2417135-66-9
Chemical Structure
Envudeucitinibum
Synonym(s): Envudeucitinib; ESK-001
- CAS No.: 2417135-66-9
- Formula:C22H18D6N6O3
- Molecular Weight:426.50
InChIKey: FKCATCQHVCOBCX-WFGJKAKNSA-N
SMILES: COC1=C(C2=NN(C([2H])([2H])[2H])C=N2)C=CC=C1NC3=CC(NC(C4CC4)=O)=NC=C3C(CC([2H])([2H])[2H])=O
Biological Activity: Envudeucitinibum (Envudeucitinib; ESK-001) is an orally active and selective TYK2 allosteric inhibitor with an IC50 range of 104-149 nM. Envudeucitinibum blocks JH1 catalytic activity by specifically binding to the JH2 domain of TYK2, thereby inhibiting downstream signaling pathways. Envudeucitinibum is used for research on plaque psoriasis, systemic lupus erythematosus, and other immune-mediated diseases[1][2][3].
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Envudeucitinibum | 99.56% | Envudeucitinibum (Envudeucitinib; ESK-001) is an orally active and selective TYK2 allosteric inhibitor with an IC50 range of 104-149 nM. Envudeucitinibum blocks JH1 catalytic activity by specifically binding to the JH2 domain of TYK2, thereby inhibiting downstream signaling pathways. Envudeucitinibum is used for research on plaque psoriasis, systemic lupus erythematosus, and other immune-mediated diseases. | ||||||||||||||||||||
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JAK-IN-26 | 98.04% | JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM). | ||||||||||||||||||||
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References
- [1]. Ucpinar S, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of the oral allosteric TYK2 inhibitor ESK-001 using a randomized, double-blind, placebo-controlled study design. Clinical and translational science. 2024 Dec;17(12):e70094. [Content Brief]
- [2]. Papp KA, et al. Safety and efficacy of envudeucitinib, a highly selective, oral allosteric TYK2 inhibitor, in patients with moderate-to-severe plaque psoriasis: Results from the 52-week open-label extension period of the phase 2 STRIDE study. Journal of the American Academy of Dermatology. 2026 Jan;94(1):187-195. [Content Brief]
- [3]. Alumis, Inc., et al. Process of making a TYK2 inhibitor and intermediates thereof. WO2026128621A3. WIPO. 2026-07-02.
