Jak1 RIMTAC-1
Jak1 RIMTAC-1 is a JAK1 RIMTAC degrader (a PROTAC-like agent) with a DC50 of 322.8 nM. Jak1 RIMTAC-1 forms a ternary complex with JAK1 and RIPK1, thereby recruiting the VHL E3 ligase complex to ubiquitinate JAK1 via the ubiquitin-proteasome system and mediate its subsequent proteasomal degradation. Jak1 RIMTAC-1 does not alter JAK1 mRNA levels (pink: Jak1 ligand-1 (HY-187503); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-B0704)).
For research use only. We do not sell to patients.
- Formula: C54H50F4N10O5S
- Molecular Weight:1027.10
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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
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
JAK1 322.8 nM (DC50) |
VHL |
RIPK1 |
In Vitro
Jak1 RIMTAC-1 (Compound 24) (0.5 μM; 24 h) potently degrades endogenous JAK1 in HEK-293T cells, with a degradation rate of over 50%[1].
Jak1 RIMTAC-1 (500 nM; 6-48 h) induces time-dependent degradation of endogenous JAK1 in HEK-293T cells[1].
Jak1 RIMTAC-1 (1.25-5.0 μM) does not reduce the mRNA expression of JAK1 in HEK-293T cells, confirming the post-translational regulation of JAK1 protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK-293T cells (endogenous JAK1)
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Concentration:0.5 μM
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Incubation Time:24 h
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Result:Induced greater than 50% degradation of endogenous JAK1 protein in HEK-293T cells after 24 h.
Emerged as the most potent JAK1 degrader among the tested series.
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Cell Line:HEK-293T cells (endogenous JAK1)
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Concentration:500 nM
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Incubation Time:6-48 h
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Result:Promoted time-dependent loss of endogenous JAK1 protein in HEK-293T cells when treated at 500 nM.
Chemical Information
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Molecular Weight 1027.10
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Formula C54H50F4N10O5S
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SMILES
O=C(C1=CC=C(C=C1)C2=CC=NC(NC3=CC=C(C=C3)N4CCN(CC4)C(CCCCCCCC(NC5=NC6=C(S5)C=C(C=C6)C7=CC=C(C(NC(CC8=CC=CC(OC(F)(F)F)=C8)=O)=C7)F)=O)=O)=N2)NCC#N
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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)
Jak1 RIMTAC-1 Related Classifications
HY-187502 Related Classifications
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