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Cat. No.: HY-162930

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PROTAC METTL3 degrader 1

PROTAC METTL3 degrader 1 is a VHL-based PROTAC METTL3 degrader (DC₅₀: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC₅₀ value of 341 nM. PROTAC METTL3 degrader 1 can be used for the research of acute myeloid leukemia and gastric cancer.
(Pink: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217); Black: linker).

For research use only. We do not sell to patients.

Formula: C₅₆H₇₇F₂N₁₁O₅S
Molecular Weight:1054.34

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

PROTAC METTL3 degrader 1 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC METTL3 degrader 1 is a VHL-based PROTAC METTL3 degrader (DC₅₀: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC₅₀ value of 341 nM. PROTAC METTL3 degrader 1 can be used for the research of acute myeloid leukemia and gastric cancer^[1]. (Pink: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217); Black: linker).

All PROTACs Isoforms :

In Vitro

PROTAC METTL3 degrader 1 (KH12) inhibits the methyltransferase activity of the purified METTL3/METTL14 complex with an IC₅₀ of 341 nM^[1].
PROTAC METTL3 degrader 1 (KH12) (0.039-5 μM; 0-48 h) induces potent, dose- and time-dependent degradation of METTL3 in MOLM-13 cells, with a DC₅₀ of 220 nM, 84% degradation at 1 μM for 24 h, and over 90% degradation at 1 μM for 24 h^[1].
PROTAC METTL3 degrader 1 (KH12) (1 μM; 2.5 h pre-incubation, 6 h treatment) induces METTL3 degradation via the ubiquitin-proteasome system, not the autophagy-lysosomal pathway, in HEK293T cells^[1].
PROTAC METTL3 degrader 1 (KH12) (72 h) potently suppresses the proliferation of MOLM-13 acute myeloid leukemia cells with an IC₅₀ of 1.04 μM^[1].
PROTAC METTL3 degrader 1 (KH12) (0.1-5 μM; 48 h) reduces c-MYC protein levels in a dose-dependent manner in MOLM-13 cells^[1].
PROTAC METTL3 degrader 1 (KH12) (5 μM; 48 h) promotes myeloid differentiation of MOLM-13 acute myeloid leukemia cells, as demonstrated by increased CD11b expression^[1].
PROTAC METTL3 degrader 1 (KH12) (1-10 μM; 48 h) induces dose-dependent apoptosis in MOLM-13 acute myeloid leukemia cells, with 78% apoptotic cells^[1].
PROTAC METTL3 degrader 1 (KH12) (0.1-10 μM; 24 h) reduces METTL3 protein levels in GES-1 normal gastric cells, AGS gastric cancer cells, and SNU484 gastric cancer cells^[1].
PROTAC METTL3 degrader 1 (KH12) (72 h) potently suppresses the proliferation of AGS and SNU484 gastric cancer cells with IC₅₀ values of 1.48 μM and 3 μM respectively, while having minimal effect on GES-1 normal gastric cells^[1].
PROTAC METTL3 degrader 1 (KH12) (1 μM; 24 h) reduces METTL3 protein levels in both cytoplasmic and nuclear fractions of AGS and SNU484 gastric cancer cells^[1].
PROTAC METTL3 degrader 1 (KH12) (0.0001-100 μM; 5 days) significantly suppresses the growth of gastric cancer patient-derived organoids (GA215T and GA352T), with GA215T organoids showing greater sensitivity to the Target Reagent than to small molecule METTL3 inhibitors^[1].

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

Western Blot Analysis^[1]

Cell Line:

HEK293T cells
Concentration:

1 μM
Incubation Time:

2.5 h (pre-incubation with inhibitors); 6 h (target reagent treatment)
Result:

Induced METTL3 degradation.
Did not have its induced METTL3 degradation rescued by pre-treatment with 3-MA.

Western Blot Analysis^[1]

Cell Line:

MOLM-13 cells
Concentration:

0.1 μM, 1 μM, 5 μM
Incubation Time:

48 h
Result:

Reduced c-MYC protein levels in a dose-dependent manner.

Cell Differentiation Assay^[1]

Cell Line:

MOLM-13 acute myeloid leukemia cells
Concentration:

5 μM
Incubation Time:

48 h
Result:

Induced a significant increase in CD11b expression, indicating promotion of myeloid differentiation.

Apoptosis Analysis^[1]

Cell Line:

MOLM-13 acute myeloid leukemia cells
Concentration:

1 μM, 5 μM, 10 μM
Incubation Time:

48 h
Result:

Induced apoptosis in a dose-dependent manner.
Induced 48% apoptotic cells at 5 μM.
Induced 78% apoptotic cells at 10 μM.

Western Blot Analysis^[1]

Cell Line:

AGS gastric cancer cells, SNU484 gastric cancer cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Reduced METTL3 protein levels in both cytoplasmic and nuclear fractions of AGS and SNU484 cells.

Chemical Information

Molecular Weight 1054.34
Formula C₅₆H₇₇F₂N₁₁O₅S
SMILES

O=C1NC2(CCN(C3=NC=NC(NCCCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)=C3)CC2)CN(C7=C(F)C=C(CN8CCC(C)(C)CC8)C(F)=C7)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Hwang K, et al. Targeted degradation of METTL3 against acute myeloid leukemia and gastric cancer. Eur J Med Chem. 2024;279:116843. [Content Brief]

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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.

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Biological Activity
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PROTAC METTL3 degrader 1

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC METTL3 degrader 1 Related Classifications

HY-162930 Related Classifications