Art. -Nr.: HY-141796

MS67

Kundenbewertung

Based on 1 Customer Validation

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a K_d of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
(Pink: WDR5 ligand (HY-184594); Blue: VHL ligand (HY-112078); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.12%
CAS. Nr.: 2407452-77-9
Formel: C₅₂H₅₉F₄N₉O₇S
Molecular Weight:1030.14

Speicherung:

-20°C, sealed storage, away from moisture

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

MS67 Chemical Structure

CAS. Nr.: 2407452-77-9

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a K_d of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects^[1]. (Pink: WDR5 ligand (HY-184594); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target^[1]

VHL	WDR5 63 nM (Kd)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
K562	GI₅₀	>2500 nM Compound: MS67	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 38085679]
MV4-11	GI₅₀	15 nM Compound: MS67	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 38085679]

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 K_d of 140 nM^[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 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.

Chemical Information

CAS. Nr. 2407452-77-9
Appearance Solid
Molecular Weight 1030.14
Formel C₅₂H₅₉F₄N₉O₇S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit

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)

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

0.9707 mL

4.8537 mL

9.7074 mL

5 mM

0.1941 mL

0.9707 mL

1.9415 mL

10 mM

0.0971 mL

0.4854 mL

0.9707 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 (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.

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 (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Xufen Yu, et al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578. [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

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

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

MS67

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Lipid Metabolism Compound Library

Heterocyclic Compound Library

PROTAC Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS67

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Lipid Metabolism Compound Library

Heterocyclic Compound Library

PROTAC Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS67 Related Classifications

HY-141796 Related Classifications