kinase

Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor), an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.

SAR348830 is an ALK inhibitor, targeting anaplastic lymphoma kinase.

Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and exhibit synergy with the anti-cancer drug doxorubicin against breast cancer cells.

Methacycline hydrochloride (Rondomycin) is a broad-spectrum semisynthetic antibiotic related to TETRACYCLINE but excreted more slowly and maintaining effective blood levels for a more extended period.

Adrenalone hydrochloride (Adrenalone HCl) is a dopamine β-oxidase inhibitor with a similar structure to the norepinephrine transporter (NET) ligand, with an IC50 of 36.9 μM. It is an adrenergic agonist that acts as a local vasoconstrictor and hemostatic agent.

Acyclovir (Aciclovir) is a guanine analog and orally active antiviral agent characterized by a narrow antiviral spectrum, high selectivity, and low toxicity. Acyclovir exhibits activity against HSV-1 (IC50 = 0.85 μM), HSV-2 (IC50 = 0.86 μM), and varicella-zoster virus. Acyclovir can be used for herpesvirus treatment research.

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).

Cytidine 5'-diphosphate trisodium salt (CDP) catalyzes the production of Cytidine triphosphate (CTP) for DNA and RNA synthesis by transferring a phosphoryl group from ATP to cytidine monophosphate (CMP) through the action of uridine monophosphate kinase (UMPK).

BAMB-4 (ITPKA-IN-C14) is a highly membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA), effectively suppressing the metastasis-promoting effect of ITPKA in lung tumor cells (with IC50 of 37 μM in ADP-Glo Assay).

SU4984 is a cell-permeable, ATP-competitive and reversible inhibitor of the fibroblast growth factor receptor 1 (FGFR1).

DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro and tumor growth in vivo[1].

ALK inhibitor 1 is a selective ALK kinase inhibitor.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

BRD0705 is a potent, orally active GSK3α inhibitor with high selectivity (IC50: 66 nM; Kd: 4.8 μM), demonstrating an 8-fold higher selectivity for GSK3α compared to GSK3β (IC50: 515 nM).

Tarlox-TKI (Kinase inhibitor-1) is a pan-ErbB inhibitor, the active ingredient of Tarloxotinib, with antitumor activity.Tarlox-TKI inhibits NRG1 and suppresses HER2 mutants.

PKR-IN-2 is a activator of pyruvate kinase (PKR).

PTC299 ((4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate) is an orally active inhibitor of VEGFA mRNA translation and selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydrolactate dehydrogenase (DHODH).

SGC-AAK1-1, a potent and selective inhibitor of AAK1 (AP2-associated kinase 1), has an IC50 of 270 nM and a Ki of 9 nM, and serves as a chemical probe.

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.

AZD-3463 (ALK/IGF1R inhibitor), an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency.

Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors[1].