multi

Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.

Multi-Leu peptide (ML-peptide) triacetate is a potent inhibitor of PACE4 (Ki=22 nM). It functions by competitively binding to the active site of PACE4, mimicking its substrate sequence, thereby inhibiting its catalytic activity. This compound can be utilized to investigate the specific role of PACE4 in the progression of prostate cancer.

Multi-Leu peptide (ML-peptide), with a K i value of 22 nM, acts as a potent inhibitor of PACE4 by competitively binding to its active site and mimicking its substrate sequence, thus suppressing the enzyme's catalytic function. This compound is useful for investigating PACE4's specific role in the progression of prostate cancer.

ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).

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).

Dovitinib lactate hydrate (TKI258) is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.

Multi-kinase-IN-5 (compound 15c) is a multi-kinase inhibitory agent that demonstrates significant inhibition of a range of protein kinases, including RET (69%), KIT (31%), cMet (62%), VEGFR1 (40%), VEGFR2 (73%), FGFR1 (74%), PDGFR (59%), and BRAF (74%). Its IC50 values are 1.287 μM for FGFR1, 0.117 μM for VEGFR, and 1.185 μM for RET kinases, indicating its potency [1].

Multi-kinase inhibitor 3 (compound 12) is an orally active and effective multikinase (multikinase) inhibitor, demonstrating potent IC50 values against FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, and PDGFRβ, at 1.59, 1.23, 1.19, 0.59, 0.22, and 1.15 nM respectively. This compound exhibits anti-proliferative and anticancer activities.

Multi-kinase inhibitor 4 (compound 14) serves as an orally effective inhibitor targeting FLT1, KDR, FLT3, FLT4, PDGFRα, and PDGFRβ, exhibiting IC50 values of 1.97 nM, 1.04 nM, 0.33 nM, 1.44 nM, 0.18 nM, and 0.89 nM respectively. This compound plays a crucial role in cancer research.

Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and a potent chemosensitizer that enhances the number of DNA double-strand breaks induced by Doxorubicin. It serves as an effective multidrug resistance (MDR) inhibitor, demonstrating inhibitory activity against P-glycoprotein (P-gp) mediated drug efflux. Multi-target kinase inhibitor 4 can be encapsulated in PEG-coated lipid nanoparticles.

Multi-target Pt (IV) is an antitumor agent that inhibits the phosphorylation of IKKβ, IκBα, and NF-κB p65, as well as the nuclear translocation of NF-κB p65, ultimately blocking the NF-κB signaling pathway.

Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor with IC50 values of 3.04 nM and 1.57 nM, respectively. It notably suppresses cancer cell proliferation, migration, and invasion, while inducing apoptosis and cell cycle arrest. By inhibiting the phosphorylation of ERK1/2 and downregulating the activity of its downstream substrate RSK, Multi-target kinase-IN-5 exhibits antitumor effects. This compound can be utilized in cancer research.

Multi-target kinase-IN-6 is a multi-target kinase inhibitor. It can inhibit cardiac RyR2 and NaV1.5 channels while stimulating the activity of the SERCA2a pump. Multi-target kinase-IN-6 is applicable in research on cardiovascular diseases, including heart failure.

Multi-kinase-IN-7 is a multi-kinase inhibitor with IC50 values of 2.19, 2.95, 3.59, and 9.31 μM against EGFR, VEGFR2, TrKA, and CDK2, respectively. It demonstrates moderate to weak activity on FAK, AKT1, GSK3β, and CDK5, with IC50 values of 6.3, 9.2, 11.7, and 23.4 μM, respectively. Multi-kinase-IN-7 exhibits broad-spectrum antiproliferative potential against NCI cancer cell lines and can induce cell cycle arrest, apoptosis (apoptosis), and necrosis. MDA-MB-231 is applicable in breast cancer research.

Multi-kinase-IN-8 is a multi-kinase inhibitor. It effectively inhibits COX-1 (IC50 = 12.6 μM), COX-2 (IC50 = 0.05 μM), and VEGFR-2 (IC50 = 0.12 nM). Additionally, it blocks tumor-associated carbonic anhydrases CA IX and CA XII with Ki values of 31.5 nM and 386.9 nM, respectively, and induces cell cycle arrest and apoptosis (apoptosis) by upregulating Caspase-9 and Bax, while downregulating Bcl-2. Multi-kinase-IN-8 also suppresses the expression of PGE2, p-VEGFR-2, MMP-9, and HIF-1α, and demonstrates growth inhibitory activity on breast, lung, and colorectal adenocarcinomas.

Multi-kinase-IN-10 (Compound IIIk) is a multi-kinase inhibitor with notable calcium channel blocking activity, exhibiting an IC50 of 26.67 μM. It acts as a potent dual cholinesterase inhibitor, with IC50 values of 0.304 μM for hAChE and 1.033 μM for hBuChE. Additionally, Multi-kinase-IN-10 demonstrates antioxidant and neuroprotective properties, along with significant anti-amnesic activity, making it suitable for Alzheimer's disease research.

Multi kinase ligand 4 is a target protein ligand utilized in the synthesis of PROTACDB-0646.

Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor, targeting VEGFR-2 with an IC50 of 58.3 nM and PDGFRβ with an IC50 of 55 nM.

Multi-kinase-IN-2 is an orally active inhibitor of angiokinases. multi-kinase-IN-2 significantly inhibits the activity of angiokinases such as VEGFR-1/2/3, PDGFRα/β, FGFR-1, LYN and c-KIT kinases. -IN-2 significantly attenuates phosphorylation of AKT and ERK proteins, induces apoptosis and has anticancer effects.

Multi-kinase-IN-1, a powerful kinase inhibitor, exhibits antitumor properties by inducing cell apoptosis. It is under investigation for its potential application in treating colorectal cancer.

Multi-kinase-IN-4 (compound 5d) is a multi-targeted kinase inhibitor effective against VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18, and 2.09 μM, respectively. It shows broad-spectrum anti-cancer activity in HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50: 1.94–7.1 µM) and exhibits lower toxicity in WI-38 cells (IC50 = 40.85 µM). Additionally, it induces apoptosis, causes S-phase cell cycle arrest in HepG2 cells, and holds potential for cancer research [1].

Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values between 40 to 204 nM. It exhibits cytotoxic effects on HepG2, HeLa, MDA-MB-231, and MCF-7 cell lines, with IC50 values of 41, 57, 51, and 59 μM, respectively. Additionally, it induces cell cycle arrest and apoptosis specifically in HepG2 cells.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX cancer cell lines with IC50s of 3.36 μM, 1.40 μM, and 3.49 μM, respectively. Additionally, Multi-kinase-IN-6 induces cell cycle arrest at the G1/S and G1 phases in MCF7 and HCT116 cells, respectively, and effectively triggers apoptosis [1].