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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
21 Results for "
IKKε
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "IKKε" in MCE Product Catalog:
42
42 Publications Verification
BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
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Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.
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29 Cited Publications
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MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells .
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4 Cited Publications
BAY-985, a chemical probe, is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy .
2
2 Cited Publications
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
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2 Cited Publications
PROTAC TBK1 degrader-2 is a potent PROTAC degrader of serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM) .
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2 Cited Publications
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TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.
1
1 Cited Publications
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GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
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Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
WS3 is an allosteric inhibitor of 14-3-3 (14-3-3ζ: Kd = 2.29 μM). WS3 activates GSK3β by disrupting the binding of 14-3-3-pGSK3β, promotes the ubiquitination and degradation of NRF2, and inhibits the NRF2-ARE signaling pathway (IC50 = 135 nM). It exerts antioxidant inhibition and chemotherapeutic/ferroptosis sensitizing effects in tumors with hyperactivated NRF2. WS3 binds to EBP1/IKKε and promotes the proliferation of β cells and retinal pigment epithelial (RPE) cells, which can be applied to islet regeneration and RPE expansion transplantation . WS3 is applicable to research related to age-related macular degeneration, retinal degeneration and non-small cell lung cancer .
TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR .
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HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .
Cat. No.: HY-13018A
CAS No.: 2095432-39-4
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MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells .
Cat. No.: HY-U00457
CAS No.: 2058264-32-5
TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC50s of <100 nM.
Cat. No.: HY-13018B
CAS No.: 1781882-89-0
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MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells .
Cat. No.: HY-B0713R
CAS No.: 68302-57-8
Synonyms: AA673 (Standard); Amoxanox (Standard); CHX3673 (Standard)
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Amlexanox (Standard) is the analytical standard of Amlexanox. This product is intended for research and analytical applications. Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.
Cat. No.: HY-138931
CAS No.: 2306877-20-1
TBK1/IKKε-IN-6 (example 110) is a TBK1 and IKKε inhibitor, with IC50 values of <100 nM for both TBK1 and IKKε .
Cat. No.: HY-181271
CAS No.: 3035441-37-0
IKKε-IN-1 is a IKKε inhibitor. IKKε-IN-1 reduces cell viability, inhibits colony formation and cell migration. IKKε-IN-1 induces autophagy (Autophagy) in cancer cells. IKKε-IN-1 can be used in the research of cancers including colorectal cancer, hepatocellular carcinoma, bladder cancer, breast cancer, lung cancer, and cervical cancer .
Cat. No.: HY-P701788
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: IKBKE; I-Kappa-B Kinase Epsilon; Inhibitor Of Nuclear Factor Kappa B Kinase Subunit Epsilon; IKK-Epsilon; IKK-I; IKK-E; IKKE; IKKI; Inhibitor Of Nuclear Factor Kappa-B Kinase Subunit Epsilon; IKK-Related Kinase Epsilon; Inducible I Kappa-B Kinase; Inducib
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-10514R
CAS No.: 702675-74-9
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BX795 (Standard) is the analytical standard of BX795 (HY-10514). This product is intended for research and analytical applications. BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
