2. Epigenetics PROTAC
  3. Histone Methyltransferase PROTACs
  4. MS67

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.

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MS67 Chemical Structure

MS67 Chemical Structure

CAS No. : 2407452-77-9

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Based on 1 publication(s) in Google Scholar

MS67 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects[1].

IC50 & Target[1]

VHL

 

WDR5

63 nM (Kd)

In Vitro

MS67 (0.001-1 μM) induces WDR5 degradation at a concentration as low as 1 nM. MS67 induces WDR5 depletion much more effectively in all six mixed lineage leukemia (MLL)-r acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines without a hook effect and in a concentration-dependent manner in PDAC cells[1].
MS67 decreases H3K4me2/3 in both MV4;11 and MIA PaCa-2 cells, whereas other examined histone methylation marks such as H3K9me3, H3K27me3, and H3K36me3 are not affected . MS67 is effective in suppressing both WDR5-related gene expression programs and WDR5/MLL-induced H3K4 methylations on chromatin[1].
The GI50 values of MS67 in the two most sensitive AML lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively. MLL-r acute leukemia cell lines including MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1 are sensitive to MS67, whereas leukemia cell lines that did not harbor MLL-r (including K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1) are insensitive to MS67[1].
. MS67 binds to VCB (VHL-Elongin C-Elongin B ternary complex), with a Kd of 140 nM[1].

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

MS67 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4;11 cells
Concentration: 0.001 μM, 0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM
Incubation Time: 18 hours
Result: Induced WDR5 degradation at a concentration as low as 1 nM with DC50 of 3.7 nM.
In Vivo

MS67 (75 mg/kg; i.p.; twice daily; 5 days a week; for 20 days) significantly inhibits tumor growth in vivo and prolongs survival of the treated mice[1].
After a single intraperitoneal (i.p.) injection of MS67 at a dose of 75 mg/kg, the Cmax reached at about 4.2 μM, and the concentration of MS67 retained above 0.5 μM over 12 hours[1].

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

Animal Model: MV4;11 MLL-r AML xenograft mouse[1]
Dosage: 75 mg/kg
Administration: i.p.; twice daily; 5 days a week; for 20 days
Result: Inhibited tumor growth in vivo.
Molecular Weight

1030.14

Formula

C52H59F4N9O7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=C(N3C[C@H](N([C@H](C3)C)C)C)C=CC(C4=CC(C(NCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(N=CS7)C)C=C6)C)=O)=O)=O)=O)=CC=C4F)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (97.07 mM; ultrasonic and warming and heat to 60°C; 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 0.9707 mL 4.8537 mL 9.7074 mL
5 mM 0.1941 mL 0.9707 mL 1.9415 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 (sealed storage, away from moisture). 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.73%

COA (255 KB) HNMR (260 KB) LCMS (117 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 0.9707 mL 4.8537 mL 9.7074 mL 24.2685 mL
5 mM 0.1941 mL 0.9707 mL 1.9415 mL 4.8537 mL
10 mM 0.0971 mL 0.4854 mL 0.9707 mL 2.4269 mL
15 mM 0.0647 mL 0.3236 mL 0.6472 mL 1.6179 mL
20 mM 0.0485 mL 0.2427 mL 0.4854 mL 1.2134 mL
25 mM 0.0388 mL 0.1941 mL 0.3883 mL 0.9707 mL
30 mM 0.0324 mL 0.1618 mL 0.3236 mL 0.8090 mL
40 mM 0.0243 mL 0.1213 mL 0.2427 mL 0.6067 mL
50 mM 0.0194 mL 0.0971 mL 0.1941 mL 0.4854 mL
60 mM 0.0162 mL 0.0809 mL 0.1618 mL 0.4045 mL
80 mM 0.0121 mL 0.0607 mL 0.1213 mL 0.3034 mL
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MS67 Related Classifications

Help & FAQs
  • 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.

Keywords:

MS672407452-77-9MS 67MS-67Histone MethyltransferasePROTACsWDR5degraderProtacacticanceracutemyeloidleukemiaH3K4me2/3Inhibitorinhibitorinhibit

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