1. PROTAC Epigenetics Apoptosis
  2. PROTACs Epigenetic Reader Domain Apoptosis
  3. MS41

MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078).

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MS41 Chemical Structure

MS41 Chemical Structure

CAS No. : 2768610-97-3

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Description

MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078)[1].

Molecular Weight

1031.27

Formula

C56H70N8O9S

CAS No.
Appearance

Solid

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

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Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9697 mL 4.8484 mL 9.6968 mL
5 mM 0.1939 mL 0.9697 mL 1.9394 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MS41
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HY-169093
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