th2

CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].

CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.

CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

TH287 is a potent inhibitor of MTH1 (NUDT1), less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.

TH287 is a selective MTH1 inhibitor(IC50 : 0.8 nM). It causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

TH251 is a highly selective antagonist of LIMK1 and LIMK2 (LIMK1 2).

CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.

SB273005 is an orally active and potent nonpeptide integrin αvβ3 antagonist that inhibits αvβ3 and αvβ5 and reduces the production of Th2 cells and the cytokine IL-10 in pregnant mice.

Valencene (NSC-148969) is a sesquiterpenoid isolated from Cyperus rotundus and is an aroma component of citrus fruits and citrus-derived odors.ValenceneValencene has anti-allergic, anti-inflammatory, anti-melanogenic, and antioxidant activities. Valencene inhibits the overexpression of Th2 chemokines and pro-inflammatory chemokines by blocking the NF-κB pathway.

NVP-QAV-680 is a potent and selective antagonist of CRTh2 receptor. NVP-QAV-680 has nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro.

BI-671800 (AP-761) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2 CRTH2). With IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has the potential to treat poorly controlled asthma[2].

GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. It suppresses NF-κB activation and transcription of target genes without inhibiting proteasome activity. GS143 has anti-asthm[atic] properties.

Fevipiprant (NVP-QAW039) is a selective, potent, reversible competitive CRTh2 antagonist.

Suplatast Tosilate (IPD 1151T) is a novel capsular anti-asthmatic drug with an IC50 above 100 μM, inhibiting both IgE production and the synthesis of IL-4 and IL-5.

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

PA452 is a selective antagonist of retinoic X receptor (RXR) and suppresses the effect of Retinoic acid on Th1 Th2 development.

Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra

4-Octylphenol is an endocrine disruptor with gender-specific effects on male germ cells, significantly reducing the mitotic index and the number of spermatogonia. It also causes inflammatory damage in the gills of carp by activating the complement system through the C3a C3a receptor (C3a C3aR) axis and C5a C5a receptor 1 (C5a C5aR1) axis. Furthermore, 4-Octylphenol induces immune suppression by disrupting the balance between helper T (Th) cells 1 Th2 and regulatory T (Treg) Th17 cells, and triggers inflammatory damage through the Toll-like receptor 7 (Toll-like Receptor (TLR)) inhibitor κBα nuclear factor κB (TLR7 IκBα NF-κB) pathway.

Timapiprant (OC000459) is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).

Naringenin chalcone (Isosalipurpol) has antiallergic activity Naringenin chalcone suppresses asthmatic symptoms by inhibiting Th2 cytokine production from CD4 T cells. Naringenin chalcone is a potent tomato flavonoid that improves adipocyte metabolic functions and exerts insulin-sensitizing effects by activating an adiponectin-related pathway. Naringenin chalcone exhibits anti-inflammatory properties by inhibiting the production of proinflammatory cytokines in the interaction between adipocytes and macrophages, may be useful for ameliorating the inflammatory changes in obese adipose tissue.

Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2, a G protein-coupled receptor for prostaglandin (PGD2), mediates key inflammatory responses related to allergy and asthma. PGD2, produced by mast cells, binds to CRTH2 on blood-borne cells, inducing chemotaxis of Th2 cells, basophils, and eosinophils, and stimulating cytokine release.

α-Galactosylceramide analog 8 (α-GalCer analog 8) is a triazole derivative of α-galactosylceramide. [1] It increases IL-2 secretion by DN32.D3 NKT hybridoma cells when co-cultured with CD1d-transfected RBL cells pre-loaded with α-GalCer analog 8 at a concentration of 32 ng/ml. α-GalCer analog 8 (32 ng/ml) induces IL-4 secretion to a greater extent than the synthetic α-GalCer KRN 7000 in mouse splenocytes in vitro and in mouse serum following administration of a 1 µg per animal dose, indicating a Th2 response.