Art. -Nr.: HY-169093

MS41

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MS41 is a selective ENL PROTAC degrader with DC₅₀ values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat) and 26.58 nM (KASUMI1), respectively. MS41 recruits the VHL E3 ubiquitin ligase, induces ubiquitination and degradation of ENL (including mutant ENL carrying mutations in the YEATS domain), and reduces the chromatin occupancy of ENL-associated transcription elongation complexes. MS41 induces G1 phase cell cycle arrest and Apoptosis. MS41 inhibits leukemia progression in xenograft models. MS41 can be used in research related to mixed lineage leukemia-rearranged leukemia and Wilms tumor.
(Pink: ENL ligand (HY-169094); Blue: VHL ligand (HY-112078); Black: linker (HY-W105744)).

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Reinheit: 98.97%
CAS. Nr.: 2768610-97-3
Formel: C₅₆H₇₀N₈O₉S
Molecular Weight:1031.27

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS41 Chemical Structure

CAS. Nr.: 2768610-97-3

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MS41 is a selective ENL PROTAC degrader with DC₅₀ values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat) and 26.58 nM (KASUMI1), respectively. MS41 recruits the VHL E3 ubiquitin ligase, induces ubiquitination and degradation of ENL (including mutant ENL carrying mutations in the YEATS domain), and reduces the chromatin occupancy of ENL-associated transcription elongation complexes. MS41 induces G1 phase cell cycle arrest and Apoptosis. MS41 inhibits leukemia progression in xenograft models. MS41 can be used in research related to mixed lineage leukemia-rearranged leukemia and Wilms tumor^[1]. (Pink: ENL ligand (HY-169094); Blue: VHL ligand (HY-112078); Black: linker (HY-W105744)).

IC₅₀ & Target^[1]

VHL	ENL 2.84 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

In Vitro

MS41 (0.1 nM-54 μM; 1 h) potently inhibits the interaction between the ENL YEATS domain and H3K9ac, with an IC₅₀ of 119.43 nM; it binds to the AF9 YEATS domain with comparable affinity, and does not bind to the YEATS domains of GAS41 or YEATS2^[1].
MS41 (0.25-256 nM; 24 h) potently, rapidly and reversibly degrades ENL in MV4;11 cells via a VHL- and ubiquitin-proteasome system-dependent mechanism, with a DC₅₀ of 3.50 nM^[1].
MS41 (days 6-12) potently inhibits the proliferation of ENL-dependent leukemia cell lines (MV4;11, RS4;11, SEMK2, KASUMI1), with GI₅₀ values ranging from 21.28 to 406.46 nM, but exerts no effect on ENL-independent Jurkat and K-562 cells^[1].
MS41 (100 nM; 24-72 h) induces time-dependent G₁ phase cell cycle arrest and apoptosis in leukemia cell line MV4;11^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4;11
Concentration:

0.25, 0.5, 1, 2, 4, 8, 16, 32, 64, 128, 256 nM
Incubation Time:

24 h
Result:

Induced concentration-dependent ENL degradation with a DC₅₀ of 3.50 nM and D_MAX of 99.8%.

Cell Proliferation Assay^[1]

Cell Line:

human leukemia cell lines MV4;11, RS4;11, SEMK2, KASUMI1, Jurkat, K-562
Concentration:

range of concentrations
Incubation Time:

6-12 days
Result:

Exhibited potent concentration-dependent growth inhibition in ENL-dependent cell lines: MV4;11 (GI₅₀ = 21.28 nM), RS4;11 (GI₅₀ = 25.06 nM), SEMK2 (GI₅₀ = 406.46 nM), KASUMI1 (GI₅₀ = 69.05 nM).
Had no significant growth inhibitory effect on non-ENL-dependent cell lines Jurkat and K-562 (GI₅₀ > 50 μM).

Cell Cycle Analysis^[1]

Cell Line:

human MLL-r leukemia cell line MV4;11
Concentration:

100 nM
Incubation Time:

24, 48, 72 hours
Result:

Induced G₁ cell cycle arrest in a time-dependent manner, with significant increases in G₁-phase cells at 48 and 72 hours.
Increased late apoptosis, with significant increases at 48 and 72 hours.
Showed no such effects with MS41N and PFI-6.

Parmacokinetics

Species	Dose	Route	C_max	Plasma Concentration
Mice^[1]	50 mg/kg	i.p.	241.8 nM	>30 nM

In Vivo

MS41 (50 mg/kg; i.p.; once daily; starting 10 days post-transplant until study endpoint) significantly delays MLL-r leukemia progression and prolongs median survival by 12.5 days in NSG xenograft mice^[1].
MS41 (50 mg/kg; i.p.; once daily; 30 consecutive days) exhibits no detectable in vivo toxicity in healthy C57BL/6J mice, with only mild, reversible effects on normal hematopoiesis^[1].

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

Animal Model:

NOD.Cg-Prkdc^scid Il2rg^tm.Wjl/SzJ (NSG) (6 to 8 weeks old, sublethally irradiated, transplanted with luciferase/turboGFP-expressing MV4;11 cells via tail vein injection)^[1]
Dosage:

50 mg/kg
Administration:

i.p.; once daily; starting 10 days post-transplant until study endpoint
Result:

Prolonged median survival to 49.5 days compared to 37 days for vehicle controls.
Reduced percentages of human CD45+ leukemia cells in peripheral blood at days 14, 28, and 35 post-treatment initiation.
Drastically reduced bioluminescent signals (leukemia burden) at days 14 and 21 post-treatment.
Showed minimal leukemia cell infiltration in bone marrow, liver, and spleen compared to extensive infiltration in vehicle controls.
Reduced proliferation of leukemia cells confirmed by Ki-67 staining.
Induced complete ENL degradation in bone marrow leukemia cells.

Chemical Information

CAS. Nr. 2768610-97-3
Appearance Solid
Molecular Weight 1031.27
Formel C₅₆H₇₀N₈O₉S
Color White to off-white
SMILES

CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCCCCNC(C4=CC=C5CC[C@H](C5=C4)NC(C6=NOC(C7=CC(O)=C(C=C7)C(N(C)C)=O)=C6)=O)=O)=O)=O)O)=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	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (96.97 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

0.9697 mL

4.8484 mL

9.6968 mL

5 mM

0.1939 mL

0.9697 mL

1.9394 mL

10 mM

0.0970 mL

0.4848 mL

0.9697 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Xue Z, et al. A potent and selective ENL degrader suppresses oncogenic gene expression and leukemia progression. Science advances. 2024 Aug 30;10(35):eado1432. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.9697 mL	4.8484 mL	9.6968 mL	24.2420 mL
	5 mM	0.1939 mL	0.9697 mL	1.9394 mL	4.8484 mL
	10 mM	0.0970 mL	0.4848 mL	0.9697 mL	2.4242 mL
	15 mM	0.0646 mL	0.3232 mL	0.6465 mL	1.6161 mL
	20 mM	0.0485 mL	0.2424 mL	0.4848 mL	1.2121 mL
	25 mM	0.0388 mL	0.1939 mL	0.3879 mL	0.9697 mL
	30 mM	0.0323 mL	0.1616 mL	0.3232 mL	0.8081 mL
	40 mM	0.0242 mL	0.1212 mL	0.2424 mL	0.6060 mL
	50 mM	0.0194 mL	0.0970 mL	0.1939 mL	0.4848 mL
	60 mM	0.0162 mL	0.0808 mL	0.1616 mL	0.4040 mL
	80 mM	0.0121 mL	0.0606 mL	0.1212 mL	0.3030 mL

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MS41

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS41

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS41 Related Classifications

HY-169093 Related Classifications