GLPBio

TG100-115

Catalog No.: GC15151Purity:>98.00%
COASDSData Sheet
TG100-115 es un inhibidor selectivo de PI3Kγ/PI3Kδ con IC50 de 83 y 235 nM, respectivamente.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.

TG100-115
Cas No.: 677297-51-7
10mM (in 1mL DMSO)In Stock
$66.00
1
1mgIn Stock
$25.00
1
5mgIn Stock
$61.00
1
10mgIn Stock
$89.00
1
25mgIn Stock
$178.00
1
50mgIn Stock
$311.00
1
100mgIn Stock
$444.00
1
200mgIn Stock
$615.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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    641, 529–536 (2025)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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Descripción (Description)

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.

Protocolo (Protocol)

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:
[1] 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.
[2] 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.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
677297-51-7
Nombre químico
3-[2,4-diamino-7-(3-hydroxyphenyl)pteridin-6-yl]phenol
SMILES
C1=CC(=CC(=C1)O)C2=NC3=C(N=C2C4=CC(=CC=C4)O)N=C(N=C3N)N
Fórmula molecular
C18H14N6O2
Peso molecular
346.34
Solubilidad
≥ 3.46mg/mL in DMSO
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

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