PROTAC YTHDC1 Degrader-1
PROTAC YTHDC1 Degrader-1 is a selective, CRBN-recruiting YTHDC1 PROTAC degrader with a DC50 of 11.42 nM. PROTAC YTHDC1 Degrader-1 induces ubiquitination and degradation of YTHDC1. PROTAC YTHDC1 Degrader-1 induces G1 phase arrest and inhibits cell cycle progression. PROTAC YTHDC1 Degrader-1 also induces Apoptosis. PROTAC YTHDC1 Degrader-1 exhibits anticancer activity against leukemia. PROTAC YTHDC1 Degrader-1 can be used for the research of acute myeloid leukemia.
(Pink: YTHDC1 Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Formula: C32H32ClN9O5
- Molecular Weight:658.11
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Storage:
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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Biological Activity
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Chemical Information
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- References
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Biological Activity
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Cereblon |
PROTAC YTHDC1 Degrader-1 (Compound XY-2) (1-5000 nM; 2-48 h) induces potent, dose-dependent and time-dependent proteasomal degradation of YTHDC1 in MOLM13 acute myeloid leukemia (AML) cells, with a DC50 of 11.42 nM and a maximum degradation rate of 95%[1].
PROTAC YTHDC1 Degrader-1 (1-5000 nM; 48 h) induces potent, dose-dependent proteasomal degradation of YTHDC1 in Kasumi-1 AML cells, with a DC50 of 13.59 nM and a maximum degradation rate of 92%[1].
PROTAC YTHDC1 Degrader-1 (1-5000 nM; 48 h) exerts selective degradation of YTHDC1 over YTHDC2 and YTHDF2 in MOLM13 AML cells[1].
PROTAC YTHDC1 Degrader-1 (72 h) potently inhibits the viability of various AML cell lines with low nanomolar IC50 values, while exhibiting low cytotoxicity in non-AML and normal cell lines[1].
PROTAC YTHDC1 Degrader-1 (10-200 nM; 7 days) dose-dependently impairs the clonogenic potential of MOLM13 and Kasumi-1 acute myeloid leukemia (AML) cells, with a superior effect compared to its parental inhibitor XY-0[1].
PROTAC YTHDC1 Degrader-1 (10-100 nM; 48 h) induces apoptosis in MOLM13 and Kasumi-1 acute myeloid leukemia (AML) cells in a dose-dependent manner, and exhibits superior potency over its parent inhibitor XY-0[1].
Treatment of MOLM13 acute myeloid leukemia (AML) cells with PROTAC YTHDC1 Degrader-1 (100 nM; 48 h) inhibits transcriptional programs associated with cell cycle progression and proliferation signals[1].
PROTAC YTHDC1 Degrader-1 reduces the stability of key G1/S transition-regulating mRNAs in MOLM13 acute myeloid leukemia (AML) cells[1].
PROTAC YTHDC1 Degrader-1 (10-100 nM; 48 h) induces G1 phase cell cycle arrest in MOLM13 acute myeloid leukemia (AML) cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM13 acute myeloid leukemia (AML) cells
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Concentration:0.1 μM; 1-5000 nM; 100 nM
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Incubation Time:48 h; 2 h, 4 h, 8 h, 12 h, 24 h, 48 h
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Result:Showed superior YTHDC1 degradation efficacy compared to other PROTAC derivatives at 0.1 μM for 48 h.
Induced dose-dependent degradation of YTHDC1 with a half-maximal degradation concentration (DC50) of 11.42 nM and a maximum degradation efficiency (Dₘₐₓ) of 95% at 1-5000 nM for 48 h.
Caused marked YTHDC1 reduction by 8 h, with nearly complete degradation by 24 h at 100 nM.
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Cell Line:Kasumi-1 acute myeloid leukemia (AML) cells
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Concentration:1-5000 nM
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Incubation Time:48 h
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Result:Induced dose-dependent degradation of YTHDC1, with a DC50 of 13.59 nM and a Dₘₐₓ of 92%.
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Cell Line:MOLM13 and Kasumi-1 AML cells
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Concentration:10-200 nM
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Incubation Time:7 days
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Result:Induced a concentration-dependent reduction in colony-forming ability in MOLM13 and Kasumi-1 cells, with significantly stronger activity than its parent inhibitor XY-0.
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Cell Line:MOLM13 and Kasumi-1 AML cells
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Concentration:10-100 nM
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Incubation Time:48 h
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Result:Induced a concentration-dependent increase in early and late apoptotic populations in MOLM13 and Kasumi-1 cells, with significantly stronger pro-apoptotic activity than its parent inhibitor XY-0.
| Species | Dose | Route | Tmax | Cmax | AUC0-∞ | T1/2 (Elimination) |
|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.p. | 0.083 h | 1587 ng/mL | 1100 ng·h/mL | 11.6 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female)[1]
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Dosage:2.5 mg/kg; 5 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Significantly reduced tumor volume and tumor weight relative to vehicle controls at 2.5 mg/kg.
Showed even greater reduction in tumor volume and tumor weight at 5 mg/kg.
Caused no appreciable body weight loss in either treatment group.
Induced marked reduction of YTHDC1 protein levels in xenograft tumor tissues in both treatment groups.
Decreased p-RB, E2F1, CCND1, CCNA2, and CDK4 protein levels in xenograft tumor tissues in both treatment groups.
Increased CDKN1A protein levels in xenograft tumor tissues in both treatment groups.
Reduced CCNA2, CCND1, CDK4, E2F1, and CCNE1 mRNA levels in xenograft tumor tissues in both treatment groups.
Increased CDKN1A mRNA levels in xenograft tumor tissues in both treatment groups.
Chemical Information
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Molecular Weight 658.11
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Formula C32H32ClN9O5
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SMILES
O=C(NCCCCCNC1=C2C(C(N(C3C(NC(CC3)=O)=O)C2=O)=O)=CC=C1)C4=CC(CN5C6=NC(Cl)=NC(NC)=C6N=C5)=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC YTHDC1 Degrader-1 Related Classifications
HY-184495 Related Classifications
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