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Emeramide

Emeramide functions as a thiol-based redox antioxidant and chelates heavy metals.

Pinealon

Pinealon is a tripeptide exhibiting neuroprotective effects. This peptide inhibits reactive oxygen species (ROS) buildup and blocks ERK 1/2 activation. It enhances functional activity of key brain tissue cellular components while decreasing spontaneous cell death rates. Studies demonstrate Pinealon's protective effects against prenatal hyperhomocysteinemia in rat offspring.

BMS-986260

BMS-986260 is an orally active immuno-oncology agent that inhibits TGFβR1 with an IC50 of 1.6 nM. It shows selectivity for TGFβR1 compared to TGFβR2 and over 200 other kinases. In MINK and NHLF cell lines, BMS-986260 blocks TGFβ-induced pSMAD2/3 nuclear translocation with IC50 values of 350 nM and 190 nM, respectively.

naperiglipron

Naperiglipron (LY3549492) (Example 2) acts as a glucagon-like peptide 1 receptor (GLP-1R) agonist, exhibiting an EC50 of 1.14 nM at hGLP-1R. In GLP-1R knock-in mouse models, it reduces blood glucose levels. The compound shows PDE10A1 enzyme inhibitory activity (IC50: 7.43 μM) and displays weak hERG inhibition. Naperiglipron has potential applications in type II diabetes mellitus (T2DM) and obesity studies.

VS-7375 (GFH375)

VS-7375 (GFH375) is an oral small-molecule inhibitor that selectively targets KRAS G12D in both its active (GTP-bound) and inactive (GDP-bound) forms. This dual-state inhibition results in stronger tumor suppression compared to single-state inhibitors. It exhibits potent anti-proliferative and anti-tumor effects in KRAS G12D-mutant models, including an intracranial GP2D tumor model.

PKN1

PKN1/2-IN-1 is a cell-permeable compound that inhibits PKN1 and PKN2, with IC50 values of 16 nM and 210 nM, and Ki values of 8 nM and 108 nM, respectively. In NanoBRET assays, it shows intracellular PKN2 binding with an IC50 of 2.1 μM. This compound is applicable for investigating tumor cell migration and related physiological processes.

HRS‑5346

Lp(a)-IN-5 (Compound A) is an orally administered lipoprotein(a) (Lp(a)) inhibitor. This compound demonstrates inhibition of Apo(a) and ApoB protein assembly with an IC50 of 0.41 nM. It may be useful for studying diseases associated with increased plasma Lp(a) levels, including cardiovascular disorders.

AS1708727

AS1708727 is an orally bioavailable Foxo1 inhibitor that exhibits EC50 values of 0.33 μM against G6Pase and 0.59 μM against PEPCK.

Atebimetinib (IMM-1-104)

Atebimetinib inhibits MEK tyrosine kinase and demonstrates antineoplastic effects.

Auceliciclib (AU3-14,Ulecaciclib )

Ulecaciclib is an orally active cyclin-dependent kinase (CDK) inhibitor with Ki values of 0.62 μM for CDK2/Cyclin A, 0.2 nM for CDK4/Cyclin D1, 3 nM for CDK6/Cyclin D3, and 0.63 μM for CDK7/Cyclin H. This compound demonstrates blood-brain barrier penetration and favorable pharmacokinetic properties.

Mazdutide (IBI362, LY330567)

Mazdutide (IBI-362; LY-3305677) is a synthetic long-acting oxyntomodulin analog that functions as a dual agonist of glucagon-like peptide-1 receptor (GLP-1R) and glucagon receptor (GCGR). The compound exhibits binding affinity for human and mouse GCGR (Ki values of 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki values of 28.6 nM and 25.1 nM, respectively). In mouse islets, mazdutide stimulates insulin secretion with an EC50 of 5.2 nM. This agent has been investigated in research related to obesity and type 2 diabetes (T2D).

SS-3091

SS-3091 is a pan-KRas inhibitor that targets the interaction interfaces of KRas. By destabilizing the ARaf/KRas complex, it modulates downstream signaling pathways. This compound exhibits activity against KRas G12D, G12C, G12V, and G12S mutants in multiple cancer cell lines.

Mito-LND (Mito-Lonidamine)

Mito-LND (Mito-Lonidamine) is an orally administered mitochondria-targeted compound that inhibits oxidative phosphorylation (OXPHOS). This agent reduces mitochondrial bioenergetics, promotes reactive oxygen species generation, and triggers autophagic cell death in lung cancer cells.

ADT-1004

ADT-1004 is a RAS inhibitor that may be investigated for Ras-mediated diseases.

Eloralintide (LY-3841136)

Eloralintide (LY 3841136) is an AMYR agonist with potential applications in type 2 diabetes and obesity research.

MCB-294

MCB-294 is a pan-KRAS inhibitor that targets both active (GTP-bound) and inactive (GDP-bound) KRAS states, exhibiting Kd values of about 1 pM and 10 nM, respectively. It shows preferential inhibition of KRAS over NRAS and HRAS. The compound inhibits proliferation of hTERT-HPNE cells harboring G12D, G12C, G12V, G12S, G13D, and wild-type KRAS variants, with IC50 values around 700 nM. MCB-294 triggers apoptosis in KRAS-mutated tumors and demonstrates activity against KRASG12C inhibitor-resistant cancer cells while modulating the tumor immune microenvironment. This compound serves as a research tool for pancreatic, colorectal, and lung cancer investigations.

RP03707

RP03707 is a PROTAC molecule designed to degrade KRASG12D, consisting of three components: a KRASG12D inhibitor (, red), a linker (black), and an E3 ligase ligand (blue).

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Selleck Chemicals is your Trusted Supplierfor Inhibitors, Antibodies, Proteins, Kits and Reagents

Selleck Chemicals is your Trusted Supplier
for Inhibitors, Antibodies, Proteins, Kits and Reagents