Art. -Nr.: HY-15650

SGC0946

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

SGC0946 is a selective DOT1L inhibitor with an IC₅₀ value of 0.3 nM. By inhibiting DOT1L, SGC0946 can induce G1 phase arrest, suppress cell self-renewal and metastatic potential, and induce cell differentiation in cancer cells. SGC0946 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.

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Reinheit: 99.68%
CAS. Nr.: 1561178-17-3
Formel: C₂₈H₄₀BrN₇O₄
Molecular Weight:618.57

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SGC0946 Chemical Structure

CAS. Nr.: 1561178-17-3

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

DOT1L

0.3 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	2.65 nM Compound: SGC0946	Downregulation of H3K79 methylation in human A-431 cells incubated for 3 to 4 days by microscopy based analysis Downregulation of H3K79 methylation in human A-431 cells incubated for 3 to 4 days by microscopy based analysis	[PMID: 23250418]
MCF-10A	IC₅₀	8.8 nM Compound: 37	Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level	[PMID: 25406853]
MCF-10A	IC₅₀	8.8 nM Compound: SGC0946	Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis	[PMID: 23250418]
NCI-H460	IC₅₀	36.01 μM Compound: SGC0946	Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mutant (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mutant (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 39255403]
NCI-H460	IC₅₀	8.83 μM Compound: SGC0946	Antiproliferative activity against human NCI-H460 cells harboring wildtype DOT1L (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells harboring wildtype DOT1L (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 39255403]

In Vitro

SGC0946 (0-100 μM; 4 days) inhibits DOT1L with IC₅₀ of 2.65 nM in A431 cells^[1].
SGC0946 (1, 5 μM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene)^[1].
SGC0946 (1 μM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation^[1].
SGC0946 (1 μM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1^[1].
SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity^[2].
SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

A431 cells
Concentration:

0-100 µM
Incubation Time:

4 days
Result:

Showed potent inhibitory activity against DOT1L with IC₅₀ of 2.65 nM in A431 cells.

Cell Viability Assay^[1]

Cell Line:

Human cord blood cells (transformed with the MLL-AF9 fusion oncogene).
Concentration:

1, 5 µM
Incubation Time:

14 days
Result:

Killed human cord blood cells transformed with an MLL-AF9 fusion oncogene.

Western Blot Analysis^[1]

Cell Line:

Molm13 MLL cells
Concentration:

1 µM
Incubation Time:

3-7 days
Result:

Reduced H3K79me2 in Molm13 MLL cells in a time- and dose-dependent manner, and a complete inhibition exhibited at day 7.

Cell Proliferation Assay^[2]

Cell Line:

SK-OV-3 and TOV21G cells
Concentration:

0.2, 2, or 20 μM
Incubation Time:

12 days
Result:

Inhibited the growth of both SK-OV-3 and TOV21G cells in a dose- and time-dependent manner.
Reduced the colony of both SK-OV-3 and TOV21G cells.

Cell Cycle Analysis^[2]

Cell Line:

SK-OV-3 and TOV21G cells
Concentration:

10 μM
Incubation Time:

12 days
Result:

Induced increased G1 population and decreased S phase and G2/M phase cells in asynchronized SK-OV-3 and TOV21G cells.

In Vivo

SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model)^[2].
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection; twice a week for 6 weeks.
Result:

Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group).
Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.

Chemical Information

CAS. Nr. 1561178-17-3
Appearance Solid
Molecular Weight 618.57
Formel C₂₈H₄₀BrN₇O₄
Color White to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

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 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 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 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 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 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.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (80.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6166 mL

8.0832 mL

16.1663 mL

5 mM

0.3233 mL

1.6166 mL

3.2333 mL

10 mM

0.1617 mL

0.8083 mL

1.6166 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 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)

Verweise

[1]. Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. [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]. 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]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6166 mL	8.0832 mL	16.1663 mL	40.4158 mL
	5 mM	0.3233 mL	1.6166 mL	3.2333 mL	8.0832 mL
	10 mM	0.1617 mL	0.8083 mL	1.6166 mL	4.0416 mL
	15 mM	0.1078 mL	0.5389 mL	1.0778 mL	2.6944 mL
	20 mM	0.0808 mL	0.4042 mL	0.8083 mL	2.0208 mL
	25 mM	0.0647 mL	0.3233 mL	0.6467 mL	1.6166 mL
	30 mM	0.0539 mL	0.2694 mL	0.5389 mL	1.3472 mL
	40 mM	0.0404 mL	0.2021 mL	0.4042 mL	1.0104 mL
	50 mM	0.0323 mL	0.1617 mL	0.3233 mL	0.8083 mL
	60 mM	0.0269 mL	0.1347 mL	0.2694 mL	0.6736 mL
	80 mM	0.0202 mL	0.1010 mL	0.2021 mL	0.5052 mL

Keywords

SGC0946

13 Cited Publications

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SGC0946

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SGC0946

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SGC0946

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SGC0946

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SGC0946 Related Classifications

HY-15650 Related Classifications