2. PI3K/Akt/mTOR Stem Cell/Wnt JAK/STAT Signaling Immunology/Inflammation Metabolic Enzyme/Protease
  3. PI3K STAT PD-1/PD-L1 Endogenous Metabolite
  4. Pabgraminone C

Pabgraminone C (IM502) is a Fungal metabolite and PI3Kγ inhibitor with an IC50 of 61.7 nM against PI3Kγ. Pabgraminone C shifts the STAT signaling pathway in cells from an immunosuppressive STAT3/STAT6-dominant profile to an immunostimulatory STAT1/STAT2-dominant profile, driving cells toward a pro-inflammatory phenotype. Pabgraminone C reprograms cells from an immunosuppressive state to an immunostimulatory state, reversing their suppressive effect on anti-tumor immunity. Pabgraminone C inhibits established tumor growth and metastasis across multiple cancer types. Pabgraminone C overcomes resistance to PD-1 checkpoint blockade strategies. Pabgraminone C can be used in research related to liver cancer, melanoma, and colorectal cancer.

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Pabgraminone C

Pabgraminone C Chemical Structure

CAS No. : 3061276-55-6

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Pabgraminone C Related Antibodies

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Human Endogenous Metabolite Microbial Metabolite

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Description

Pabgraminone C (IM502) is a Fungal metabolite and PI3Kγ inhibitor with an IC50 of 61.7 nM against PI3Kγ. Pabgraminone C shifts the STAT signaling pathway in cells from an immunosuppressive STAT3/STAT6-dominant profile to an immunostimulatory STAT1/STAT2-dominant profile, driving cells toward a pro-inflammatory phenotype. Pabgraminone C reprograms cells from an immunosuppressive state to an immunostimulatory state, reversing their suppressive effect on anti-tumor immunity. Pabgraminone C inhibits established tumor growth and metastasis across multiple cancer types. Pabgraminone C overcomes resistance to PD-1 checkpoint blockade strategies. Pabgraminone C can be used in research related to liver cancer, melanoma, and colorectal cancer[1].

IC50 & Target[1]

PI3Kγ

61.7 nM (IC50)

PI3Kα

252.3 nM (IC50)

PI3Kβ

532.5 nM (IC50)

PI3Kδ

407.9 nM (IC50)

STAT3

 

STAT6

 

STAT1

 

STAT2

 

Fungal Metabolite

 

In Vitro

Pabgraminone C (0-1500 nM; 30 min) potently inhibits the activity of purified PI3Kγ enzyme, with an IC50 of 61.7 nM[1].
Pabgraminone C (10 μM; 24 h) reverses the immunosuppressive effect of monocyte-derived macrophages polarized by TCM, and promotes CD8+ T cell proliferation and cytokine production[1].
Pabgraminone C (10 μM; 6 h) alleviates oxidative stress in mouse TCM-polarized macrophages, reduces the levels of ROS and lipid peroxidation, and restores mitochondrial function and antioxidant levels[1].

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

Pabgraminone C Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human monocyte-derived macrophages and human CD8+ T cells
Concentration: 10 μM
Incubation Time: 24 h (macrophage pre-treatment)
Result: Restored human CD8+ T cell proliferation and increased secretion of IFNγ and IL-2.
In Vivo

Pabgraminone C (1.5 mg/kg; intravenous injection; initiated when the tumor volume reaches ~17 mm2, administered once every 2 days for a total of 4 doses) significantly inhibits subcutaneous tumor growth of various solid tumors[1].
Pabgraminone C (6 mg/kg; intravenous injection; administered twice on day 0 and day 3 after tumor inoculation) inhibits experimental melanoma lung metastasis by more than 50% in immunocompetent mice[1].
Pabgraminone C (1.5 mg/kg; intravenous injection) enhances the antitumor efficacy of Sorafenib (HY-10201) in orthotopic liver tumors, and exhibits superior inhibitory effects on tumor growth and metastasis compared with either single-agent treatment[1].
Pabgraminone C (1.5 mg/kg; intravenous injection; administered once every 2 days for a total of 4 doses starting when the tumor volume reaches ~17 mm2) does not inhibit the growth of subcutaneous MC38 tumors in immunodeficient Rag2-/- mice, which confirms that its antitumor activity is immune-mediated[1].

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

Animal Model: C57BL/6J WT (6-8 weeks old); Balb/C WT[1]
Dosage: 1.5 mg/kg
Administration: i.v.; 4 doses every 2 days starting when tumors reached ~17 mm2
Result: Significantly reduced mean tumor growth in Hepa1-6BL hepatocellular carcinoma, B16F10 melanoma, CT26 colorectal carcinoma, and MC38 colorectal carcinoma subcutaneous models compared to control.
Achieved comparable efficacy to first-line chemotherapy FOLFOX in MC38 tumor-bearing mice, reducing tumor weight significantly compared to control.
Animal Model: C57BL/6J WT (6-8 weeks old)[1]
Dosage: 6 mg/kg
Administration: i.v.; 2 doses on days 0 and 3 post-tumor inoculation
Result: Reduced B16F10 lung metastasis by >50% compared to control.
Molecular Weight

276.33

Formula

C16H20O4
CAS No.
SMILES

[H][C@@]12CC[C@@]([C@@]1([H])[C@@H](O)C3=C(C(C=CC3=O)=O)C2(C)C)(C)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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Pabgraminone C 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:

Pabgraminone C3061276-55-6IM502IM 502IM-502PI3KSTATPD-1/PD-L1Endogenous MetabolitePhosphoinositide 3-kinasePD-1/Programmed death-ligand 1PI3KγSTAT6STAT2natural killerPD-1 checkpoint blockademacrophagesCD8+ T cellSTAT3tumor-associated macrophagesSTAT1Inhibitorinhibitorinhibit

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