2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis
  3. PDGFR Carbonic Anhydrase STAT Akt ERK Apoptosis Caspase
  4. PDGFRA/CAIX/XII-IN-1

PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia.

For research use only. We do not sell to patients.

PDGFRA/CAIX/XII-IN-1

PDGFRA/CAIX/XII-IN-1 Chemical Structure

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PDGFRA/CAIX/XII-IN-1 Related Antibodies

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PDGFR PDGFRβ PDGFRα

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CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

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STAT3 STAT5 STAT6 STAT1

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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

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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

  • Biological Activity

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Description

PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia[1].

IC50 & Target[1]

CA IX

93.3 nM (Ki)

CA XII

80 nM (Ki)

STAT3

 

ERK1

 

ERK2

 

Caspase-9

 

Caspase 3

 

In Vitro

PDGFRA/CAIX/XII-IN-1 (Compound 9d) potently inhibits recombinant PDGFRA protein, with an IC50 of 20 nM[1].
PDGFRA/CAIX/XII-IN-1 (1 μM) exerts targeted inhibitory effects on specific RTK subfamilies, and exhibits potent activity against PDGFRα and closely related class III RTKs[1].
PDGFRA/CAIX/XII-IN-1 inhibits recombinant human cancer-associated CA IX (Ki = 93.3 nM) and CA XII (Ki = 80.0 nM) with moderate potency, while exhibiting only weak activity against normal CA I/II isoforms[1].
PDGFRA/CAIX/XII-IN-1 (72 h) potently inhibits the proliferation of FIP1L1-PDGFRA-driven EOL-1 eosinophilic leukemia cells (GI50 = 2 nM), also exhibits significant cytotoxicity against MV4-11 cells (GI50 = 0.263 μM), and shows weak cytotoxicity against Kasumi-1 and RS4-11 cells with GI50 values of 2.081 μM and 4.599 μM, respectively[1].
PDGFRA/CAIX/XII-IN-1 (0-2500 nM; 1 h) dose-dependently inhibits the phosphorylation of FIP1L1-PDGFRA and its downstream STAT3, AKT and ERK1/2 signaling pathways in EOL-1 cells; after treatment at a concentration of 100 nM for 1 h, the inhibitory effect on PDGFRA is nearly complete[1].
PDGFRA/CAIX/XII-IN-1 (0-2500 nM; 24 h) induces apoptosis in EOL-1 eosinophilic leukemia cells by activating the intrinsic apoptotic pathway. The effect is detectable at a concentration of 0.8 nM, and the pathway is potently activated at subnanomolar concentrations, while no pro-apoptotic effect is observed on THP-1 cells[1].
PDGFRA/CAIX/XII-IN-1 (0.16-100 nM; 24 h) induces dose-dependent G0/G1 cell cycle arrest in EOL-1 eosinophilic leukemia cells, with a significant arrest effect observed at 0.8 nM; additionally, after 24 h of treatment, concentrations of 4 nM and above induce apoptotic cell death (characterized by a sub-G1 cell population)[1].

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

PDGFRA/CAIX/XII-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: EOL-1 cells
Concentration: 0, 4, 20, 100, 500, 2500 nM
Incubation Time: 1 h
Result: Induced a dose-dependent inhibition of FIP1L1-PDGFRA phosphorylation (p-PDGFRA/B Y849/857), with substantial reduction at 20 nM and near-complete dephosphorylation at 100 nM.
Reduced phosphorylation of downstream signaling molecules STAT3 (p-STAT3 Y705) from 20 nM upward, AKT (p-AKT S473) with substantial inhibition at 100 nM and above, and ERK1/2 (p-ERK1/2 T202/Y204) with strong inhibition from 100 nM.
Maintained unchanged total protein levels of PDGFRA, STAT3, AKT, and ERK1/2.

Apoptosis Analysis[1]

Cell Line: EOL-1 cells, THP-1 cells
Concentration: 0.032, 0.16, 0.8, 4, 20, 100, 500 2500 nM (caspase 3/7 activity, Western blot); 0.16, 4, 100 nM (Annexin V/PI staining)
Incubation Time: 24 h
Result: In EOL-1 cells: induced dose-dependent cleavage of PARP-1 (detectable at 0.8 nM, accumulating at 4 nM and higher), reduced antiapoptotic Mcl-1 expression (substantial reduction at 4 nM, near-complete depletion at 20 nM), activated caspase 9 (cleavage detected at 4 nM and higher) and caspase 3 (cleavage detected at 4 nM and higher).
Caused a robust, dose-dependent increase in caspase 3/7 activity (significant activation at 0.032 nM, ~7-fold increase at 0.8 nM).
Induced a concentration-dependent shift from viable cells to early and late apoptotic populations via Annexin V/PI staining.
In THP-1 cells: showed no significant signs of apoptosis or caspase 3/7 activation at tested concentrations.

Cell Cycle Analysis[1]

Cell Line: EOL-1 cells
Concentration: 0.16, 0.8, 4, 20, 100 nM
Incubation Time: 24 h
Result: Caused a dose-dependent accumulation of cells in the G0/G1 phase, accompanied by a decrease in S and G2/M populations.
Induced modest G0/G1 arrest at 0.16 nM, significant arrest at 0.8 nM and higher.
Triggered a sub-G1 apoptotic population from 4 nM onward, which expanded markedly at 20 and 100 nM.
Molecular Weight

507.56

Formula

C25H25N5O5S
SMILES

O=C(NC1=CC(S(=O)(N)=O)=C(C=C1)C)NC2=CC=C(C=C2)NC3=C4C=C(C(OC)=CC4=NC=C3)OC
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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PDGFRA/CAIX/XII-IN-1 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:

PDGFRA/CAIX/XII-IN-1PDGFRCarbonic AnhydraseSTATAktERKApoptosisCaspasePlatelet-derived growth factor receptorCarbonate dehydratasePKBProtein kinase BExtracellular signal regulated kinasesPDGFRA/CA IX/CA XII inhibitorleukemiaEOL-1 cellsTHP-1 cells
Inhibitorinhibitorinhibit

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