TG100-115 |
Catalog No.GC15151
One-Click Copy Product Info
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TG100-115 es un inhibidor selectivo de PI3Kγ/PI3Kδ con IC50 de 83 y 235 nM, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 677297-51-7
Sample solution is provided at 25 µL, 10mM.
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TG100-115 is an orally active selective inhibitor of PI3Kγ (IC50=83nM) and PI3Kδ (IC50=235nM). TG100-115 blocks the VEGF signaling pathway and inhibits mTOR and p70S6 kinase phosphorylation. TG100-115 can be used in research related to myocardial ischemia/reperfusion injury, inflammatory diseases, and asthma[1-4].
In vitro, MDA-MB-231 cells were co-treated with TG100-115 (10μM) and recombinant TRAIL (1-10ng/ml) for 16 hours. TG100-115 did not significantly affect cell proliferation and had no effect on TRAIL-induced apoptosis[5]. MDA-MB-231 cells were treated with TG100-115 (1-50μM) for 27 hours and MDA-MB-468 cells for 48 hours. TG100-115 significantly inhibited cell migration and invasion[6].
In vivo, in a ConA-induced acute hepatitis model in BALB/C mice (6-8 weeks old), TG100-115 (10mg/kg or 50mg/kg; single injection) was administered intraperitoneally 0.5 hours after intravenous injection of ConA (15mg/kg). TG100-115 exacerbated liver injury, increased serum transaminase activity, liver necrosis, inflammatory cell infiltration, hepatocyte apoptosis, and mortality, and increased serum IL-2 levels[7]. In a neonatal hypoxic-ischemic brain injury model in P7 CD1 mice, TG100-115 (1-5mg/kg) was administered intraperitoneally 30 minutes before or 1-3 hours after hypoxic-ischemic brain injury (HIBI). TG100-115 significantly reduced brain infarct volume and improved brain morphology and functional recovery in mice[8].
References:
[1] Doukas J, Wrasidlo W, Noronha G, et al. Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71.
[2] Cives-Losada C, Macias RIR, Lozano E, et al. Pharmacological strategies to enhance the response of hepatoblastoma to chemotherapy through MDR1 inhibition. Acta Pharmacol Sin. 2026 Apr 23.
[3] Doukas J, Wrasidlo W, Noronha G, et al. Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction. Biochem Soc Trans. 2007 Apr;35(Pt 2):204-6.
[4] Nadolni W, Immler R, Hoelting K, et al. TRPM7 Kinase Is Essential for Neutrophil Recruitment and Function via Regulation of Akt/mTOR Signaling. Front Immunol. 2021 Feb 15;11:606893.
[5] Kaneda MM, Cappello P, Nguyen AV, et al. Macrophage PI3Kγ Drives Pancreatic Ductal Adenocarcinoma Progression. Cancer Discov. 2016 Aug;6(8):870-85.
[6] Song C, Choi S, Oh KB, et al. Suppression of TRPM7 enhances TRAIL-induced apoptosis in triple-negative breast cancer cells. J Cell Physiol. 2020 Dec;235(12):10037-10050.
[7] Song C, Bae Y, Jun J, et al. Identification of TG100-115 as a new and potent TRPM7 kinase inhibitor, which suppresses breast cancer cell migration and invasion. Biochim Biophys Acta Gen Subj. 2017 Apr;1861(4):947-957.
[8] Liu Y, Xiong L, Chang Y, et al. Phosphoinositide 3-kinase δ/γ inhibition does not prevent concanavalin A-induced hepatitis. Mol Med Rep. 2013 Nov;8(5):1305-10.
| Cell experiment [1]: | |
Cell lines | MDA-MB-231 cells (human breast cancer cell line) and MDA-MB-468 cells (human breast cancer cell line) |
Preparation Method | MDA-MB-231 or MDA-MB-468 cells were cultured in RPMI 1640 or DMEM media supplemented with 10% fetal bovine serum (FBS), penicillin (100U/mL) and streptomycin (100μg/mL) in a humidified 5% CO₂ incubator at 37°C. Cells were treated with TG100-115 at concentrations of 1, 10, and 50μM for 27 hours (MDA-MB-231) or 48 hours (MDA-MB-468). |
Reaction Conditions | 1-50μM; 27h (MDA-MB-231) or 48h (MDA-MB-468) |
Applications | TG100-115 significantly decreases cell migration and invasion of MDA-MB-231 and MDA-MB-468 cells. TG100-115 inhibits TRPM7 kinase regulated phosphorylation of the myosin IIA heavy chain and phosphorylation of focal adhesion kinase (FAK). TG100-115 also suppresses TRPM7 ion channel activity. |
| Animal experiment [2]: | |
Animal models | P7 CD1 mice (neonatal hypoxic-ischemic brain injury model) |
Preparation Method | P7 CD1 mouse pups were subjected to right common carotid artery occlusion followed by 60 minutes of hypoxia (7.5% O₂). TG100-115 (1.0, 2.5, 5.0mg/kg) was administered intraperitoneally (i.p.) at a volume of 50μL/5g body weight. Treatment paradigms included pre-treatment (30 minutes before hypoxia-ischemia) and post-treatment (1, 2, or 3 hours after hypoxia-ischemia). |
Dosage form | 1.0, 2.5, 5.0mg/kg; i.p.; single injection |
Applications | TG100-115 significantly reduced brain infarct volume when administered before or up to 3 hours after hypoxia-ischemia. TG100-115 preserved whole brain morphology, reduced ipsilateral liquefaction volume, and increased brain weight. TG100-115 improved short-term functional recovery, as evidenced by enhanced performance in cliff avoidance reflex, geotaxis reflex, righting reflex, and grip strength tests. TG100-115 treatment normalized TRPM7 protein levels, modulated the caspase-3-associated apoptotic pathway, and attenuated NLRP3 inflammasome activation (reduced expression of NLRP3, ASC, and IL-18). |
References: | |
| Cas No. | 677297-51-7 | SDF | |
| Chemical Name | 3-[2,4-diamino-7-(3-hydroxyphenyl)pteridin-6-yl]phenol | ||
| Canonical SMILES | C1=CC(=CC(=C1)O)C2=NC3=C(N=C2C4=CC(=CC=C4)O)N=C(N=C3N)N | ||
| Formula | C18H14N6O2 | M.Wt | 346.34 |
| Solubility | ≥ 3.46mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8873 mL | 14.4367 mL | 28.8734 mL |
| 5 mM | 577.5 μL | 2.8873 mL | 5.7747 mL |
| 10 mM | 288.7 μL | 1.4437 mL | 2.8873 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)