2. PROTAC Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Cell Cycle/DNA Damage Stem Cell/Wnt MAPK/ERK Pathway JAK/STAT Signaling PI3K/Akt/mTOR Apoptosis
  3. PROTACs FLT3 HSP ERK STAT Akt Apoptosis
  4. MA191

MA191 is a FLT3 PROTAC degrader. MA191 abrogates FLT3 inhibitor resistance from rebound activation of mitogen-activated kinases. MA191 mediates rapid FLT3-ITD degradation through a mechanism requiring VHL, neddylation, and BIM. MA191 reduces FLT3-ITD levels before inducing apoptosis. MA191 halts AML cell proliferation in Danio rerio. MA191 can be used for the study of acute myeloid leukemia (AML) (Pink: FLT3 ligand: (HY-175311), Blue: E3 ligase CRBN Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175312)).

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

MA191

MA191 Chemical Structure

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MA191 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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Akt Akt1 Akt2 Akt3

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Description

MA191 is a FLT3 PROTAC degrader. MA191 abrogates FLT3 inhibitor resistance from rebound activation of mitogen-activated kinases. MA191 mediates rapid FLT3-ITD degradation through a mechanism requiring VHL, neddylation, and BIM. MA191 reduces FLT3-ITD levels before inducing apoptosis. MA191 halts AML cell proliferation in Danio rerio. MA191 can be used for the study of acute myeloid leukemia (AML) (Pink: FLT3 ligand: (HY-175311), Blue: E3 ligase CRBN Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175312))[1].

In Vitro

MA191 (0-100 nM, 24-72 h) inhibits the growth of MV4-11 and MOLM-13 cells with IC50 values between 9.6 and 11 nM[1].
MA191 (50 nM, 6-24 h) inhibits autophosphorylation of FLT3 (pY591) and phosphorylation of ERK1/ERK2, STAT5 and AKT in MV4-11 and MOLM-13 cells[1].
MA191 (10-50 nM, 16-24 h) decreases FLT3-ITD and HSP110 dose- and time-dependently in MV4-11 cells[1].
MA191 (0-100 nM, 6-24 h treatment) induces BIM-dependent and neddylation-dependent degradation of FLT3-ITD in MV4-11 cells, demonstrating DC50 values of 10.5 nM at 16 h and 10 nM at 24 h[1].
MA191 (0-1000 nM, 24-48 h) induces apoptosis of cultured and primary AML cells with FLT3-ITD and does not affect normal immune cells, hematopoietic stem cells, and progenitor cells[1].
MA191 (50-200 nM, 24-72 h) breaks mechanisms of FLT3 inhibitor resistance of AML cells[1].

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

MA191 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 50 nM
Incubation Time: 6, 24 h
Result: Inhibited the autophosphorylation of FLT3 (pY591) and phosphorylation of ERK1/ERK2, STAT5 and AKT.
Decreased the FLT3-ITD levels after 24 h, whereas in RS4-11, FLT3 was less affected.
Increased the level of caspase-3.

Western Blot Analysis[1]

Cell Line: MV4-11 cells, BIM-KD-MV4-11 cells and VHL-KD-MV4-11 cells
Concentration: 10, 20, 50 nM
Incubation Time: 6, 16, 24 h
Result: Degraded FLT3-ITD in MV4-11 cells which was inhibited in BIM-KD-MV4-11 cells.
Degraded HSP110, HSP70, HSP27, and HSP90.
Inhibited the phosphorylation of FLT3-ITD.
Attenuated phosphorylated STAT5 dose- and time-dependently.
Showed a time- and dose-dependent accumulation of active caspase-3 and BIM-EL after 16 h.
Rescued the degradation of FLT3 in cells with a KD of VHL.

Apoptosis Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 100, 200 nM
Incubation Time: 24, 72 h
Result: Did not induce apoptosis in RS4-11 after a 72-h treatment. In MV4-11 cell cultures, the death rate was nearly 100% and in the case of MOLM-13 cell cultures it was 50%.
Induced cell death in MOLM-13, MOLM-13-RES and MOLM-13-RES-AC.
In Vivo

MA191 (200 nM, 48 h, single dose) halts AML cell proliferation without significant toxicity in Danio rerio larvae model[1].

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

Animal Model: MV4-11 cells at density of 1×106 cells/mL were injected into the yolk sac of zebrafish wild-type AB line embryos on day 2 post fertilization[1].
Dosage: 200 nM
Administration: 48 h
Result: Halted AML cell proliferation.
Showed no significant toxicity .
Molecular Weight

1088.32

Formula

C57H73N11O9S
SMILES

[H]N([C@@H](C)C1=CC=C(C2=C(C)N=CS2)C=C1)C([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC([C@@H]4CC[C@H](C(N5CCN(CCNC(C6=CC(OC7=CC=C(NC(NC8=NOC(C(C)(C)C)=C8)=O)C=C7)=CC=N6)=O)CC5)=O)CC4)=O)=O)=O
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
References
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MA191 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:

MA191MA 191MA-191PROTACsFLT3HSPERKSTATAktApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Heat shock proteinsExtracellular signal regulated kinasesPKBProtein kinase Bacute myeloid leukemiaAKTapoptosisInhibitorinhibitorinhibit

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