Cat. No.: HY-13281

PIK-75 hydrochloride

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC₅₀s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM). PIK-75 hydrochloride induces apoptosis.

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

Purity: 99.66%
CAS No.: 372196-77-5
Formula: C₁₆H₁₅BrClN₅O₄S
Molecular Weight:488.74

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

PIK-75 hydrochloride Chemical Structure

CAS No.: 372196-77-5

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

DNA-PK

2 nM (IC₅₀)

p110α

5.8 nM (IC₅₀)

p110γ

76 nM (IC₅₀)

p110δ

510 nM (IC₅₀)

p110β

1.3 μM (IC₅₀)

hsVPS34

2.6 μM (IC₅₀)

PI3KC2β

1 μM (IC₅₀)

PI3KC2α

10 μM (IC₅₀)

mTORC1

1 μM (IC₅₀)

mTORC2

10 μM (IC₅₀)

ATM

2.3 μM (IC₅₀)

ATR

21 μM (IC₅₀)

PI4KIIIβ

50 μM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.058 μM Compound: 8c	Inhibition of serum-induced proliferation of human A375 cells Inhibition of serum-induced proliferation of human A375 cells	[PMID: 17601739]
A549	IC₅₀	0.069 μM Compound: 8c	Inhibition of serum-induced proliferation of human A549 cells Inhibition of serum-induced proliferation of human A549 cells	[PMID: 17601739]
HeLa	IC₅₀	0.051 μM Compound: 8c	Inhibition of serum-induced proliferation of human HeLa cells Inhibition of serum-induced proliferation of human HeLa cells	[PMID: 17601739]
MCF7	IC₅₀	0.019 μM Compound: 8c	Inhibition of serum-induced proliferation of human MCF7 cells Inhibition of serum-induced proliferation of human MCF7 cells	[PMID: 17601739]
MCF7	IC₅₀	0.039 μM Compound: 8c	Inhibition of serum-induced proliferation of human adriamycin-resistant MCF7 cells Inhibition of serum-induced proliferation of human adriamycin-resistant MCF7 cells	[PMID: 17601739]
Sf9	IC₅₀	0.04 μM Compound: 8c	Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.1 μM Compound: 8c	Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.85 μM Compound: 8c	Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.0003 μM Compound: 8c	Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.3 nM Compound: 8c	Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]

In Vitro

PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC₅₀s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively^[1].
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC₅₀ values of 1.2 and 1.3 μM, respectively^[1].
PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC₅₀ of 78 nM^[2].
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death^[3].
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells^[3].

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

Cell Viability Assay^[3]

Cell Line:

Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1)
Concentration:

0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM
Incubation Time:

48 hours
Result:

Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment.

Western Blot Analysis^[2]

Cell Line:

Overnight-starved CHO-IR cells
Concentration:

1, 10, 100, 1000 nM
Incubation Time:

5 minutes
Result:

Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner.

In Vivo

PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice^[3].

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

Animal Model:

Mice bearing tumors of MIA PaCa-2^[3]
Dosage:

2 mg/kg; or combination with Gemcitabine (20 mg/kg)
Administration:

Administered injection; 5 times per week. 25 days
Result:

Reduced the tumor growth and enhanced the antitumor effect.

Chemical Information

CAS No. 372196-77-5
Appearance Solid
Molecular Weight 488.74
Formula C₁₆H₁₅BrClN₅O₄S
Color White to off-white
SMILES

BrC(C=C1)=CN2C1=NC=C2/C=N/N(S(=O)(C3=C(C=CC([N+]([O-])=O)=C3)C)=O)C.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (5)

All

Sort by:

Journal Impact Factor

Adv Sci (Weinh)

TRIM24 Cooperates with Ras Mutation to Drive Glioma Progression through snoRNA Recruitment of PHAX and DNA-PKcs. [Abstract]

2024 Jun 3:e2400023. PMID: 38828688
Clin Cancer Res

Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Cell Rep

Meteorin-like alleviates hepatic steatosis by regulating hepatic triglyceride secretion and fatty acid oxidation. [Abstract]

2025 Feb 5;44(2):115246. PMID: 39918960
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Res Sq

Haploinsufficiency of ZNF251 causes DNA-PKcs-dependent resistance to PARP inhibitors in BRCA1-mutated cancer cells. [Abstract]

2023 Apr 6:rs.3.rs-2688694. PMID: 37066268

Solvent & Solubility

In Vitro:

DMSO : 11 mg/mL (22.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0461 mL

10.2304 mL

20.4608 mL

5 mM

0.4092 mL

2.0461 mL

4.0922 mL

10 mM

0.2046 mL

1.0230 mL

2.0461 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. [Content Brief]

[2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [Content Brief]

[3]. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69. [Content Brief]

[4]. Hayakawa M, Kawaguchi K, Kaizawa H, et al. Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007;15(17):5837-5844. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0461 mL	10.2304 mL	20.4608 mL	51.1519 mL
	5 mM	0.4092 mL	2.0461 mL	4.0922 mL	10.2304 mL
	10 mM	0.2046 mL	1.0230 mL	2.0461 mL	5.1152 mL
	15 mM	0.1364 mL	0.6820 mL	1.3641 mL	3.4101 mL
	20 mM	0.1023 mL	0.5115 mL	1.0230 mL	2.5576 mL

Keywords

PIK-75 hydrochloride

5 Cited Publications

100 mg Get Quote

Subscribe to the

MedChemExpress

Newsletter

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PIK-75 hydrochloride

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) PIK-75 hydrochloride

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (5)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PIK-75 hydrochloride Related Classifications

HY-13281 Related Classifications