isomer

INCB3344 is a potent CCR2 antagonist. INCB3344 R-isomer is the R-isomer of INCB3344.

Eltanexor Z-isomer exhibits different inhibitory effects on Z138, MM15, 3T3 cell lines, with IC50s of 100 nM-50 μM, < 100 nM, > 30 μM, respectively.Eltanexor Z-isomer is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.

LY-411575 isomer 1 is a potent γ-secretase inhibitor. LY-411575 isomer 1 is an isomer of LY411575.

NVP-BHG712 isomer shows conserved non-bonded binding to EPHA2 and EPHB4.

T3-ATA S-isomer, the S-isomer of T3-ATA, represents the active form of the thyroid hormone.

T4-ATA S-isomer, the active form of the thyroid hormone, represents the S-isomer of T4-ATA.

Ulevostinag isomer 2 (MK-1454 isomer 2) is an isomer of Ulevostinag, which acts as a STING agonist.

Ulevostinag (isomer 3) (example 246) is an effective stimulator of the STING (stimulator of interferon genes) pathway. It plays a significant role in anti-tumor research.

Ulevostinag isomer 4 (MK-1454 isomer 4) is an isomer of Ulevostinag, which functions as a STING agonist.

Edoxaban Isomer is an impurity of Edoxaban, which is a novel inhibitor of factor Xa.

Sotorasib (AMG-510) isomer is a less active isomer of Sotorasib (AMG-510), which is a potent covalent inhibitor of KRAS G12C.

BAY-598 R-isomer is the R-isomer of BAY589, which is used as a reference compound. It is is an inhibitor of lysine N-methyltransferase (SMYD2) and is selective for SMYD2 over protease-activated receptor 1 (PAR1).

Trichostatin A S-isomer is the s-isomer of Trichostatin A. Trichostatin A is a histone deacetylase inhibitors (HDIs or HDACIs) that have a broad spectrum of epigenetic activities. Trichostatin A inhibits HDACs 1, 3, 4, 6 and 10 with IC50 values around 20

SCH900776 S-isomer (MK-8776 S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependent kinase CDK2 (IC50: 160 nM).

IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

ISRIB (trans-isomer) is a potent inhibitor of PERK (IC50=5 nM) that restores protein translation and prevents SG formation in the presence of P-eIF2α.

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC.

TIC10 Isomer (ONC201 isomer) is an isomer of TIC10, which inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.

BAY-6035 is an inhibitor of the methylation of MEKK2 peptide.

MKC-963 is a platelet aggregation inhibitor and autoinducer of CYP3A4.

APTO-253 isomer is an isomer of APTO-253 with the Fluoro-atom in 6-position. APTO-253 also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.

Dolutegravir RR Isomer is an isomer of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.

Dolutegravir SR Isomer is an isomeric derivative of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.

Oxybutynin R-isomer , also known as Aroxybutynin, is a muscarinic receptor antagonist. Aroxybutynin is the optically avtice inhibitor of proliferation and supresses gene expression in bladder smooth muscle cells. Oxybutynin exerts direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. It exhibits one-fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects).