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Cat. No.: HY-13007B

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PF-3758309 dihydrochloride

(Synonyms: PF-03758309 dihydrochloride)

11 Cited Publications

Customer Review

Based on 11 publication(s) in Google Scholar

PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

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

Formula: C₂₅H₃₂Cl₂N₈OS
Molecular Weight:563.55

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

PF-3758309 dihydrochloride Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PAK4

18.7 nM (Ki)

PAK1

13.7 nM (Ki)

PAK5

18.1 nM (Ki)

PAK6

17.1 nM (Ki)

PAK2

190 nM (IC₅₀)

PAK3

99 nM (IC₅₀)

PAK4

2.7 nM (Kd)

All PAK Isoforms :

In Vitro

PF-3758309 dihydrochloride has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, K_i=18.1 nM; PAK6, K_i=17.1 nM) and group A PAK1 (K_i=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC₅₀=190 nM; PAK3, IC₅₀=99 nM)^[1].
In cells, PF-3758309 dihydrochloride inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC₅₀=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC₅₀=4.7 nM)^[1].
PF-3758309 dihydrochloride also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC₅₀=20 nM) and anchorage-independent growth (IC₅₀=27 nM) of A549 cells^[1].

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

In Vivo

PF-3758309 dihydrochloride (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models^[1].

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

Animal Model:

Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors)^[1]
Dosage:

7.5-30 mg/kg
Administration:

Oral administration; twice daily for 9-18 days
Result:

Significant tumor growth inhibition (TGI) in HCT116 and A549 models.

Chemical Information

Molecular Weight 563.55
Formula C₂₅H₃₂Cl₂N₈OS
SMILES

CC1=NC2=C(SC=C2)C(NC3=NNC4=C3CN(C(N[C@@H](C5=CC=CC=C5)CN(C)C)=O)C4(C)C)=N1.[H]Cl.[H]Cl
Synonyms

PF-03758309 dihydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (11)

All OthersCell Imaging/StainingCell Proliferation/Viability Assay

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Int J Mol Sci

Inhibition of NAMPT by PAK4 Inhibitors. [Abstract]

2024 Sep 21;25(18):10138. PMID: 39337621

PF-3758309 dihydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Sep 21;25(18):10138. [Abstract]

NAMPT activity in response to PAK4 inhibitors (KPT-9274, PF-3758309, GNE2861, and LCH7749944), group I (PAK1-3) inhibitors (IPA-3 and FRAX486), phloretin (a natural compound unrelated to kinase inhibitors), MEK inhibitors (BI-847325 and PD0325901), the solvent control (DMSO), and FX866, the positive control.
Biochem J

Up-regulation of the PI3K/AKT and RHO/RAC/PAK signalling pathways in CHK1 inhibitor resistant Eµ-Myc lymphoma cells. [Abstract]

2022 Oct 14;479(19):2131-2151. PMID: 36240067
Exp Cell Res

PAK5 promotes the cell stemness ability by phosphorylating SOX2 in lung squamous cell carcinomas. [Abstract]

2020 Oct 15;395(2):112187. PMID: 32721391
Anticancer Drugs

AZD7762 induces CRBN dependent BAG3 degradation through ubiquitin-proteasome pathway. [Abstract]

2024 Jan 1;35(1):46-54. PMID: 37449977
bioRxiv

2026 May 29.
bioRxiv

2025 April 26.

PF-3758309 dihydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 April 26.

Viability of CUTO32 and LC-2/Ad cells upon co-treatment with pralsetinib and the PAK inhibitor PF-3758309 (CUTO32: 1 μM; LC2/Ad: 0.1 μM) for 3 days .
bioRxiv

Network analysis of α-synuclein pathology progression reveals p21-activated kinases as regulators of vulnerability. [Abstract]

2024 Oct 22:2024.10.22.619411. PMID: 39484617

PF-3758309 dihydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Oct 22:2024.10.22.619411. [Abstract]

Representative images of pS129 α-synuclein in vehicle treated neurons compared to neurons treated with the highest dose of PF-3758309 or GNE2861.
Necmettin Erbakan University

2022 Jun.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Murray, Brion W., et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(20), 9446-9451, S94. [Content Brief]

[2]. Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70. [Content Brief]

[3]. Ryu BJ, et al. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings. Mol Cell Biochem. 2014 Apr;389(1-2):69-77. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

PF-3758309 dihydrochloride

11 Cited Publications

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Purity & Documentation
References

1/16
1/16

PF-3758309 dihydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 April 26.

Customer Validation
Viability of CUTO32 and LC-2/Ad cells upon co-treatment with pralsetinib and the PAK inhibitor PF-3758309 (CUTO32: 1 μM; LC2/Ad: 0.1 μM) for 3 days .
1/16

PF-3758309 dihydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Sep 21;25(18):10138. [Abstract]

Customer Validation
NAMPT activity in response to PAK4 inhibitors (KPT-9274, PF-3758309, GNE2861, and LCH7749944), group I (PAK1-3) inhibitors (IPA-3 and FRAX486), phloretin (a natural compound unrelated to kinase inhibitors), MEK inhibitors (BI-847325 and PD0325901), the solvent control (DMSO), and FX866, the positive control.
1/16

PF-3758309 dihydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Oct 22:2024.10.22.619411. [Abstract]

Customer Validation
Representative images of pS129 α-synuclein in vehicle treated neurons compared to neurons treated with the highest dose of PF-3758309 or GNE2861.

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PF-3758309 dihydrochloride

Publications Citing Use of MedChemExpress (MCE) PF-3758309 dihydrochloride

All PAK Isoforms

Biological Activity

Chemical Information

Publications (11)

Purity & Documentation

References

Calculators

Help & FAQs

PF-3758309 dihydrochloride Related Classifications

HY-13007B Related Classifications