vitamin k-1

8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridine-6-car is a H+/K+ ATPase inhibitor with IC50 of 0.38μM.

K-Ras-IN-1 is a K-Ras inhibitor.

Cyclin K degrader 1 is a Cyclin K degrader.Cyclin K degrader 1 is a degrader converted from AT-7519.Cyclin K degrader 1 has weak degrading activity against Cyclin K but does not result in a sustained decrease in degradation affinity.Cyclin K degrader 1 is a degrader converted from AT-7519.

PROTAC K-Ras Degrader-1 is potent degrader of K-Ras based PROTAC.

High affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). Blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.

Vitamin K (Kephton) has blood coagulation action and is important for coagulation factors, matrix-Gla protein, and osteocalcin.

K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C.

K-(D-1-Nal)-FwLL-NH2 TFA is a potent and high-affinity inverse agonist of the ghrelin receptor, exhibiting Ki values of 4.9 nM in COS7 cells and 31 nM in HEK293T cells. This compound effectively inhibits ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.

K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ.It binds to the farnesyl binding pocket of PDEδ(Kd of 8 nM).

K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1].

Vitamin K1 (Phylloquinone) a fat-soluble, naturally occurring vitamin with antihemorrhagic and prothrombogenic activity.

SARS-CoV-2-IN-66 (1), a derivative of vitamin K, functions as an inhibitor of SARS-CoV-2, exhibiting an effective concentration (EC50) of 70.8 μM in VeroE6/TMPRSS2 cells [1].

2-(Isopentylamino)naphthalene-1,4-dione is a vitamin K analog.1It inhibits spasms induced by pentylenetetrazole and tonic hindlimb extension induced by maximal electroshock (MES) in mice (ED50s = 349.2 and 108.1 mg/kg, respectively). It also protects mice against seizures in the 6 Hz psychomotor seizure test (ED50s = 152.7 and 263.7 mg/kg at stimulus intensities of 32 and 44 mA, respectively). 1.Li, X., Himes, R.A., Prosser, L.C., et al.Discovery of the first vitamin K analogue as a potential treatment of pharmacoresistant seizuresJ. Med. Chem.63(11)5865-5878(2020)

SARS-CoV-2-IN-67 (Compound 16), a derivative of vitamin K, exhibits anti-SARS-CoV-2 properties, with an effective concentration (EC50) of 64.8 μM in VeroE6/TMPRSS2 cells, and inhibits SARS-CoV-2 RdRp activity [1].

Cis-Vitamin K1 is an endogenous metabolite of Vitamin K [1] .

Activated Protein C (390-404), human, a peptide derived from the vitamin K-dependent serine protease, effectively suppresses the anticoagulant activity of APC[1].

Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity [3]. Betrixaban, now developed by Portola Pharmaceuticals Inc., is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE [2]. VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients [4].

Phenprocoumon is an antagonist of vitamin K(IC50:1 μM).

Vitamin K1 2,3-epoxide (Phylloquinone oxide) is reduced to vitamin k and is involved in the vitamin k cycle.

PPM-18 (NSC 73233) is a potent anti-inflammatory agent which inhibits nitric oxide synthase expression. PPM-18 is a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter [1]. PPM-18 is an analog of Vitamin K remarkably suppressed the proliferation and induced apoptosis in bladder cancer cells [2].

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

Tecarfarin (ATI-5923) is an orally active and potent vitamin K epoxide reductase (VKOR) antagonist and cannabinoid-1 receptor inverse agonist with antithrombotic activity that attenuates abdominal pain and increases intestinal transit in mice.

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.