PROTAC HSP70 Degrader-1
PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia.
(Pink: HSP70 ligand (HY-181148); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Formula: C34H31N7O4
- Molecular Weight:601.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
PROTAC HSP70 Degrader-1 (compound C4) (2-32 μM; 48-72 h) degrades HSP70 in RKO cells with 56% degradation at 8 μM for 48 h, showing concentration- and time-dependent activity[1].
PROTAC HSP70 Degrader-1 (8 μM; 48 h) inhibits RKO cell viability by 26% at 8 μM for 48 h[1].
PROTAC HSP70 Degrader-1 (8 μM; 48 h) selectively degrades cytosolic HSP70 isoforms (HSP70α, HSP70β, HSP76) but not BiP in RKO cells at 8 μM for 48 h[1].
PROTAC HSP70 Degrader-1 (8 μM; 48 h) combined with 4 μM DTHIB inhibits RKO cell viability by 78%[1].
PROTAC HSP70 Degrader-1 (24 h) increases HSP70 ubiquitination in RKO cells[1].
PROTAC HSP70 Degrader-1 facilitates HSP70-CRBN ternary complex formation, which is blocked by R17 or thalidomide[1].
PROTAC HSP70 Degrader-1 (16 μM; 72 h) had its HSP70 degradation activity in RKO cells impaired by CRBN depletion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RKO cells
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Concentration:2-32 μM; 8 μM; 16 μM
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Incubation Time:48 h; 72 h
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Result:Degraded HSP70 by 56% at 8 μM for 48 h. Exhibited concentration-dependent degradation activity across 2-32 μM for 48 h. Caused noticeable HSP70 degradation at 16 μM for 48 h, with further reduction at 72 h.
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Cell Line:RKO cells
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Concentration:8 μM
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Incubation Time:48 h
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Result:Inhibited RKO cell viability by 26% at 8 μM for 48 h.
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Cell Line:RKO cells
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Concentration:8 μM
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Incubation Time:48 h
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Result:Degraded cytosolic HSP70 isoforms HSP70α, HSP70β, and HSP76 at 8 μM for 48 h but exerted minimal effect on the endoplasmic reticulum-resident BiP.
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Cell Line:RKO cells
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Concentration:8 μM (in combination with 4 μM DTHIB)
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Incubation Time:48 h
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Result:Inhibited RKO cell viability by 78% at 8 μM for 48 h when combined with 4 μM DTHIB.
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Cell Line:RKO cells
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Concentration:16 μM
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Incubation Time:72 h
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Result:Lost most of its HSP70 degradation ability at 16 μM for 72 h after CRBN depletion via siRNA knockdown.
Chemical Information
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Molecular Weight 601.65
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Formula C34H31N7O4
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SMILES
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCNC4=C5C=CC=CC5=NC(C(N6)=CC7=C6C=CC=C7)=N4)=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)
PROTAC HSP70 Degrader-1 Related Classifications
HY-181147 Related Classifications
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