XY-09-36
XY-09-36 is a HDAC8 PROTAC degrader with a DC50 value of 30 nM (HEK 293T eGFP.HDAC8-IRES-mCherry reporter cells, 24 h). XY-09-36 binds HDAC8 and recruits VHL E3 ubiquitin ligase, inducing HDAC8 ubiquitination and proteasomal degradation; the IC50 values of XY-09-36 against HDAC8 and HDAC6 are 2.03 μM and 7.21 μM, respectively. XY-09-36 selectively reduces the viability of STAG2-mutant Ewing sarcoma cells. XY-09-36 increases acetylated SMC3 levels. XY-09-36 can be used for research on Ewing sarcoma.
(Pink: HDAC8 Target protein ligand; Blue: VHL ligand (HY-125905); Black: linker (HY-W007469)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3025448-71-6
- Formule: C48H58FN7O8S
- Masse moléculaire:912.08
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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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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
HDAC8 2.03 μM (IC50) |
HDAC6 7.21 μM (IC50) |
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | DC50 |
100 nM
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HDAC8 degradation in HEK 293T eGFP.HDAC8-IRES-mCherry reporter cells after 5 h exposure to XY-09-36 measured by GFP/mCherry ratio.
HDAC8 degradation in HEK 293T eGFP.HDAC8-IRES-mCherry reporter cells after 5 h exposure to XY-09-36 measured by GFP/mCherry ratio.
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42677456 |
| HEK-293T | DC50 |
30 nM
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HDAC8 degradation in HEK 293T eGFP.HDAC8-IRES-mCherry reporter cells after 24 h exposure to XY-09-36 measured by GFP/mCherry ratio.
HDAC8 degradation in HEK 293T eGFP.HDAC8-IRES-mCherry reporter cells after 24 h exposure to XY-09-36 measured by GFP/mCherry ratio.
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42677456 |
| TC-32 | DC50 |
100 nM
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HDAC8 degradation in STAG2-mutant Ewing sarcoma TC32 cells after XY-09-36 exposure estimated by Western blot.
HDAC8 degradation in STAG2-mutant Ewing sarcoma TC32 cells after XY-09-36 exposure estimated by Western blot.
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42677456 |
In Vitro
XY-09-36 (5-24 h) degrades HDAC8 in HEK 293T eGFP.HDAC8-IRES-mCherry reporter cells, with a DC50 value of 100 nM at 5 h and 30 nM at 24 h[1].
XY-09-36 (10 nM-5 μM; 0.5-72 h) degrades HDAC8 in STAG2-mutant TC32 Ewing sarcoma cells with a cellular DC50 of approximately 100 nM and increases acSMC3 without affecting other HDACs[1].
XY-09-36 (1 μM; 6 h) selectively degrades HDAC8 in EW8 Ewing sarcoma cells without affecting other HDACs or HDAC8-related complexes[1].
XY-09-36 (5 h) selectively downregulates HDAC8 in Kelly cells[1].
XY-09-36 (1 μM)-induced HDAC8 degradation is rescued by proteasome, neddylation, HDAC8 ligand, and VHL ligand interventions, confirming a VHL/proteasome-dependent mechanism[1].
XY-09-36 (250 nM-5 μM; 3-12 days) selectively reduces the viability of STAG2-mutant TC32 and SKES-1 Ewing cells and increases acSMC3, inducing acSMC3 at 250 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:STAG2-mutant Ewing sarcoma TC32 cells
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Concentration:1 μM
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Incubation Time:0.5, 1, 2, 4, 6, 24, 48, 72 h
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Result:Time-course with 1 μM XY-09-36 revealed rapid and sustained degradation as early as 30 min, maintained through 24 h, with maximum degradation at 24 h; after 24 h, limited HDAC8 recovery was observed.
In TC32 immunoblotting, robust HDAC8 depletion was accompanied by increased acSMC3, whereas levels of other HDACs remained unaffected.
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Cell Line:STAG2-WT (A673, TC71) and STAG2-mut (TC32, SKES-1) Ewing cells
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Concentration:1 μM
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Incubation Time:12 days
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Result:Induced a modest but selective reduction in viability of STAG2-mut cells only.
Chemical Information
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CAS No. 3025448-71-6
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Masse moléculaire 912.08
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Formule C48H58FN7O8S
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SMILES
ONC(C1=CC2=C(C=CN2CCOC3=CC=C(CN(C)CCCOC4=CC(C5=C(C)N=CS5)=CC=C4CNC([C@H]6N(C([C@H](C(C)(C)C)NC(C7(F)CC7)=O)=O)C[C@H](O)C6)=O)C=C3)C=C1)=O
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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.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XY-09-36 Related Classifications
HY-189823 Related Classifications
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