2. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Histone Demethylase Apoptosis Caspase PARP
  4. YTHu78

YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145)).

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

YTHu78

YTHu78 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

YTHu78 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Demethylase Isoform Specific Products:

View All Isoforms
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

View All Caspase Isoform Specific Products:

View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145))[1].

IC50 & Target[1]

Cereblon

 

KDM5B

 

Caspase 3

 

In Vitro

YTHu78 (72 h) shows antiproliferative activity against MV-4-11, HL60, MM.1S and OCI-AML3 cells, with IC50s of 1.34 μM, 6.58 μM, 1.03 μM, 9.07 μM[1].

YTHu78 (0.03-20 μM, 1-24 h) reduces KDM5B protein levels through the proteasome-mediated pathway in MV-4-11 and MM.1S cells[1].

YTHu78 (0.03-20 μM, 48 h) induces lytic apoptosis dependent on caspase in MV-4-11 and MM.1S cells[1].

YTHu78 (72 h) exhibits negligible anti-proliferative effects against primary HUVEC, GM00637 fibroblasts, HaCaT keratinocytes, GES-1, and HEK293 cells, with IC50s >20 μM[1].

YTHu78 (72 h) shows limited antiproliferative effects on refractory solid tumors and modestly sensitive solid tumor models, including HCC, PDAC, gGBM, and TNBC cells, with IC50s >20 μM and Huh-7, HCC1937, PANC-1 cells, IC50s 6-20 μM[1].

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

YTHu78 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11 cells, MM.1S cells
Concentration: 0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
Incubation Time: 1 h, 3 h, 6 h, 12 h, 24 h,48 h
Result: Induced KDM5B protein degradation at a concentration of 0.74 μM and depleted KDM5B in a time-dependent manner, with maximal degradation achieved after 12 hours of treatment at a concentration of 5 μM.
Increased H3K4me3 levels.
Activated Caspase-3, induced PARP cleavage, and upregulated cleaved-GSDMD and cleaved-GSDME after 48 h of 5 μM treatment.

RT-PCR[1]

Cell Line: MV-4-11 cells, MM.1S cells
Concentration: 0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
Incubation Time: 24 h
Result: Did not affect KDM5B mRNA levels at low doses, increased mRNA levels at high concentrations in MM.1S cells.

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells, MM.1S cells
Concentration: 0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
Incubation Time: 48 h
Result: Increased apoptotic population, induced mild G0/G1 cell cycle arrest at high doses, and increased LDH release.
Molecular Weight

632.63

Formula

C33H28N8O6
SMILES

O=C1NC(OC2=CN(CC3=CC=C(CCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)C=C3)N=C2)=NC7=CN=CC=C71
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

YTHu78 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

YTHu78YTHu 78YTHu-78PROTACsHistone DemethylaseApoptosisCaspasePARPpoly ADP ribose polymeraseDegraderHematologic malignanciesMV-4-11 cellsMM.1S cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
YTHu78
Cat. No.:
HY-175036
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.