amg 1

AMG-1 is a specific CRAC channel inhibitor. AMG-1 blocks the function of effector T cells, but not regulatory T cells in vitro and it attenuates the progression and severity of EAE in vivo.

SYN1143 (AMG-1) is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol L, respectively.

AMG-Tie2-1 is a potent inhibitor of endothelial endothelial cell kinase 2 (Tie2) and VEGFR2 with anticancer and antitumor activity that affects cardiovascular production, and may be used in the study of cardiovascular disease and cancer.

AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

AMG 517 is an effective and specific TRPV1 antagonist, antagonizes proton (IC50: 0.76 nM), capsaicin (IC50: 0.62 nM), and heat activation (IC50: 1.3 nM) of TRPV1.

AMG-208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1.

AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM

AMG-548 dihydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulate

Anakinra (Raleukin) is a cytokine inactivator and interleukin 1 receptor antagonist that can be used to study secondary phagocytic lymphohistiocytosis and rheumatoid arthritis.

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

Tapotoclax (AMG-176) is an orally active MCL1 inhibitor for the study of myeloid leukemia.

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks (Kis of 4 nM, 6 nM, 2 nM, and 1 nM for PI3Kα, β, δ, and γ, respectively), exhibiting anti-tumor activity in a mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling as indicated by a decrease in p-Akt (Ser473).

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t

AMG-25 (c-Kit-IN-5-1) is a selective and potent c-Kit inhibitor that inhibits c-Kit, KDR, p38, Lck, and Src, and can be used in the study of mast cell-associated fibrosis.

AMG-076 is an antagonist of melanin-concentrating hormone receptor 1. It also reduced hERG inhibition.

AMG-548 hydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and a 1000-fold selectivity for p38γ and p38δ. AMG 548 hydrochloride also effectively inhibits whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 hydrochloride directly inhibited casein kinase 1 isoforms δ and ε, which in turn inhibited Wnt signaling.

AMG 925 HCl is a selective and potent dual inhibitor of FLT3 (IC50: 2±1 nM) and CDK4 (IC50: 3±1 nM).

AMG-548 dihydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and >1000-fold selectivity for p38γ and p38δ. AMG-548 dihydrochloride exhibits inhibition of whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 dihydrochloride directly inhibited casein kinase 1 isoforms δ and ε, and inhibited Wnt signaling.

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A B C with IC50 values of 5 nM, 4 nM, and 1 nM, respectively. It exhibits over 10-fold selectivity for Aurora kinases compared to p38α, Tyk2, JNK2, Met, and Tie2. [Phase 1].

AMG 925 is a potent and orally bioavailable dual FLT3 CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.

BI-0314 is a selective allosteric STEP activator.

AMG-315 is a Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes. AMG-315 is a chiral arachidonoyl ethanolamide (AEA) analogue or (13S,1′R)-dimethylanandamide. AMG-315 is a high affinity ligand for the CB1 receptor (Ki of 7.8 ± 1.4 nM) that behaves as a potent CB1 agonist in vitro (EC50 = 0.6 ± 0.2 nM). AMG-315 is the first potent AEA analogue with significant stability for all endocannabinoid hydrolyzing enzymes as well as the oxidative enzymes COX-2. AMG-315 will serve as a very useful endocannabinoid probe.

AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.