2. PROTAC Epigenetics Apoptosis
  3. PROTACs METTL3 Apoptosis Bcl-2 Family
  4. AF151

AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)).

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

AF151

AF151 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Customer Review

Based on 1 publication(s) in Google Scholar

AF151 Related Antibodies

Top Publications Citing Use of Products

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875))[1].

IC50 & Target[1]

Bcl-2

 

VHL

 

Mcl-1

 

In Vitro

AF151 (0-10 μM, 0-72 h) can efficiently degrade METTL3 protein in a time-dependent manner and significantly inhibit cell growth of MOLM-13 cells (DC50 = 0.43 μM, IC50 = 0.45 μM)[1].
AF151 (2 μM, 24-48 h) can significantly reduce m6A levels in MOLM-13 cells[1].
AF151 (0.1-5 μM, 48 h) can dose dependently induce cell apoptosis and reduce the level of anti apoptotic proteins in MOLM-13 cells[1].
AF151 (72 h) can work synergistically with Venetoclax (HY-15531) in MOLM-13 cells[1].
AF151 (0.001-10 μM) can promote the binding of METTL3 and VHL (AF151 = 363 nM, AF151-METTL3 = 79.9 nM)[1].

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

AF151 Related Antibodies

Cell Viability Assay[1]

Cell Line: MOLM-13 cells
Concentration: 0.1-10 μM
Incubation Time: 72 h
Result: Significantly inhibited cell growth with the IC50 of 0.45 μM, superior to STM2457 (HY-134836) (IC50 = 1.82 μM) and WD6305 (HY-160415) (IC50 = 0.78 μM).

Western Blot Analysis[1]

Cell Line: MOLM-13 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Decreased the protein level of Mcl-1 and Bcl-2.

RT-PCR[1]

Cell Line: MOLM-13 cells
Concentration: 2 μM
Incubation Time: 24-48 h
Result: Did not cause significant changes in the expression of METTL3 and METTL14 genes.
Molecular Weight

1043.32

Formula

C61H70N8O6S
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(C2=CC=C(CNC([C@H]3N(C([C@@H](NC(CCC4=CC=C(C5=CC=C(COC6=CN=CC(C(NCC7=CC(NC(CN8CCC(C)(C)CC8)=C9)=C9C=C7)=O)=C6)C=C5)C=C4)=O)C(C)(C)C)=O)C[C@H](O)C3)=O)C=C2)SC=N1
Shipping

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 (95.85 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 0.9585 mL 4.7924 mL 9.5848 mL
5 mM 0.1917 mL 0.9585 mL 1.9170 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.

  • Molarity Calculator

  • Dilution Calculator

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
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Calculation results:
Working solution concentration: mg/mL
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 0.9585 mL 4.7924 mL 9.5848 mL 23.9620 mL
5 mM 0.1917 mL 0.9585 mL 1.9170 mL 4.7924 mL
10 mM 0.0958 mL 0.4792 mL 0.9585 mL 2.3962 mL
15 mM 0.0639 mL 0.3195 mL 0.6390 mL 1.5975 mL
20 mM 0.0479 mL 0.2396 mL 0.4792 mL 1.1981 mL
25 mM 0.0383 mL 0.1917 mL 0.3834 mL 0.9585 mL
30 mM 0.0319 mL 0.1597 mL 0.3195 mL 0.7987 mL
40 mM 0.0240 mL 0.1198 mL 0.2396 mL 0.5990 mL
50 mM 0.0192 mL 0.0958 mL 0.1917 mL 0.4792 mL
60 mM 0.0160 mL 0.0799 mL 0.1597 mL 0.3994 mL
80 mM 0.0120 mL 0.0599 mL 0.1198 mL 0.2995 mL
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AF151 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:

AF151AF 151AF-151PROTACsMETTL3ApoptosisBcl-2 FamilyMethyltransferase-like 3PROTACcancerapoptosisBcl-2m6AMOLM-13Inhibitorinhibitorinhibit

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