MTP3
MTP3 is a MYC PROTAC Degrator. MTP3 facilitates ternary complex formation with CRBN, driving proteasome-dependent full-length MYC degradation and partially proteasome-independent N-terminal truncated MYC (tMYC) generation. MTP3 induces tMYC formation across multiple cancer cell lines with context-dependent response variability. MTP3 can be used for the research of prostate cancer, breast cancer.
(Pink: c-Myc ligand (HY-173469); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008296)).
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- Formule: C44H38N6O8
- Masse moléculaire:778.81
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Activité biologique
Description
In Vitro
MTP3 (0.5-20 μM; 0.5-4 h) induces dose- and time-dependent loss of full-length MYC and formation of N-terminally truncated tMYC in PC3 prostate cancer cells, with no effect on MYC mRNA levels, and reduces the half-life of full-length MYC from 30.4 min to 15.7 min[1].
MTP3 (20 μM; 2 h) induces tMYC formation in PC3, VCaP, DU145, and MCF7 cancer cell lines, but not in SUM159 or MV4-11 cell lines[1].
MTP3 (10 μM; 2 h) induces CRBN-dependent tMYC formation in PC3 prostate cancer cells[1].
MTP3-induced loss of full-length MYC in PC3 prostate cancer cells is partially proteasome-dependent, while tMYC formation is largely proteasome-independent, as Bortezomib (HY-10227) rescues 50% of full-length MYC levels but not tMYC levels[1].
MTP3 (10 μM; 2 h) induces tMYC that localizes to the nucleus, like full-length MYC, in PC3 prostate cancer cells[1].
MTP3 (20 μM; 96 h) does not reduce viability of PC3 prostate cancer cells, as MYC maintains oncogenic proliferative function[1].
MTP3 (10 μM; 2 h treatment, 24 h post-wash) induces reversible MYC depletion in prostate cancer PC3 cells, with MYC levels recovering within 24 hours after a 2-hour 10 μM treatment and washout[1].
MTP3 (20 μM; 24 h) does not alter MYC gene mRNA transcript read coverage in treated cells after a 24-hour 20 μM treatment[1].
MTP3 (10-20 μM; 2 h) induces context-dependent MYC alteration, causing MYC truncation in breast cancer MCF7 cells and full-length MYC reduction in prostate cancer DU145 and VCaP cells, with no effect on GSPT1 levels, after a 2-hour treatment at 20 μM (MCF7) or 10 μM (DU145, VCaP)[1].
MTP3 (10 μM; 2 h) induces N-terminal truncation of MYC in prostate cancer PC3 cells, with truncated MYC present in both cytoplasmic and nuclear fractions, after a 2-hour 10 μM treatment[1].
MTP3 (20 μM; 24 h) induces subtle gene regulatory changes in PC3 prostate cancer cells, with tMYC serving as a functional proxy for full-length MYC in most gene regulatory processes[1].
MTP3 (10-40 μM; 72 h) enhances the anti-proliferative efficacy of nonsteroidal antiandrogen agent, second-generation nonsteroidal antiandrogen agent, and taxane chemotherapy agent in both androgen receptor-independent PC3 cells and androgen receptor-dependent VCaP cells after 72 hours of combined treatment at concentrations of 10-40 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 prostate cancer cells
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Concentration:0.5; 1; 5; 10; 20 μM
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Incubation Time:0.5-4 h
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Result:Induced dose- and time-dependent loss of full-length MYC and formation of N-terminally truncated tMYC in PC3 prostate cancer cells, with no effect on MYC mRNA levels, and reduces the half-life of full-length MYC from 30.4 min to 15.7 min.
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Cell Line:PC3, VCaP, DU145, MCF7, SUM159, MV4-11 cancer cell lines
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Concentration:20 μM
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Incubation Time:2 h
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Result:Induced formation of tMYC in prostate cancer cell lines PC3, VCaP, and DU145, and breast cancer cell line MCF7.
Caused no detectable changes in full-length MYC or tMYC levels in breast cancer cell line SUM159 and AML cell line MV4-11.
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Cell Line:PC3 prostate cancer cells
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Concentration:10 μM
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Incubation Time:2 h
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Result:Failed to produce tMYC when paired with 10 μM MTP3-O (CRBN-binding deficient analogue) for 2 h, unlike when used alone at 10 μM.
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Cell Line:PC3 prostate cancer cells
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Concentration:10 μM
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Incubation Time:2 h
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Result:Restricted both full-length MYC and tMYC exclusively to the nuclear fraction, with tMYC absent from the cytoplasmic fraction.
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Cell Line:PC3 prostate cancer cells
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Concentration:20 μM
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Incubation Time:96 h
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Result:Left viability of PC3 cells unchanged compared to DMSO-exposed cells, unlike direct and indirect MYC inhibitors which reduced cell viability.
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Cell Line:prostate cancer PC3 cells
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Concentration:10 μM
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Incubation Time:2 h (treatment); 0 h, 2 h, 24 h (post-wash)
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Result:Showed MYC protein levels recovered over the 24-hour period after the initial 2-hour treatment.
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Cell Line:breast cancer MCF7 cells, prostate cancer DU145 cells, prostate cancer VCaP cells
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Concentration:20 μM (MCF7 cells); 10 μM (DU145 and VCaP cells)
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Incubation Time:2 h
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Result:Detected truncated MYC (tMYC) in MCF7 cells, while full-length MYC levels were reduced in DU145 and VCaP cells.
Showed GSPT1 levels remained unchanged across all cell lines.
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Cell Line:prostate cancer PC3 cells
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Concentration:10 μM
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Incubation Time:2 h
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Result:Detected truncated MYC (tMYC) in both cytoplasmic and nuclear fractions, recognized by central and C-terminal MYC antibodies but not N-terminal antibodies.
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Cell Line:androgen receptor-independent prostate cancer PC3 cells, androgen receptor-dependent prostate cancer VCaP cells
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Concentration:20-40 μM (PC3 cells); 10-40 μM (VCaP cells)
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Incubation Time:72 h
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Result:Reduced relative viability of PC3 cells to ~0.25-0.3 when combined with 100 μM nonsteroidal antiandrogen agent, to ~0.6-0.7 when combined with 25 μM second-generation nonsteroidal antiandrogen agent, and to ~0.15-0.2 when combined with 2 μM taxane chemotherapy agent.
Reduced relative viability of VCaP cells to ~0.6-0.7 when combined with 100 μM nonsteroidal antiandrogen agent, to ~0.6-0.7 when combined with 25 μM second-generation nonsteroidal antiandrogen agent, and to ~0.3-0.5 when combined with 2.5 μM taxane chemotherapy agent.
Chemical Information
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Masse moléculaire 778.81
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Formule C44H38N6O8
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SMILES
N#CC(C=C1)=CC=C1C2=CC(C3=CC=C(C(NCCCCCCNC(COC4=C(C(N(C5C(NC(CC5)=O)=O)C6=O)=O)C6=CC=C4)=O)=O)C=C3)=CC(C7=CC=CO7)=N2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MTP3 Related Classifications
HY-173467 Related Classifications
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