2. Immunology/Inflammation Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Apoptosis
  3. COX VEGFR HIF/HIF Prolyl-Hydroxylase Caspase Bcl-2 Family Apoptosis MMP
  4. Multi-kinase-IN-8

Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma.

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Multi-kinase-IN-8

Multi-kinase-IN-8 Chemical Structure

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Multi-kinase-IN-8 Related Antibodies

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COX COX-1 COX-2 COX-3

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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HIF-1α HIF

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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Description

Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma[1].

IC50 & Target[1]

COX-2

0.05 μM (IC50)

COX-1

12.6 μM (IC50)

VEGFR2

0.12 nM (IC50)

In Vitro

Multi-kinase-IN-8 (Compound 5j) inhibits the proliferation of cancer cell lines, with IC50 of 1.30 μM (MB 231 cell), 9.53 μM (MCF-7 cell), 2.07 μM (A549 cell), and 2.28 μM (Caco-2 cell), respectively[1].
Multi-kinase-IN-8 (2.07 μM, 72 h) inhibits VEGFR-2 in Caco-2 cells[1].
Multi-kinase-IN-8 (24 h and 48 h) induces cell cycle arrest at the G1 phase in Caco-2 cells[1].
Multi-kinase-IN-8 (24 h and 48 h) induces cell death by triggering apoptosis in Caco-2 cells[1].
Multi-kinase-IN-8 (24 h and 48 h) downregulates HIF-1α mRNA expression, and reduces PGE2, total VEGFR-2, p-VEGFR-2 production in MDA-MB 231[1].
Multi-kinase-IN-8 has selective targeting potential towards the tumor-associated CA isoforms, particularly hCA IX, due to its interaction with the catalytic zinc binding site[1].
Multi-kinase-IN-8 reduces expression levels of the initiator caspase-9 and mitochondrial apoptotic markers Bcl-2 and Bax in Caco-2 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Multi-kinase-IN-8 Related Antibodies

Cell Migration Assay [1]

Cell Line: Caco-2 cells
Concentration: 2.07 μM
Incubation Time: 72 h
Result: Suppressed Caco-2 cell migration with 56.29 % wound closure.

Cell Cycle Analysis[1]

Cell Line: Caco-2 cells
Concentration:
Incubation Time: 24 h and 48 h
Result: Increased of % Caco-2 cells in G0 / G1 phase from 62.07 % in the control to 86.36 %.
Reduced nearly 3-fold in % Caco-2 cells in both S phase and G2 / M phase.

Apoptosis Analysis[1]

Cell Line: Caco-2 cells
Concentration:
Incubation Time: 24 h and 48 h
Result: Increased 42 fold in total apoptosis.
Increased the ratio of annexin V-FITC positive early apoptotic cells from 0.54 % to 20.26 %, whilst the percentage of late apoptotic cells rose from 0.22 % to 11 %.
Resulted in a combined percentage of early and late apoptotic cells that significantly exceeded the percentage of necrotic cells. (Early apoptotic cells is 20.26%, late apoptotic cells is 11.32%, necrotic cells is 3.61%).
In Vivo

Multi-kinase-IN-8 (Compound 5j) (50 mg/kg, s.c., five consecutive days.) exhibits antitumor activity in an MDA-MB-231 xenograft model established in male BALB/c mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cyclosporine (HY-100563A)-preconditioned (30 mg/kg/day, for 1 week) male BALB/c mice and then injected with MDA-MB 231 cells (1 × 106 per mouse)[1].
Dosage: 50 mg/kg
Administration: s.c., daily, five consecutive days, dissolved in 100 μL of DMSO (HY-Y0320C) /PBS (HY-K3005) (1:20, v/v).
Result: Reduced tumor size.
Induced 92.3 % tumor regression.
Had no significant changes in body weight were observed during the treatment course, indicating a satisfactory safety profile.
Molecular Weight

531.54

Formula

C25H21N7O5S
SMILES

O=S(C1=CC=C(N2N=NC(COC3=CC=C(/C=N/N=C4C(NC5=C\4C=C(OC)C=C5)=O)C=C3)=C2)C=C1)(N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Multi-kinase-IN-8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Multi-kinase-IN-8COXVEGFRHIF/HIF Prolyl-HydroxylaseCaspaseBcl-2 FamilyApoptosisMMPCyclooxygenaseVascular endothelial growth factor receptorHypoxia-inducible factorsHIFsHIF-PHMatrix metalloproteinasesbreast cancerlung cancercolorectal adenocarcinomaInhibitorinhibitorinhibit

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