th2

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.

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.

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

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-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.

CMP-5 is a PRMT5 inhibitor with antiviral activity, inhibits PRMT5 methyltransferase activity, and can be used in the study of SARS virus infection.

CAY10595 is an antagonist of the CRTh2 (DP2) receptor with a Ki of 10 nM.

Emeramide (BDTH2) is a thiol-redox antioxidant. It is also a heavy metal chelator.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker whose mechanism of action involves antagonizing the Angiotensin 2 Receptor.

Ramatroban (BAY u3405) (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.

TH-263 is inactive toward both LIMK1 and LIMK2 and thus can be used as negative control for TH-257, and is a diaryl sulfonamide derivative.

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].

CMP-5 hydrochloride is a potent and selective PRMT5 inhibitor, while displays no activity against PRMT1/4/7 enzymes. It selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations.

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.

AMG-009 is a selective and potent dual antagonist of CRTH2 and DP, with an IC50 value of 3 nM for CRTH2 and 12 nM for DP receptors.

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

TH-237A is a novel neuroprotective agent exhibiting favorable permeation across the blood-brain barrier.