ms98

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.

BMS-986122 is a IRAK4 Inhibitor. BMS-986126 attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity. BMS-986126 inhibited TLR7- and TLR9-dependent responses using cells derived from lupus patients, suggesting that inhibition of IRAK4 has the potential for therapeutic benefit in treating lupus.

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

BMS986187 is a novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Receptor.

BMS986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor.

BMS986299 is a modulator of NLRP3 with an EC50 of 1.28 μM and can be used in studies about NLRP3 signaling and the treatment of associated diseases.

Deucravacitinib is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12/23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 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.

Afimetoran (BMS-986256) is a toll-like receptor antagonist. Afimetoran can be used in the research of inflammatory and autoimmune diseases.

Linrodostat (BMS-986205) is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1).

Milvexian (BMS-986177/JNJ-70033093) is an orally bioavailable, small-molecule, reversible, and direct antagonist of Factor XIa (FXIa). It exhibits potent inhibitory activity across species, with Ki values of 0.11 nM for human, 0.38 nM for rabbit, and 0.64 nM for dog. By targeting FXIa, Milvexian selectively inhibits the intrinsic pathway of the coagulation cascade. It demonstrates robust antithrombotic efficacy in various in vitro and in vivo models while maintaining a favorable safety profile regarding bleeding risk. It is a critical tool for investigating novel anticoagulant strategies in thrombosis and cardiovascular research.

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.

(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins.

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.