PIK-75

Cat. No.: HY-107834: FAQs
Data Sheet Handling Instructions

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PIK-75 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 inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM). PIK-75 induces apoptosis.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (PIK-75 hydrochloride) usually boasts enhanced water solubility and stability.

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

PIK-75 Chemical Structure

CAS No. : 372196-67-3

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Other In-stock Forms of PIK-75:

Other Forms of PIK-75:

PIK-75 hydrochloride In-stock

3 Publications Citing Use of MCE PIK-75

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•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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)

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. PIK-75 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].

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.

Molecular Weight

452.28

Formula

C₁₆H₁₄BrN₅O₄S

CAS No.

372196-67-3

SMILES

O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)/N=C/C2=CN=C3C=CC(Br)=CN32)=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

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]

PIK-75 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:

PIK-75372196-67-3PIK75PIK 75DNA-PKPI3KApoptosisDNA-dependent protein kinasePhosphoinositide 3-kinasep110αPKBCHO-IRcellspancreaticcancerapoptoticInhibitorinhibitorinhibit

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