Gamitrinib TPP
Based on 16 publication(s) in Google Scholar
Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
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- CAS 番号: 1131626-46-4
- 分子式: C52H65N3O8P
- 分子量:891.06
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Gamitrinib TPP
More- Nature. 2020 Mar;579(7799):433-437. [Abstract]
- Nat Neurosci. 2026 Jun 26. [Abstract]
- Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
- Cancer Lett. 2025 Nov 1:632:217977. [Abstract]
- Cancer Lett. 2022 Nov 28:549:215915. [Abstract]
- Clin Cancer Res. 2022 May 13;28(10):2180-2195. [Abstract]
- Aging Cell. 2026 Jun;25(6):e70573. [Abstract]
- J Invest Dermatol. 2025 Feb 18:S0022-202X(25)00110-1. [Abstract]
- Am J Physiol Cell Physiol. 2026 Jun 1;330(6):C1721-C1736. [Abstract]
- Front Biosci (Landmark Ed). 2023 Sep 26;28(9):227. [Abstract]
- Exp Ther Med. 2021 Nov;22(5):1246. [Abstract]
- bioRxiv. 2024 September 03.
- bioRxiv. 2024 Jan 2.
- SSRN. 2023 Jul 11.
- Elife. 2021 Jun 16:10:e63104. [Abstract]
- Research Square Preprint. 2020 Sep.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Imaging/Staining
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IF
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WB
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Cell Proliferation/Viability Assay
生物活性
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HSP90 |
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Cell Line
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Type | Value | Description | References |
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| Panel NCI-60 (60 carcinoma cell lines) | IC50 |
0.2 μM
Compound: 20
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Antiproliferative activity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell growth inhibition
Antiproliferative activity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell growth inhibition
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[PMID: 36507721] |
Within a 16-hour exposure, concentrations of Gamitrinib TPP of 15-20 μM indistinguishably kill patient-derived and cultured glioblastoma cell lines. This cell death response has the hallmarks of mitochondrial apoptosis, with loss of organelle inner membrane potential, release of cytochrome c in the cytosol, activation of initiator caspase-9 and effector caspase-3 and -7, and cellular reactivity for annexin V. Because Hsp90s are selectively present in mitochondria of tumor cells, but not normal tissues, Gamitrinib TPP does not kill normal fetal human astrocytes (FHAS). Under comparable conditions, nonsubcellularly targeted 17-AAG has no effect on normal or tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1131626-46-4
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分子量 891.06
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分子式 C52H65N3O8P
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SMILES
O=C(C=C1NC(/C(C)=C/C=C/[C@H](OC)[C@@H](OC(N)=O)/C(C)=C/[C@H](C)[C@H]2O)=O)C(NCCCCCC[P+](C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5)=C(C[C@H](C[C@@H]2OC)C)C1=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (16)
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Journal Impact Factor
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Most Recent
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Nature
2020 Mar;579(7799):433-437. PMID: 32132706
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Nature. 2020 Mar;579(7799):433-437. [Abstract]
HeLa cells, 293T cells, BJEH fibroblasts and N/TERT-1 keratinocytes were exposed to sgRNAs directed against the specified genes and pharmacologically stimulated for 9-12 h before immunoblotting (one representative experiment shown of n = 2 (HeLa and 293T) or n = 3 (BJEH and N/TERT-1) independent experiments). sgCTR, non-targeting control sgRNA. GTPP, Gamitrinib TPP hexafluorophosphate, HY-102007A, 10 μM.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Nature. 2020 Mar;579(7799):433-437. [Abstract]
Clonal HAP1 knockout and stably reconstituted cells were treated as indicated (CCCP, 20 μM, 9 h; Tunicamycin, HY-A0098, 10 μM, 9 h; Oligomycin (OM), 9 h; CDDO, Bardoxolone, HY-14909, 2.5 μM, 11 h; GTPP, HY-102007A, 10 μM, 11 h) and analysed by immunoblotting.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Nature. 2020 Mar;579(7799):433-437. [Abstract]
HAP1 CHOPNeon cells of the indicated genotypes were treated for 9 h (CCCP, 20 μM; Tunicamycin, HY-A0098, 10 μM; CDDO, Bardoxolone, HY-14909, 2.5 μM) or 12 h (GTPP, HY-102007A, 10 μM) and analysed by flow cytometry. Per genotype and treatment, the CHOPNeonsignal was normalized to its DMSO control and statistical significance is indicated compared to identically treated wild-type cells (mean ± s.d. of n = 3 independent experiments; one-way ANOVA with Dunnett’s multiple comparisons correction).
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Nat Neurosci
The mitochondrial unfolded protein response in human microglia disrupts neuronal-glial communication and promotes senescence. [Abstract]2026 Jun 26. PMID: 42362883 -
Sci Adv
In situ characterization of mitochondrial Hsp60-Hsp10 chaperone complex under folding stress. [Abstract]2025 Oct 24;11(43):eadw6064. PMID: 41124257
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Representative immunofluorescence images showing Parkin-eGFP (green) and the mitochondrial marker COXIV (red) in HeLa cells. Cells were treated with dimethyl sulfoxide (DMSO) for 4 hours (h) (top) or GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) for 4 hours (bottom). Colocalization between Parkin-eGFP and COXIV was assessed using fluorescence intensity profiles. Scale bars, 20 μm.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Representative tomographic slices (top) and corresponding segmentation images (bottom) of untreated, truncated OTC–expressing, and GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM; for 4 hours)-treated cells. Blue arrowheads indicate electron-dense calcium phosphate granules (untreated), and green arrowheads indicate amorphous aggregates (OTC-expressing and GTPP condition). Scale bars, 50 nm.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Mitochondrial morphology changes upon stressor treatment. Representative immunofluorescence images of HeLa cells stained for COXIV following treatment with vehicle (CTRL; DMSO), CCCP (4 hours), or GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM; 4 hours). Zoomed-in views highlight mitochondrial network organization under each condition.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Silver staining analysis of soluble and insoluble protein fractions from siControl and siHsp60/10-treated cells, with or without GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) treatment. MW, molecular weight.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Quantification of cellular stress markers following GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM)-induced folding stress under control and knockdown conditions: Cell viability , mitochondrial membrane potential (MitoTracker fluorescence), and mtROS levels. Data are shown as means ± SD. Statistical significance was assessed using unpaired t tests or one-way ANOVA with Tukey’s post hoc test. *P < 0.05; **P < 0.01; ***P < 0.001; ****P < 0.0001.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Representative immunofluorescence images of HeLa cells under increasing folding stress, comparing siControl (left) and siHsp60/10 knockdown (right) conditions. Cells were treated with DMSO or GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) for 4 or 8 hours and stained for Parkin-eGFP (green), MitoTracker Red (red), and COXIV (blue). Merged images highlight the mitochondrial network and Parkin puncta localization. Scale bars, 20 μm.
Gamitrinib TPP purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Western blot analysis of mitochondrial proteins (TOM20, NDUFS3, Tim23, COXIV, mtHsp60, and mtHsp10) following GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) treatment for the indicated times. Tubulin was used as a loading control.
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Cancer Lett
Restricting metabolic plasticity enhances stress adaptation through the modulation of PDH and HIF1A in TRAP1-depleted colon cancer. [Abstract]2025 Nov 1:632:217977. PMID: 40789509 -
Cancer Lett
Metabolic targeting of NRF2 potentiates the efficacy of the TRAP1 inhibitor G-TPP through reduction of ROS detoxification in colorectal cancer. [Abstract]2022 Nov 28:549:215915. PMID: 36113636 -
Clin Cancer Res
2022 May 13;28(10):2180-2195. PMID: 35247901 -
Aging Cell
Oxidative Stress and Diminished Mitochondrial Proteostatic Reserve Are Linked to Enhanced mtUPR Initiation in Aged Mouse Muscle. [Abstract]2026 Jun;25(6):e70573. PMID: 42243621 -
J Invest Dermatol
The Differential Roles of HSP90 Isoforms in Skin Inflammation: Anti-Inflammatory Potential of TRAP1 Inhibition. [Abstract]2025 Feb 18:S0022-202X(25)00110-1. PMID: 39978584 -
Am J Physiol Cell Physiol
Divergent mitochondrial stressors elicit specific retrograde signaling pathways in muscle myotubes. [Abstract]2026 Jun 1;330(6):C1721-C1736. PMID: 42126081 -
Front Biosci (Landmark Ed)
Inhibition of TRAP1 Accelerates the DNA Damage Response, Activation of the Heat Shock Response and Metabolic Reprogramming in Colon Cancer Cells. [Abstract]2023 Sep 26;28(9):227. PMID: 37796715 -
Exp Ther Med
2021 Nov;22(5):1246. PMID: 34539842 -
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Elife
2021 Jun 16:10:e63104. PMID: 34132194 -
プロトコル
Human glioblastoma cell lines LN229 (p53 mutant; PTEN, WT), U87 (p53 WT; PTEN mutant), U251 (p53 mutant), prostate adenocarcinoma PC3, breast adenocarcinoma MCF-7, and human epithelial kidney (HEK) 293T are used. The various cell types are seeded in triplicate onto 96-well plates at 2×103 cells/well, treated with vehicle, Gamitrinib TPP (G-TPP), or nontargeted 17-AAG ( 0-20 μM) for up to 24 h, and quantified for metabolic activity by a MTT colorimetric assay with absorbance at 405 nm. For determination of apoptosis, control or treated tumor cell types (1×106) are labeled for annexin V and propidium iodide (PI) and analyzed by multiparametric flow cytometry. For G-TPP-TRAIL combination studies, tumor cell types are simultaneously incubated with suboptimal concentrations of G-TPP at 5 μM and TRAIL depending on the cell type at 100 ng/mL (U87), 20 ng/mL (U251), 40 ng/mL (PC3, MCF-7, FHAS), or 200 ng/mL (LN229), and analyzed after 16 h for cell viability by MTT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
U87 glioblastoma cells stably transfected with a luciferase expression plasmid (U87-Luc) are suspended in sterile PBS, pH 7.2, and stereotactically implanted (1×105) in the right cerebral striatum of immunocompromised nude mice. Animals with established tumors are randomized in 4 groups (4 animals/group) and started on sterile vehicle (cremophor), TRAIL alone, Gamitrinib TPP alone, or the combination of TRAIL plus Gamitrinib TPP. In all animal groups, TRAIL is injected stereotactically in the right cerebral striatum (2 ng on days 7 and 10 after implantation), and Gamitrinib TPP is given systemically (10 mg/kg as daily i.p. injections on days 6, 7, 9, and 10 after implantation). Treatment is suspended on day 10 after tumor implantation, and tumor growth is assessed weekly by bioluminescence imaging after i.p injection of 110 mg/kg D-luciferin. In some experiments, nude mice carrying established U87-Luc intracranial glioblastomas are treated with systemic Gamitrinib TPP monotherapy at 20 mg/kg as daily i.p. injections and monitored for tumor growth by bioluminescence imaging. Animal survival is calculated per group[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Gamitrinib TPP 関連分類
HY-102007 関連分類
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