YL633
YL633 is a selective CRBN-recruiting HDAC8 PROTAC degrader with DC50 = 3.3 nM. YL633 binds to the CRBN E3 ubiquitin ligase and mediates HDAC8 degradation. YL633 inhibits HDAC3 enzymatic activity with IC50 of 342.9 nM, and induces degradation of HDAC6 and HDAC7. YL633 inhibits DLBCL cell proliferation. YL633 can be used in research related to diffuse large B-cell lymphoma.
(Pink: HDAC8 ligand (HY-189873); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3100239-28-6
- Formula: C33H40N6O5
- Molecular Weight:600.71
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
HDAC8 3.3 nM (DC50) |
HDAC8 1.3 nM (IC50) |
HDAC6 |
HDAC7 |
HDAC3 342.9 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | DC50 |
3.3 nM
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Half-maximal degradation of HDAC8 in human MDA-MB-231 breast cancer cells after 8 hrs assessed by Western blot.
Half-maximal degradation of HDAC8 in human MDA-MB-231 breast cancer cells after 8 hrs assessed by Western blot.
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acs.jmedchem.6c01636 |
| MDA-MB-231 | DC50 |
14 nM
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Half-maximal degradation of HDAC7 in human MDA-MB-231 breast cancer cells assessed by Western blot.
Half-maximal degradation of HDAC7 in human MDA-MB-231 breast cancer cells assessed by Western blot.
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acs.jmedchem.6c01636 |
| MDA-MB-231 | DC50 |
8 nM
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Half-maximal degradation of HDAC6 in human MDA-MB-231 breast cancer cells assessed by Western blot.
Half-maximal degradation of HDAC6 in human MDA-MB-231 breast cancer cells assessed by Western blot.
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acs.jmedchem.6c01636 |
In Vitro
YL633 inhibits the proliferation of DLBCL cells at low micromolar concentrations[1].
YL633 (A27) is a potent cell-free HDAC8 inhibitor (IC50 = 1.3 nM) with selectivity over HDAC3 (IC50 = 342.9 nM); it also maintains effective CRBN binding in the His-CRBNmidi FP assay[1].
YL633 (0.2-16000 nM; 0-24 h) selectively degrades HDAC8 in MDA-MB-231 cells with DC50 = 3.3 nM and does not affect HDAC1/2/3[1].
YL633 (100 nM; 14 h) induces HDAC8 degradation in MDA-MB-231 cells, and this degradation effect is completely blocked by proteasome inhibitors, neddylation inhibitors, and excess Pomalidomide (HY-10984)[1].
YL633 (0-1000 nM; 8 h) preferentially downregulates HDAC8 and also downregulates HDAC6/HDAC7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human breast cancer cells
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Concentration:0.2, 1, 4, 16, 64, 250, 1000, 4000, 16000 nM (dose-dependent)
100 nM (time-dependent and washout assay) -
Incubation Time:8 h (dose-dependent)
1, 2, 4, 8, 16, 24 h (time-dependent)
0, 2, 4, 8, 16, 24 h (washout) -
Result:Degradesd HDAC8 in MDA-MB-231 cells with DC50 = 3.3 nM and spares HDAC1/2/3.
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Cell Line:MDA-MB-231 human breast cancer cells
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Concentration:100 nM
MG132 (HY-13259) (10uM)
Bortezomib (HY-10227) (1uM)
MLN4934 (1uM)
Pomalidomide (HY-10984) (10uM)
CB-5083 (HY-12861) (3uM) -
Incubation Time:14 h
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Result:Induced HDAC8 degradation in MDA-MB-231 cells, and this degradation effect is completely blocked by proteasome inhibitors, neddylation inhibitors, and excess Pomalidomide.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 0.25, 4, 16, 64, 250, 1000 nM
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Incubation Time:8 h
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Result:Downregulated HDAC8 and also downregulated HDAC6/HDAC7.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 3100239-28-6
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Molecular Weight 600.71
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Formula C33H40N6O5
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SMILES
CCNNC(C1=CC=C(C=C1)C2CCN(CC2)CC3CCN(CC3)C4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O
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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)
YL633 Related Classifications
HY-189839 Related Classifications
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