k 22

ZIKV-IN-K22 is a potent antiviral agent against a broad range of coronaviruses by targeting membrane-bound viral RNA replication, effectively inhibiting ZIKV with IC50 of 2.1 μM.

BN80933 is a dual inhibitor of lipid peroxidation and neuronal nitric oxide synthase; Neuroprotectant.

PI3Kδ-IN-22 (Compound 26) is a selective inhibitor of PI3Kδ with a pKi value of 9.3. It effectively inhibits the PI3Kδ-AKT signaling pathway in THP-1 cells, demonstrating a pIC50 of 9.4. Additionally, PI3Kδ-IN-22 exhibits favorable pharmacokinetic properties in rats.

LL-K8-22 is a potent, selective, and durable dual degrader of CDK8-cyclin C, demonstrating DC50 values of 2.52 and 2.64 μM, respectively. This compound effectively suppresses STAT1 Ser 727 phosphorylation and inhibits carcinogenic transcriptional programs driven by E2F and MYC. LL-K8-22 is specifically utilized in research for triple-negative breast cancer (TNBC) [1].

PI3Kα-IN-22 (Compound 17) is a potent, selective, and orally active inhibitor targeting the PI3Kα H1047R mutation, exhibiting an IC 50 of 1 nM in the pAKT T47D AlphaLISA assay. It has demonstrated the ability to induce tumor regressions in the HCC1954 tumor model in mice [1].

UK 227786 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.

FK 224 is an antagonist of tachykinin receptor.

GSK 224876 is a novel next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). It has activity against efavirenz-resistant strains in the treatment of treatment-naive HIV-1-infected subjects.

CK 2289 is an inhibitor of type III cyclic 3'5' -adenosine monophosphate phosphodiesterase with potential use in the treatment of congestive heart failure.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1/2/4/6 (IC50=36/47/510/1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator.

Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.

Fosdevirine (GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological related disorders such as late-onset epilepsy.

MK-2295 is a potent TRPV1 antagonist. MK-2295 can be used in studies about the treatment of chronic pain.

GSK2292767 is a potent and selective inhibitor of PI3Kδ.

GSK2292767 FA is a potent and selective inhibitor of PI3Kδ (pIC50 : 10.1).GSK2292767 FA is more than 500-fold more selective than other PI3K isoforms.GSK2292767 FA can be used in the study of respiratory diseases.

N 0861 is a selective adenosine A1 receptor antagonist that attenuates renal insufficiency during adenosine-controlled hypotension in rats.

Ceritinib (LDK378) is an ALK tyrosine kinase inhibitor (IC50=200 pM) with selective, ATP-competitive, and oral activity. Ceritinib also inhibits IGF-1R, InsR, and STK22D (IC50=8/7/23 nM). Ceritinib has antitumor activity.

GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

GSK2256294A (GSK 2256294) is potent, selective inhibitor of recombinant human, rat and mouse sEH with IC50 of 27 pM, 61 pM and 189 pM, respectively.

Retosiban is an effective and selective oxytocin antagonist (Ki: 0.65 nM).

TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5.