ks-i

Perfluorinated SAHA is an HDAC inhibitor for use in cancer treatment regimens, with demonstrated greater antiproliferative properties than SAHA . PFSAHA has also been shown to have higher selectivity for PA3774, an HDAC-like enzyme from P. aeruginosa, as well as other HDACs, which may prove beneficial for developing novel chemotherapeutic treatments for cancer.

KSI-3716 is a c-Myc inhibitor used as a bladder chemotherapy agent. It blocks the formation of the c-MYC/MAX complex with the target gene promoter and induces cell cycle arrest and apoptosis. It can be used for bladder cancer research.

KSI-6666 is an orally effective competitive antagonist of sphingosine 1-phosphate receptor 1 (S1PR1), with an IC50 value of 6.4 nM. It exhibits anti-inflammatory activity in models of autoimmune encephalomyelitis and T-cell transfer-induced colitis.

PI5P4Ks-IN-2 is an inhibitor of the phosphatidylinositol 5-phosphate 4-kinase PI5P4Kγ. Targeting the PI5P4K isoforms, PI5P4Ks-IN-2 inhibited PI5P4Kα, PI5P4Kβ, PI5P4Kγ, and PI5P4Kγ+, with IC50 values of <4.3, <4.6, 6.2, and 0.32, respectively.

DYRKs-IN-1 has antitumor activity. DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively.

DYRKs-IN-2 has antitumor activity. DYRKs-IN-2 is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively.

TNKS-IN-3 (Compound 6) is a TNKS2 inhibitor with a Ki of 8.5 nM. It demonstrates strong activity with an IC50 of 71 nM, effectively inhibiting the WNT/β-catenin signaling pathway, and is useful for research in cancer and fibrosis.

TNKS-IN-41 highly potent and selective inhibitor of tankyrase.

TNKS-IN-1 is a highly potent and selective inhibitor of tankyrase.

PI5P4Ks-IN-1 (compound 7) is an active compound that interacts with PI5P4Kγ[1].

LDHA/PDKs-IN-2 (compound 20k) is a potent dual inhibitor of LDHA and PDKs, with IC50 values of 0.7 and 1.6 μM, respectively. It increases oxygen consumption, decreases lactate formation, and shows potential for cancer research by reducing the proliferation of A549 cells with an EC50 of 15.7 μM [1].

LDHA/PDKs-IN-1 (compound 20e) is a highly effective dual inhibitor of PDKs and LDHA, with IC50 values of 0.8 μM and 0.15 μM, respectively. It significantly suppresses A549 cell proliferation (EC50 = 13.2 μM), reduces lactate formation, and enhances oxygen consumption, holding great promise for cancer research [1].

DYRKs-IN-1 hydrochloride is a potent inhibitor of Dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), with IC50 values of 5 nM for DYRK1A and 8 nM for DYRK1B, and exhibits antitumor activity.

SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, functions as an inhibitor of Salt-inducible kinases (SIKs), which play a role in M1/M2 macrophage polarization linked to inflammation. By inhibiting SIK activity, this compound increases anti-inflammatory cytokine IL-10 and decreases pro-inflammatory cytokine IL-12, demonstrating significant anti-inflammatory efficacy in a DSS-induced colitis model [1].

PI5P4Ks-IN-3 (compound 30) is a covalent inhibitor of PI5P4K with inhibition constants (IC50s) of 1.34 μM for PI5P4Kα and 9.9 μM for PI5P4Kβ, but demonstrates weak cellular activity [1].

KS I is a gonadotropin antagonist and is a cyclolignan isolated from extracts of Lycopus and Lithosperum after oxidation with caffeic acid.

HMR 1556 is a chromanol derivative and is an IKs blocker (IC50s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively).

Diazepinomicin is a secondary metabolite produced by Micromonospora sp. It inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. Diazepinomicin also is an anti-tumor agent for K-Ras mutant models.

Bitriben is an agent with the anthelmintic effect.

Gentamicin (Centicin) is a broad-spectrum aminoglycoside antibiotic with antibacterial activity, inhibiting the growth of Gram-positive and Gram-negative bacteria, and can be used to study ocular infections.

Decamethoxine is a biochemical.

KS IV is a cyclolignan isolated from extract of Lycopus and Lithosperum after oxidation with caffeic acid.

PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.

The compound AVSEHQLLHDKGKSIQDLRRRFFLHHLI-{Aib}-EIHTAYRFGG facilitates bone ossification and has potential applications in the study of conditions associated with osteogenic insufficiency or diminished bone mineral density (BMD), including osteoporosis [1].