SGC0946 TFA
Based on 13 publication(s) in Google Scholar
SGC0946 TFA is a selective DOT1L inhibitor with an IC50 value of 0.3 nM. By inhibiting DOT1L, SGC0946 TFA can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 TFA can be used in the research of tumors such as leukemia and breast cancer, and also serves as a probe to further investigate the cellular mechanisms of DOT1L in normal and diseased cells.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C30H41BrF3N7O6
- 分子量:732.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 SGC0946 TFA
More- Cancer Res. 2026 Jul 15;86(14):3588-3603. [Abstract]
- Mol Cell. 2021 Oct 7;81(19):4076-4090.e8. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Leukemia. 2026 Mar 25. [Abstract]
- Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]
- Oncogenesis. 2021 Jul 12;10(7):48. [Abstract]
- Elife. 2020 Oct 1;9:e57858. [Abstract]
- Biochem Pharmacol. 2025 Dec;242(Pt 3):117402. [Abstract]
- Mol Carcinog. 2023 Aug;62(8):1119-1135. [Abstract]
- Genes (Basel). 2024 Sep 13;15(9):1206. [Abstract]
- Technol Cancer Res Treat. 2023 Jan-Dec:22:15330338231167249. [Abstract]
- Oncol Lett. 2024 Jul 19;28(3):444. [Abstract]
- Patent. US20180263995A1.
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Cell Imaging/Staining
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RT-PCR
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Flow Cytometry
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
More
生物活性
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DOT1L 0.3 nM (IC50) |
化学情報
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分子量 732.59
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分子式 C30H41BrF3N7O6
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SMILES
CC(C)(C1=CC=C(C=C1)NC(NCCCN(C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C4=C(C(Br)=C3)C(N)=NC=N4)O2)C(C)C)=O)C.O=C(C(F)(F)F)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 (13)
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Journal Impact Factor
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Most Recent
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Cancer Res
Targeting DOT1L Reactivates HERV-K to Drive Cell-Autonomous and Paracrine Senescence in Adenocarcinoma of the Esophagogastric Junction. [Abstract]2026 Jul 15;86(14):3588-3603. PMID: 42084229 -
Mol Cell
A proteomic and phosphoproteomic landscape of KRAS mutant cancers identifies combination therapies. [Abstract]2021 Oct 7;81(19):4076-4090.e8. PMID: 34375582 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Leukemia
A Perturb-seq map of a differentiation hub reveals synergistic vulnerabilities in KMT2A-rearranged acute myeloid leukemia. [Abstract]2026 Mar 25. PMID: 41882099 -
Sci Adv
Gain-of-function mutations in the catalytic domain of DOT1L promote lung cancer malignant phenotypes via the MAPK/ERK signaling pathway. [Abstract]2023 Jun 2;9(22):eadc9273. PMID: 37256945
SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]
CCK-8 assay data showing the sensitivity of NCI-H460-DOT1L-WT/R231Q cells to SGC0946 (0.01,.0.1, 1, 10, 100 μM, 6 days).
SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]
CDX-bearing mice were treated with vehicle Cisplatin (3 mg/kg, twice per week), Vinorelbine (4 mg/kg, twice per week), or SGC0946 (20 mg/kg, five times per week) through intraperitoneal administration. The graphs show the tumor images and weights, with the tumor inhibition rate.
SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]
Crystal violet staining of NCI-H460-DOT1L-WT/R231Q cells treated with SGC0946 (2.5 or 7.5 μM), binimetinib (2.5 or 7.5 μM), or the combination at the same concentrations for 7 to 14 days (top). Comparison of relative colony formation between groups at 7.5 μM drug concentration.
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Oncogenesis
Disruptor of telomeric silencing 1-like promotes ovarian cancer tumor growth by stimulating pro-tumorigenic metabolic pathways and blocking apoptosis. [Abstract]2021 Jul 12;10(7):48. PMID: 34253709 -
Elife
Functional interrogation of HOXA9 regulome in MLLr leukemia via reporter-based CRISPR/Cas9 screen. [Abstract]2020 Oct 1;9:e57858. PMID: 33001025
SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Elife. 2020 Oct 1;9:e57858. [Abstract]
Q-PCR analysis of the HOXA9P2A-mCherry cells with or without the 6-day treatment of the DOT1L inhibitor SGC0946 by using specific primers targeting the mRNA sequences of mCherry and HOXA9. The correlation of transcription reduction in mCherry and HOXA9 in response to inhibitor–mediated transcription repression was calculated by performing Pearson’s correlation test.
SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Elife. 2020 Oct 1;9:e57858. [Abstract]
Flow cytometry analysis of the HOXA9P2A-mCherry cells treated with DMSO and various dosages of the DOT1L inhibitor SGC0946 (1, 5 μM).
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Biochem Pharmacol
Targeting DOT1L-mediated histone methylation by hesperetin alleviates retinal microvascular endothelial cell dysfunction and diabetic retinopathy. [Abstract]2025 Dec;242(Pt 3):117402. PMID: 41047037 -
Mol Carcinog
PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]2023 Aug;62(8):1119-1135. PMID: 37144835 -
Genes (Basel)
CHIR99021 and Brdu Are Critical in Chicken iPSC Reprogramming via Small-Molecule Screening. [Abstract]2024 Sep 13;15(9):1206. PMID: 39336797 -
Technol Cancer Res Treat
DOT1L Epigenetically Regulates Autophagy and Mitochondria Fusion in Cell Lines of Renal Cancer. [Abstract]2023 Jan-Dec:22:15330338231167249. PMID: 37365941 -
Oncol Lett
Pan‑cancer analysis on the role of KMT2C expression in tumor progression and immunotherapy. [Abstract]2024 Jul 19;28(3):444. PMID: 39091583 -
純度とドキュメンテーション
参考文献
[1]. Zhang L, et al. Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer. Oncotarget. 2014 Nov 15;5(21):10665-77. [Content Brief]
[2]. Zhang X, et al. Prognostic and therapeutic value of disruptor of telomeric silencing-1-like (DOT1L) expression in patients with ovarian cancer. J Hematol Oncol. 2017 Jan 23;10(1):29. [Content Brief]
[3]. Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. [Content Brief]
Calculators
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