TK-1

Carotegrast methyl (AJM300), an orally-active small molecule, can antagonize the α4 integrin receptor. It is a specific and dual α4β1 α4β7 integrin antagonist.

JTK-109 is an inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitor and inhibits G1b and G3a subgenomic replicons and recombinant enzymes.

STK-15 is a candidate for use as an inhibitor of fatty acid binding protein 5 (FABP5).

TK-129 is an orally active, potent inhibitor of KDM5B with an IC50 of 44 nM and is low-toxicity. TK-129 exhibits cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 can be used in cardiovascular disease studies to reduce isoprenaline-induced myocardial remodelling and fibrosis in vivo, as well as to reduce ang II-induced activation of cardiac fibroblasts in vitro [1].

JTK-101 is a potent and selective Tat-dependent HIV-1 replication inhibitor.

YTK-105 is a ligand targeting autophagy that binds to p62.

gamma-preprotachykinin amide (72-92) acetate is a 21 amino acid peptide belonging to the tachykinin (TK) family and including neurokinin A (NKA) in its C-terminal sequence. gamma-preprotachykinin amide (72-92) acetate possesses higher affinity than NKA for central NK-2 receptors; it shows lower affinity for NK-1 receptors, however, it potently stimulates salivary secretion, which is mediated by NK-1 receptor activation.

Lon-TK is a glycolysis inhibitor of LTB, linked with a linker conjugate. LTB is an intelligent responsive prodrug, comprised of Lonidamine (Lon) and a PD-L1 inhibitor (BMS-1), which are connected through a thioketal linkage. It effectively inhibits glycolytic metabolism in tumor cells and blocks the PD-1 PD-L1 immune escape pathway. Lon-TK holds potential for use in photodynamic-enhanced immunotherapy research.

LTB is a prodrug formed through the conjugation of the glycolysis inhibitor (Lonidamine) and the PD1 PDL1 blocker (BMS-1) via a thioketal bond. LTB can encapsulate the photosensitizer Chlorin e6 (Ce6), constructing a co-delivery photodynamic nanoplatfform through self-assembly (LTB-6 NPs).

A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16 46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th

NSC81111 shows anticaner effects which is a potent and orally active inhibitor of EGFR-TK (IC50 = 0.15 nM) [1].

NSC114126 is a highly effective and orally bioavailable inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR-TK). This compound exhibits robust antiproliferative properties, making it a promising candidate for further investigation in the field of cancer research [1].

AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. It inhibits FLT3 autophosphorylation and induces a dose-dependent cytotoxic response (mean IC50 = 1 μM). AKN-028 acetate also induces apoptosis by activation of caspase 3 and can be used in acute myeloid leukemia (AML) research [1].

NSC381467, a potent and orally active inhibitor of the EGFR tyrosine kinase (EGFR-TK), exhibits robust antiproliferative activity, making it a promising candidate for cancer research [1].

EGFR-IN-51 (Compound 6) is a highly potent EGFR inhibitor with IC50 values of 0.493, 102.60, and 461.63 μM against EGFR, EGFR L858R-TK, and EGFR T790M-TK targets, respectively. Additionally, EGFR-IN-51 exhibits cytotoxicity against cancer cell lines, effectively inducing apoptosis [1].

EGFR-IN-52 (Compound 4) is a highly effective inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 0.358, 86.02, and 432.67 μM against EGFR, EGFR L858R-TK, and EGFR T790M-TK, respectively. Additionally, it demonstrates potent cytotoxic effects on cancer cell lines and triggers apoptosis [1].

EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR tyrosine kinase (EGFR-TK) inhibitor with an IC50 of 0.054 μM. It also inhibits VEGFR-2, CK2α, topoisomerase IIβ, and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13, and 3.61 μM, respectively. The compound promotes cell cycle arrest at the G2 M and pre-G1 phases and induces apoptosis in cancer cells [1].

HSV-1 HSV-2-IN-1 is an HSV-1 and HSV-2 inhibitor effective against HSV-1 (KOS) (EC50: 7.6 μM), HSV-2 (G) (EC50: 7.6 μM), HSV-1 TK-KOS ACVr (EC50: 4 μM), and cowpox virus (EC50: 12 μM).

Transketolase-IN-3, a potent inhibitor of transketolase (TK), exhibits herbicidal activity by effectively suppressing Digitaria sanguinalis (DS) and Amaranthus retroflexus (AR). This compound holds potential for herbicide research applications [1].

EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer. It exhibits anti-proliferative properties, impedes EGFR phosphorylation, and induces G2 M phase cell cycle arrest [1].

Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19 T790M C797S TK and 113 nM for EGFRL858R T790M C797S TK. It effectively suppresses EGFR phosphorylation, induces G1 phase arrest, and triggers apoptosis in KC-0116 (BaF3-EGFRDel19 T790M C797S) cells. Moreover, Os30 demonstrates strong antitumor activity in non-small cell lung cancer (NSCLC) harboring the EGFmRC797S mutation [1].

Locustatachykinin II (Lom-TK II), an insect neuropeptide analogous to the vertebrate tachykinin family, serves as a research tool for investigating insect endocrine systems [1].

(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor that preferentially inhibits the TK activity of the EGF receptor, restricting the EGF-stimulated growth of cultured cells. It demonstrates an IC50 of 11 μM for DNA synthesis in HN5 cells, showcasing thrice the potency of its isomer, (E)-RG-13022 (IC50 = 38 μM). This compound is applied in breast cancer cell research [1] [2].

Oxythiamine (Hydroxythiamine) chloride, a thiamine antagonist and analogue of anti-metabolite, inhibits transketolase (TK) and suppresses the non-oxidative synthesis of ribose, leading to cell apoptosis. It inhibits cancer cell proliferation and induces apoptosis [1] [2] [3].