP37 (RIPK2 inhibitor CSLP37) is a novel potent, ATP pocket-binding RIPK2 inhibitor with IC50 of 16.3 nM in ADPGlo assay, demonstrates inhibition of both the RIPK2-XIAP interaction, and of cellular and in vivo NOD2 signaling; exhibits inhibition of TNF…
CAS 1337878-62-2
ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
CAS 2079939-05-0
Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
CAS 1334294-76-6
GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibition of G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-response element-binding protein-based reporter and…
CAS 905586-69-8
AZ960 also inhibits many kinases less than 50% at a concentration of 0.1 μM such as JAK3 (IC50=9 nM), TrkA, Aurora, and ARK5. In cells, AZ 960 inhibits the phosphorylation of STAT5 in TEL-JAK2 cells with an average IC50 of 15 nM and exhibits 15-30 -fold…
CAS 1172933-44-6
Bexin-1 is a specific inhibitor that targets Munc13-4, a protein critical for regulated exocytosis, particularly in secretory cells such as immune cells (e.g., cytotoxic T lymphocytes, mast cells) and neuroendocrine cells. Munc13-4 plays a key role in vesicle…
NH-23-C2 (Caspase-2 inhibitor NH-23-C2) is a potent, selective and cell-permeable endogenous caspase-2 inhibitor, does not block caspase-3 or caspase-8.NH-23-C2 displays off-reactivity with cysteine and threonine proteases (cathepsins B, L, V, S).HCT116 cells…
CAS 1229236-86-5
Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
CAS 1024828-77-0
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney…
CAS 211096-49-0
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM,…
CAS 1216540-18-9
BX-513 hydrochloride inhibits MIP-1α-induced intracellular calcium mobilization (IC50 = 2.5 μM). Selective CCR1 receptor antagonist (Ki values are 0.04, > 10, > 10 and > 10 nM for CCR1, CCR5, CXCR2 and CXCR4 receptors respectively). A full inverse agonist at…
CAS 2375420-34-9
SR-717 is an agonist of stimulator of interferon genes STING for treating cancer. SR-717 demonstrates broad interspecies and interallelic specificity. SR-717 functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that…
CAS 1346623-17-3
Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor inhibitor with an IC50 of 0.1 nM.
CAS 945865-02-1
UNC10225761A is a multi-kinase inhibitor, cocktail of UNC10225387B, UNC10225263A and UNC10225761A, promotes stem-cell-like chimeric antigen receptor T cells (CAR T cells).
CAS 566914-00-9
TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses[1].
CAS 1239600-18-0
LMT-28 (LMT28) is a specific blocker of IL-6 signaling via inhibits IL-6Rβ (gp130) with IC50 of 5.9 uM (IL-6–induced luciferase activity), selectively inhibits IL-6–induced phosphorylation of STAT3, JAK2, and gp130; does not affect LIF-induced STAT3…
CAS 841290-81-1
R406 is a competitive Syk inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value.
CAS 1450881-55-6
SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
CAS 540737-29-9
Tofacitinib citrate is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
CAS 1435467-38-1
PF-1355 is a selective 2-thiouracil mechanism-based MPO inhibitor, used for treatment of vasculitic diseases.
CAS 1092939-17-7
Ruxolitinib phosphate is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
CAS 1341224-83-6
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50 of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
CAS 477600-75-2
Tofacitinib is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
CAS 1884461-72-6
Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic…
CAS 1675201-83-8
PD-1/PD-L1 inhibitor C1 is a potent and selective small molecule inhibitor of the PD-1/PD-L1 protein/protein interactions with IC50 < 100 nM (PD-1/PD-L1 Homogenous Time-Resolved Fluorescence (HTRF) binding assay). It may potentially be useful in the treatment…
