Cat. No.: HY-169093

MS41

고객리뷰

Based on 1 Customer Validation

MS41 is a ENL PROTAC degrader with a DC₅₀ of 3.50 nM. MS41 recruits the VHL E3 ubiquitin ligase, triggers ENL degradation via the ubiquitin-proteasome system, and simultaneously induces AF9 degradation. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation complexes, suppresses oncogene expression, and activates differentiation gene expression. MS41 inhibits leukemia cell growth and induces cell cycle arrest and apoptosis. MS41 inhibits leukemia progression in xenograft mouse models. MS41 can be used for research on mixed lineage leukemia-rearranged leukemia and nephroblastoma.
(Pink: ENL ligand (HY-169094); Blue: VHL ligand (HY-112078); Black: linker (HY-W105744)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.97%
CAS No.: 2768610-97-3
화학식: C₅₆H₇₀N₈O₉S
분자량:1031.27

보관:

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

MS41 Chemical Structure

CAS No.: 2768610-97-3

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

MS41 is a ENL PROTAC degrader with a DC₅₀ of 3.50 nM. MS41 recruits the VHL E3 ubiquitin ligase, triggers ENL degradation via the ubiquitin-proteasome system, and simultaneously induces AF9 degradation. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation complexes, suppresses oncogene expression, and activates differentiation gene expression. MS41 inhibits leukemia cell growth and induces cell cycle arrest and apoptosis. MS41 inhibits leukemia progression in xenograft mouse models. MS41 can be used for research on mixed lineage leukemia-rearranged leukemia and nephroblastoma^[1]. (Pink: ENL ligand (HY-169094); Blue: VHL ligand (HY-112078); Black: linker (HY-W105744)).

IC₅₀ & Target

VHL	ENL 2.84 nM (DC₅₀)

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

In Vitro

MS41 (0.1 nM-54 μM; 1 hour) potently inhibits the ENL YEATS domain-H3K9ac interaction with an IC₅₀ of 119.43 nM, binds comparably to AF9 YEATS domain, and does not bind GAS41 or YEATS2 YEATS domains^[1].
MS41 (0.25-256 nM; 24 hours) 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 and >99% maximal degradation^[1].
MS41 (0.25-256 nM; 24 hours) potently and rapidly degrades ENL in SEMK2, Jurkat, and KASUMI1 human leukemia cells, with DC₅₀ values ranging from 2.84 to 26.58 nM and >93% maximal degradation^[1].
MS41 is a highly selective ENL degrader in MV4;11 cells, with no detectable off-target protein degradation at the proteome-wide level^[1].
MS41 (6 days, 12 days for Jurkat and K-562) potently inhibits proliferation of ENL-dependent human leukemia cell lines (MV4;11, RS4;11, SEMK2, KASUMI1) with GI₅₀ values ranging from 21.28 to 406.46 nM, while having no effect on non-ENL-dependent Jurkat and K-562 cells^[1].
MS41 (100 nM; 7-10 days) impairs the clonogenic potential of ENL-dependent human leukemia cell lines MV4;11, SEMK2, and KASUMI1, but not non-ENL-dependent Jurkat cells^[1].
MS41 (10-300 nM; 24 h) suppresses ENL-dependent oncogenic gene expression programs in MV4;11 cells, down-regulating key leukemia-associated genes and up-regulating myeloid differentiation markers, with effects matching those of ENL knockout^[1].
MS41 (100 nM; 6, 24 hours) reduces chromatin occupancy of ENL and its associated transcription elongation machinery (SEC, DOT1L, elongating Pol II) on target genes, leading to suppressed gene expression in MV4;11 cells^[1].
MS41 (1-1000 nM; 24, 72 hours) potently degrades wild-type and YEATS domain mutant ENL proteins and suppresses the aberrant HOXA gene expression induced by mutant ENL in HEK293 cells^[1].
MS41 (100 nM; 24-72 hours) induces time-dependent G₁ cell cycle arrest and apoptosis in MV4;11 human leukemia cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

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

0.25, 0.5, 1, 2, 4, 8, 16, 32, 64, 128, 256 nM (24-hour treatment)
100 nM (washout and mechanism validation)
0, 0.2, 1, 5 μM PFI-6 (HY-155412), VH298 (HY-100947), MG132 (HY-13259) (pretreatment)
0, 0.1, 0.3, 1 μM MLN4924 (HY-70062) (pretreatment)
Incubation Time:

24 hours (concentration-dependent degradation)
0.5, 1, 2, 6, 12, 24, 48, 72 hours (washout)
2 hours (MS41 treatment with 1-hour pretreatment)
Result:

Induced concentration-dependent ENL degradation with a DC₅₀ of 3.50 nM and D_max of 99.8%.
Induced rapid ENL degradation detected as early as 30 minutes, maximal at 6 hours with 100 nM MS41.
Restored ENL levels by 6 hours and fully restored by 12 hours after washout.
Blocked MS41-mediated ENL degradation in a concentration-dependent manner with pretreatment of PFI-6, VH298, MG132, or MLN4924.
Completely abolished MS41-induced ENL degradation with CRISPR-Cas9-mediated VHL ablation.

Western Blot Analysis^[1]

Cell Line:

human leukemia cell lines SEMK2, Jurkat, KASUMI1
Concentration:

0.25, 0.5, 1, 2, 4, 8, 16, 32, 64, 128, 256 nM (24-hour treatment)
100 nM (time-course)
Incubation Time:

24 hours (concentration-dependent degradation)
0.5, 1, 2, 6, 12, 24, 48, 72 hours (time-course)
Result:

Induced concentration-dependent ENL degradation with DC₅₀ values of 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), with D_max > 93% across all cell lines.
Induced rapid ENL degradation detected as early as 30 minutes, maximal at 6 hours with 100 nM MS41.

Cell Cycle Analysis^[1]

Cell Line:

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

100 nM
Incubation Time:

24, 48, 72 h
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.

Apoptosis Analysis^[1]

Cell Line:

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

100 nM
Incubation Time:

24, 48, 72 h
Result:

Induced time-dependent apoptosis in MV4;11 human leukemia cells.

Real Time qPCR^[1]

Cell Line:

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

10, 30, 100, 300 nM
Incubation Time:

24 h
Result:

Suppressed ENL-dependent oncogenic gene expression programs in MV4;11 cells, down-regulating key leukemia-associated genes and up-regulating myeloid differentiation markers.

Western Blot Analysis^[1]

Cell Line:

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

100 nM
Incubation Time:

6, 24 hours
Result:

Reduced chromatin occupancy of ENL and its associated transcription elongation machinery (SEC, DOT1L, elongating Pol II) on target genes, leading to suppressed gene expression in MV4;11 cells.

Real Time qPCR^[1]

Cell Line:

HEK293 cells
Concentration:

100 nM
Incubation Time:

72 h
Result:

Suppressed the aberrant HOXA gene expression induced by mutant ENL in HEK293 cells.

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 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.
Drastically reduced bioluminescent signals (leukemia burden).
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 No. 2768610-97-3
Appearance Solid
분자량 1031.27
화학식 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
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 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)

References

[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

상품명:
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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

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

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

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

MS41 Related Classifications

HY-169093 Related Classifications