ms-98

MS98 is a highly effective and specific PROTAC AKT degrader compound that effectively targets and depletes total AKT (T-AKT) within cells, exhibiting a DC 50 value of 78 nM. This compound readily binds to AKT1, AKT2, and AKT3 with respective dissociation constants (Kd s) of 4 nM, 140 nM, and 8.1 nM.

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl/Prkl family of serine/threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.

BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614 exhibits significant antithrombotic effects.

BMS-986365 (CC-94676) is an orally available, selective and highly potent AR degrader with potential anticancer activity that inhibits AR signaling and suppresses tumor growth for the study of prostate cancer.

BMS-986169 is a high-affinity and selective negative allosteric modulator of the NMDA receptor GluN2B subunit, with an IC50 of 24 nM in oocytes, and exhibits antidepressant-like activity in mice, making it a potential treatment for treatment-resistant depression.

BMS-986224 is an orally active, potent, and selective APJ receptor agonist. BMS-986224 has the potential to study heart failure.

BMS-986449 is an IKZF2 (Helios)/IKZF4 (Eos) degrader and CELMoD molecular glue. It redirects the interaction between the E3 ubiquitin ligase Cereblon and Helios/Eos in primary Treg cells, inducing their degradation, and may be utilised for anti-tumour immunotherapy.

BMS-986470 is a CRBN E3 ubiquitin ligase modulator (CELMoD) that activates fetal hemoglobin (HbF). It is an orally available molecular glue degradator targeting ZBTB7A and WIZ protein degradation, thereby inducing gamma globin synthesis and activating HbF. It is applicable for studying sickle cell disease (SCD).

BMS-986463 is a WEE1 kinase molecule gel degrader and a CRBN E3 ligase regulator (CELMoD). BMS-986463 significantly inhibits tumor regression and reduces the level of phosphorylated CDK2. BMS-986463 can be used in the research of advanced malignant solid tumors such as non-small cell lung cancer (NSCLC).

BMS-986242 is an orally active, potent, and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, suitable for cancer research.

BMS-983970 is an oral inhibitor of pan-Notch, and for the treatment of multiplecancers.

BMS-986120 is a first-in-class oral, reversible protease-activated receptor 4 (PAR4) antagonist with IC50s of 9.5 nM in human blood and 2.1 nM in monkey blood, exhibiting potent and selective antiplatelet effects[1][2].

BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells.

BMS-986163 is an effective GluN2B negative allosteric modulator prodrug that converts to the active form BMS-986169 (Ki=4 nM, IC50=24 nM) in vivo, exhibiting antidepressant-like activity in mice.

BMS-986458 is a highly selective, orally active BCL6 PROTAC degrader. It specifically targets cereblon (CRBN) and the BCL6 N-terminal BTB domain to catalyze proximity-induced BCL6 degradation. BMS-986458 is applicable for research in B-cell non-Hodgkin lymphoma.

BMS-986238 is a second-generation macrocyclic peptide and an effective PD-L1 inhibitor. It holds potential for research in the treatment of solid tumors and lymphomas (cancer of the lymphatic system).

(R,R)-BMS-986397 is a CK1α degrader with a DC50 ranging from 0.1 to 0.5 pM. This compound is applicable in leukemia research.

BMS-986497 (ORM-6151) is a CD33-targeted antibody conjugated with a GSPT1 degrader. It delivers the GSPT1 degrader SMol006 to CD33-expressing cells, inducing the degradation of the GSPT1 protein. BMS-986497 holds potential for research in acute myeloid leukemia (AML).

BMS-986104 is a potent and selective S1P1 receptor modulator.

BMS-986118 is a full agonist of GPR40, is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial a

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

BMS-986124 is an allosteric modulator of the μ-Opioid Receptor.

INX 08189 is an RNA-directed RNA polymerase (NS5B) inhibitor.

BMS-984923 is an orally available and blood-brain barrier permeable mGluR5 silencing allosteric modulator that inhibits β-amyloid oligomer-induced aberrant synaptic signaling, and can be used to study Alzheimer's disease.