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Art. -Nr.: HY-184495

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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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₃₂H₃₂ClN₉O₅
Molecular Weight:658.11

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC YTHDC1 Degrader-1 Chemical Structure

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Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: YTHDC1 Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker).

IC₅₀ & Target

^[1]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

MOLM13 acute myeloid leukemia (AML) cells
Concentration:

0.1 μM; 1-5000 nM; 100 nM
Incubation Time:

48 h; 2 h, 4 h, 8 h, 12 h, 24 h, 48 h
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.

Western Blot Analysis^[1]

Cell Line:

Kasumi-1 acute myeloid leukemia (AML) cells
Concentration:

1-5000 nM
Incubation Time:

48 h
Result:

Induced dose-dependent degradation of YTHDC1, with a DC₅₀ of 13.59 nM and a Dₘₐₓ of 92%.

Cell Proliferation Assay^[1]

Cell Line:

MOLM13 and Kasumi-1 AML cells
Concentration:

10-200 nM
Incubation Time:

7 days
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.

Apoptosis Analysis^[1]

Cell Line:

MOLM13 and Kasumi-1 AML cells
Concentration:

10-100 nM
Incubation Time:

48 h
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.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-∞	T_1/2 (Elimination)
Rat^[1]	5 mg/kg	i.p.	0.083 h	1587 ng/mL	1100 ng·h/mL	11.6 h

In Vivo

XY-2 (2.5-5 mg/kg; i.p.; daily; 10 days) exerts significant, dose-dependent antileukemic activity in BALB/c nude mice bearing MOLM13 xenografts by inducing YTHDC1 degradation and suppressing the RB-E2F cell cycle regulatory axis, with no observed body weight loss indicating favorable tolerability^[1].

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

Animal Model:

BALB/c nude (female)^[1]
Dosage:

2.5 mg/kg; 5 mg/kg
Administration:

i.p.; daily; 10 days
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.

Related Protocols :

Chemical Information

Molecular Weight 658.11
Formel C₃₂H₃₂ClN₉O₅
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Xie Z, et al. Development of the First YTHDC1 Degrader with Improved Antileukemia Activity[J]. JACS Au, 2026.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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