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Cat. No.: HY-15650A

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SGC0946 TFA

13 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

Formula: C₃₀H₄₁BrF₃N₇O₆
Molecular Weight:732.59

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

SGC0946 TFA Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Publications (13)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

DOT1L

0.3 nM (IC₅₀)

All Histone Methyltransferase Isoforms :

Chemical Information

Molecular Weight 732.59
Formula C₃₀H₄₁BrF₃N₇O₆
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (13)

All RT-PCRFlow CytometryCell Proliferation/Viability AssayIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

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.
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 HOXA9^P2A-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 HOXA9^P2A-mCherry cells treated with DMSO and various dosages of the DOT1L inhibitor SGC0946 (1, 5 μM).
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
Patent

US20180263995A1.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Publications (13)
Purity & Documentation
References

1/16
1/16

SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]

Customer Validation
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).
1/16

SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]

Customer Validation
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.
1/16

SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273. [Abstract]

Customer Validation
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.
1/16

SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Elife. 2020 Oct 1;9:e57858. [Abstract]

Customer Validation
Q-PCR analysis of the HOXA9^P2A-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.
1/16

SGC0946 TFA purchased from MedChemExpress. Usage Cited in: Elife. 2020 Oct 1;9:e57858. [Abstract]

Customer Validation
Flow cytometry analysis of the HOXA9^P2A-mCherry cells treated with DMSO and various dosages of the DOT1L inhibitor SGC0946 (1, 5 μM).

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SGC0946 TFA

Publications Citing Use of MedChemExpress (MCE) SGC0946 TFA

All Histone Methyltransferase Isoforms