2. PROTAC Epigenetics
  3. PROTACs METTL3
  4. 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).

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PROTAC METTL3 degrader 1

PROTAC METTL3 degrader 1 Chemical Structure

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PROTAC METTL3 degrader 1 Related Antibodies

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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).

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.

PROTAC METTL3 degrader 1 Related Antibodies

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.
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
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Please store the product under the recommended conditions in the Certificate of Analysis.
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PROTAC METTL3 degrader 1 Related Classifications

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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:

PROTAC METTL3 degrader 1PROTACsMETTL3Methyltransferase-like 3METTL14gastric cancer patient-derived organoidsMOLM-13 cellsVHLleukemia cellsgastric cancer cellsubiquitingastric canceracute myeloid leukemiaInhibitorinhibitorinhibit

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