Immunology and Inflammation

IL-17 modulator 5 is a IL-17 inhibitor, with an IC 50 of 1 nM .

Factor B-IN-3 is a potent inhibitor of complement factor B. Factor B-IN-3 can be used to study inflammatory and immune-related diseases.

(S,R,S)-AHPC-Boc derivative 1 (Compound 80-9; VH032-Boc derivative 1) is a selective proteasomal degrader targeting MALT1, which recruits the E3 ubiquitin ligase CRBN to form a ternary complex with MALT1. This interaction leads to the ubiquitination and subsequent proteasomal degradation of MALT1. By disrupting the CBM complex, (S,R,S)-AHPC-Boc derivative 1 inhibits the NF-κB signaling pathway and shows potential in inducing apoptosis in ABC-DLBCL cells. It holds promise for research into MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL).

BMY-25551, a Mitomycin A analog, exhibits cytotoxicity 8 to 20 times greater than Mitomycin C against both murine and human tumor cell lines. It is applicable in research pertaining to cancer and hematological disorders.

Compound O15, an Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM; it inhibits Keap1-Nrf2 binding and Nrf2 ubiquitination.

Lobaric acid, from Stereocaulon lichen, has antioxidant and anticancer properties, inhibits PTP1B and 12(S)-LOX, and reduces TMV lesions in plants.

IKZF1-degrader-1 (Compound 9-B) serves as a potent degrader of the IKZF1 protein, exhibiting a DC50 of 0.134 nM. It is applicable in the degradation of tumors [1].

TLR4/JNK/NF-κB-IN-1 (Racemic-11k) is an inhibitor of TLR4, JNK, and NF-κB. It suppresses NO production in LPS-stimulated RAW264.7 cells with an IC50 of 23.2 µM. By inhibiting TLR4 expression and reducing JNK phosphorylation, TLR4/JNK/NF-κB-IN-1 prevents NF-κB activation. This leads to a decrease in the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and the production of inflammatory mediators such as NO, PGE2, and TNF-α, thereby exhibiting anti-inflammatory activity. TLR4/JNK/NF-κB-IN-1 holds potential in the study of inflammatory diseases, including rheumatoid arthritis and various other inflammatory conditions.

AS2690168 hydrochloride is an orally active inhibitor of RANKL signaling that can suppress RANKL-induced osteoclastogenesis in RAW264 cells. AS2690168 is applicable in research related to pathological bone resorption.

(R)-Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) that exhibits oral activity and analgesic properties. Unlike its counterpart, (R)-Ketoprofen does not significantly enhance the increase of inflammatory cytokines (such as Tumor Necrosis Factor (TNF) and Interleukin-1 (IL-1)) induced by LPS. However, it can inhibit the anti-inflammatory activity of (S)-Ketoprofen.

TLR7/8 agonist 7 activates immune cells, useful in ISAC synthesis and immunity research.

IRAK1/4/pan-FLT3 Kinase-IN-2 (compound 27) is a potent dual inhibitor of IRAK1/4 and FLT3 with IC50 values of 10 nM, 0.7 nM, and < 0.5 nM, respectively. This compound enhances survival in mice models of acute myeloid leukemia.

Pentacyclic triterpene, anti-inflammatory agent 12, inhibits LPS inflammation (IC50: 2.22 μM). May benefit inflammatory disease studies.

GNE-2256, also known as molecule 19, is an orally active compound that inhibits Interleukin 1 receptor-associated kinase 4 (IRAK4) with a K i of 1.4 nM and has

PSMA-IN-4 (compound 9) functions as a potent PSMA inhibitor, exhibiting an IC 50 value of 1.2 μM [1].

MAO-B-IN-7 inhibits MAO-B/AChE, crossing the blood-brain barrier; IC50: 41/87 nM (h/eel AChE), 0.3 μM (MAO-B). Reduces oxidative stress and neuroinflammation.

<p>NLRP3-IN-70 (Compound 5m) is an inhibitor of the NLRP3 inflammasome with low oral bioavailability. It binds directly to the NACHT domain of the NLRP3 protein, thereby blocking its interaction with ASC, which inhibits ASC oligomerization and the assembly of the NLRP3 inflammasome. NLRP3-IN-70 is applicable in studies on sepsis and non-alcoholic steatohepatitis.</p>

<p>ODN 21158 is a potent, non-cytotoxic inhibitor of G-modified TLR3 and TLR9. ODN 21158 dose-dependently inhibits IFN-α secretion.</p>

VS-15 is a selective inhibitor of IDO1, specifically binding to its apo-heme form. Additionally, VS-15 serves as an inhibitor of iNOS.

NLRP3-IN-53 (compound 1) is an NLRP3 inhibitor with an IC50 of 3.4nM.

Galectin-8-IN-1 selectively binds galectin-8N with 48 μM affinity, 15x more than galectin-3.

mPGES1-IN-4 (compound 32) is a multi-substituted pyrimidine compound acting as a submicromolar inhibitor of PGE2 production. It primarily exerts its anti-inflammatory effects by inhibiting mPGES-1 and significantly suppresses acute inflammation models in vivo.

PZ-3022 is an orally active, conformational PanK activator that counteracts C3-CoA inhibition. In a mouse model of propionic acidemia, it elevates hepatic CoASH and C2-CoA levels while reducing C3-CoA, making it useful for studying mitochondrial defects in propionic acidemia.

IRAK4-IN-14 is a selective, potent, orally active IRAK4 inhibitor (IC50: 0.003 μM) with favorable PK parameters in rats and mice. effect.

S-MTC acetate (S-Methyl-L-thiocitrulline acetate) serves as a potent inhibitor of inducible nitric oxide synthases and is especially effective in inhibiting the constitutive (neuronal) type rather than the inducible (endothelial) type.

<p>IRAK4-IN-30 (Compound I) is an inhibitor of IRAK4, with an IC50 of 0.6 nM.</p>

CD73-IN-13, a potent CD73 inhibitor, may be developed for tumor-related disease treatment.

Anti-inflammatory agent 102 (Compound 11a) is an orally effective anti-inflammatory compound. It exerts its effects by inhibiting the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. This agent displays significant anti-inflammatory activity by suppressing the release of NO, ROS, and inflammatory cytokines such as IL-6, TNF-α, and IL-1β. Anti-inflammatory agent 102 is applicable in research concerning inflammatory diseases, including ulcerative colitis (UC).

Cryptopleurine is an inhibitor of gene products associated with cell proliferation, survival, invasion and angiogenesis. It acts by targeting the NF-κB pathway.

MALT1-IN-5 is a potent inhibitor of the MALT1 protease and can be used in cancer research.

Galectin-3-IN-4 (compound 5), a carboxamide analog, effectively and selectively inhibits both human and mouse galectin-3. This compound demonstrates notable potency with IC50 values of 21 nM for hGal-3 and 167 nM for mGal-3. It is also orally bioavailable. For other galectins, Galectin-3-IN-4 shows IC50 values of 1580 nM for hGal-1 and 2750 nM for hGal-9, respectively [1].

Itaconic acid prodrug-1 (Compound P2) is an orally active prodrug of Itaconic acid that efficiently delivers Itaconic acid to skin tissues upon oral administration. It exhibits immunomodulatory effects, significantly inhibiting Poly(I:C)/IFNγ-induced inflammatory cytokines in human epidermal keratinocytes. Itaconic acid prodrug-1 is useful for research into alopecia areata and other inflammatory skin conditions.

COX-2-IN-12: Potent, selective COX-2 inhibitor, IC50=19.98μM, safe anti-inflammatory with low acute toxicity.

ROS151 is an AChE inhibitor with IC50 values of 14 nM (hAChE), 1.68 μM (eqBChE), and 8.17 μM (hFAAH). Additionally, it acts as a chelating agent for Fe3+ and Cu2+. ROS151 is utilized in research related to Alzheimer's disease.

(S)-MALT1-IN-5: Potent MALT1 protease inhibitor, may help in abnormal T/B-cell signalling and MALT1-linked diseases.

E5090 is a novel orally active inhibitor of IL-1 generation. It also has anti-inflammatory properties.

STING-IN-11 is a potent, orally bioavailable STING inhibitor (IC₅₀ = 37.8 nM) that blocks STING protein palmitoylation and downstream signaling.

TLR7 agonist28 (compound 3) is a potent TLR7 agonist. This compound can be combined with anti-tumor monoclonal antibodies (mAb) for use in cancer immunotherapy.

<p>CD73-IN-19 (Compound 4ab) is an inhibitor of CD73, demonstrating a 44% inhibition rate of CD73 enzyme activity at 100 μM. It entirely counters T cell proliferation blockade triggered by TCR activation (induced by CD73 activity) at 10 μM and 100 μM and inhibits hA2A receptor activity in HEK-293 cells with a Ki of 3.31 μM. CD73-IN-19 holds potential for research in the field of immune diseases.</p>

IRAK4-IN-31 is a crystalline inhibitor of IRAK4. It is applicable in research related to myelodysplastic syndromes (MDS).

iNOs-IN-1 (YPW) is a strong iNOS inhibitor with dose-dependent anti-inflammatory properties, reducing IL-6, iNOS, and NO levels.

Factor B-IN-4 is a potent inhibitor (IC50: 1 μM) of complement factor B. Factor B-IN-4 can be used to study inflammatory and immune-related diseases.

Anti-inflammatory agent 18: NO activity blocker (IC50: 15.94 μM), hampers HMGB1-induced inflammation, potential for COVID-19, sepsis study.

AS2690168 freebase is an orally active inhibitor of RANKL signaling, capable of suppressing RANKL-induced osteoclastogenesis in RAW264 cells. AS2690168 is applicable in research related to pathological bone resorption.

FK-565 is a ligand of nucleotide-binding oligomerization domain-1 (NOD1) that induces a mouse model of arteritis.

mPGES1-IN-9 (compound 1_8) is an mPGES1 inhibitor with an IC50 of 0.5 μM and is utilized in anti-inflammatory research.

NDT-30805, a triazolopyridine, blocks IL-1β in PBMC (IC50: 0.013μM) & NLRP3 inflammasome, for inflammation research.

HG-12-6 is a type II IRAK4 inhibitor, targeting its inactive form with an IC50 of 165 nM, and is used in autoimmunity and inflammation.

Ac5GalNTGc, an analog of hexosamine, inhibits mucin-type O-linked glycosylation biosynthesis [1].

CD73-IN-12, a compound from CN114437038A, shows strong anti-tumor activity by effectively inhibiting CD73 enzyme.