||BAY-598 R-isomer is the R-isomer of BAY589. BAY-598 R-isomer may be used as a reference compound. BAY-598 is a potent, peptide-competitive chemical probe for SMYD2. BAY-598 has a unique chemotype relative to the current SMYD2 chemical probe LLY-507. BAY-598 inhibits in vitro methylation of p53K370 with IC50 = 27 nM and has more than 100-fold selectivity over other histone methyltransferases and other non-epigenetic targets. BAY-598 inhibits the methylation of p53K370 in cells with IC50 < 1 µM. (Further to this, BAY-598 has properties that are compatible with in vivo experiments.) A control compound, BAY-369, has also been developed. BAY-369 inhibits the in vitro methylation of p53K370 with IC50 > 70 micromolar.
||BAY-598 is a potent, peptide-competitive chemical probe for SMYD2. BAY-598 has a unique chemotype relative to the current SMYD2 chemical probe LLY-507. BAY-598 inhibits in vitro methylation of p53K370 with IC50 = 27 nM and has more than 100-fold selectivity over other histone methyltransferases and other non-epigenetic targets. BAY-598 inhibits the methylation of p53K370 in cells with IC50 < 1 µM. (Further to this, BAY-598 has properties that are compatible with in vivo experiments.) A control compound, BAY-369, has also been developed. BAY-369 inhibits the in vitro methylation of p53K370 with IC50 > 70 micromolar.
||R-268712 is a specific inhibitor of activin receptor-like kinase 5 (ALK5). It is also an orally active transforming growth factor-β type I receptor inhibitor.
||AZD7507 is a potent and selective CSF-1R inhibitor (32 nM cell activity), AZD7507 is considered a promising compound as it retained the desired potency and oral pharmacokinetic properties of AZ683. Moreover, in a telemetry study in dogs given a single oral dose, there was no cardiovascular toxicity, no elevation of troponin related to the treatment, and no alteration in the ECG.
||GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity.
||BI1744 is a long acting β2-adrenoceptor agonist with an EC50 of 1.4±0.08 nM.
||Parathyroid hormone (PTH) is essential for calcium homeostasis and its action is mediated by the PTH type 1 receptor (PTHR1), a class B G-protein-coupled receptor. Hypoparathyroidism and osteoporosis can be treated with PTH injections; however, no orally effective PTH analogue is available.
||Baloxavir is an anti-influenza agent extracted from patent WO 2017104691 A1.
||BLU-667 is a potent and selective inhibitor of RET mutations, fusions, and predicted resistant mutants. RET fusions are key drivers of multiple cancers, including lung and thyroid cancer, and our research suggests that RET also plays a key role in some colon and breast cancers. By simultaneously targeting the primary driver and predicted resistant mutants that render cancer cells insensitive to treatment with currently approved drugs,
||Mirogabalin, also known as DS-5565, is an α2δ-1 ligand being developed for pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia. It has shown promising results in Phase II clinical trials for the treatment of diabetic peripheral neuropathic pain.
||Resmetirom, or MGL-3196, shows outstanding safety in a rat heart model and is efficacious in a preclinical model at doses that showed no impact on the central thyroid axis.
||ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.
||IACS-010759 or IACS-10759 is a potent and selective Oxidative Phosphorylation Inhibitor (IC50 < 10 nM) with potential antineoplastic activity.
||Ertugliflozin, also known as also known as PF-04971729, is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus.
||Omarigliptin, also known as MK-3102, is a potent and long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
||Retagliptin, also known as SP-2086, is a DPP-4 inhibitor potentially used for the treatment of Type 2 diabetes.
||Trelagliptin, also known as SYR-472, is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed by Takeda for the treatment of type 2 diabetes (T2D).
||Vardenafil, also known as BAY 38-9456, is a PDE5 inhibitor used for treating erectile dysfunction.
||Etoricoxib is a synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic, and potential antineoplastic properties.
||CAS 545445-44-1, 3-morpholino-1-(4-(2-oxopiperi...