TO-1187
TO-1187 is a selective HDAC6 PROTAC degrader (DC50: 5.81 nM). TO-1187 promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors.
(Pink: HDAC6 ligand (HY-173386); Blue: Cereblon ligand (HY-41547 ); Black: linker (HY-140212)).
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- Formel: C34H35N9O7
- Molecular Weight:681.70
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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HDAC6 5.81 nM (DC50) |
Cereblon |
TO-1187 (100 nM, 6 h) highly selectively degrades HDAC6 in human multiple myeloma cells (MM.1S) (Dmax: 94%, DC50: 5.81 nM)[1].
TO-1187 (100 nM, 72 h) does not show significant antiproliferative activity in MM.1S cells, indicating that it has low toxicity[1].
TO-1187 (1-10000 nM) also exhibits a dose-dependent HDAC6 degradation ability in HeLa cells[1].
TO-1187 (100 nM, Pre-treatment for 1 h, then treatment for 6 h) HDAC6 is degraded by CRBN E3 ligase and proteasome in MM.1S cells[1].
TO-1187 (100 nM, 6 h) only degrades HDAC6 in MM.1S cells without affecting other proteins (such as CRBN novel substrates: IKZF1, IKZF3, CK1α, SALL4 and GSPT1), further confirming its high selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human multiple myeloma cells (MM.1S)
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Concentration:100 nM
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Incubation Time:0.5-24 h
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Result:Showed monoselectivity for HDAC6, and no degradation selectivity for other HDAC (such as HDAC3 and HDAC8) was observed at a concentration of 25 µM.
Initiated HDAC6 degradation within 30 minutes, the degradation rate reaches 45% within 1 hour, and the maximum degradation effect is achieved within 6 hours (Dmax: 94%).
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Cell Line:human multiple myeloma cells (MM.1S)
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Concentration:100 nM
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Incubation Time:Pre-treatment for 1 h, then treatment for 6 h
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Result:Degraded HDAC6 via the ubiquitin-proteasome system mediates by CRBN E3 ligase, and its degradation can be competitively inhibited by proteasome inhibitors (MG132 (HY-13259) and Bortezomib (HY-10227)).
Dose-dependently blocked HDAC6 degradation by Thalidomide (HY-14658) (CRBN ligand), demonstrated its dependence on CRBN recruitment for degradation.
Chemical Information
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Molecular Weight 681.70
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Formel C34H35N9O7
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SMILES
O=C(C1=CC=C(C=C1)CN(CC2=CN=CC=C2)CC3=CN(N=N3)CCOCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)NO
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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