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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
30 Results for "
Kelch domain
" in MedChemExpress (MCE) Product Catalog:
Products (30)
30 Results for "Kelch domain" in MCE Product Catalog:
23
23 Cited Publications
Target:
Research Areas:
KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human Kd value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation .
12
Target:
Research Areas:
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
Cat. No.: HY-148480
CAS No.: 2728780-74-1
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Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4) .
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Research Areas:
KI696 isomer is an isomer of KI696 (HY-101140). KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human Kd value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation .
Cat. No.: HY-172563A
Target:
Research Areas:
BTR2000 TFA, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 TFA can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562) .
Cat. No.: HY-157558
Synonyms: 8SGE
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Research Areas:
KDRLKZ-1 (8SGE) is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 0.36 μM), with an IC50 of 0.21 μM and 0.31 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-1 binds to the substrate-binding pocket of the KLHDC2 kelch domain, mimics the interaction of natural substrates and displaces them. KDRLKZ-1 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-1 can be used in scaffold ligand research for PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-P10530
CAS No.: 1364173-77-2
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Research Areas:
Cat. No.: HY-157559
Target:
Research Areas:
KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-172563
Target:
Research Areas:
BTR2000, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562) .
Synonyms: (R,S,R)-LH601A
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Research Areas:
(R,S,R)-ML334 is the isomer of ML334 (HY-110258), and can be used as an experimental control. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
Cat. No.: HY-P5909F
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Research Areas:
Cat. No.: HY-175548
CAS No.: 1912404-14-8
Target:
Research Areas:
Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch
domain and disrupts Keap1-Nrf2 interactions and activate
antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury .
Cat. No.: HY-182927
KLHL12 ligand-1 is a KLHL12 Kelch domain ligand with a Ki of 0.33 μM, Ka of 0.33 μM, submicromolar binding affinity, and selective binding over KEAP1/KLHL19. KLHL12 ligand-1 binds in the substrate cleft of KLHL12, with its 4-methyl group forming a CH-π interaction with Tyr334. KLHL12 ligand-1 binds to cellular KLHL12 in permeabilized and intact cells, and has solvent-exposed positions suitable for modification to create PROTACs. KLHL12 ligand-1 can be used for the research of cancer .
Cat. No.: HY-181887
CAS No.: 3109883-60-2
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Research Areas:
Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with KD values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis .
Cat. No.: HY-P701575
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KBTBD2; BTB And Kelch domain-Containing Protein 1; Prev. BKLHD1; DKFZP566C134; Kelch Repeat And BTB (POZ) domain Containing 2; KIAA1489; Kelch Repeat And BTB domain-Containing Protein 2; Kelch Repeat And BTB domain Containing 2; BTB And Kelch domain Conta
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P701576
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KBTBD2; BTB And Kelch domain-Containing Protein 1; Prev. BKLHD1; DKFZP566C134; Kelch Repeat And BTB (POZ) domain Containing 2; KIAA1489; Kelch Repeat And BTB domain-Containing Protein 2; Kelch Repeat And BTB domain Containing 2; BTB And Kelch domain Conta
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P701574
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KBTBD11; Kelch Repeat And BTB (POZ) domain Containing 11; Kelch Repeat And BTB domain Containing 11; Chronic Myelogenous Leukemia-Associated Protein; KLHDC7C; Kelch domain-Containing Protein 7B; KIAA0711; CMLAP; Kelch Repeat And BTB domain-Containing Prot
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P701579
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KBTBD8; KIAA1842; Kelch Repeat And BTB domain Containing 8; Kelch Repeat And BTB domain-Containing Protein 8; TA-KRP; Kelch Repeat And BTB (POZ) domain Containing 8; T-Cell Activation Kelch Repeat Protein; TAKRP
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P701580
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KBTBD8; KIAA1842; Kelch Repeat And BTB domain Containing 8; Kelch Repeat And BTB domain-Containing Protein 8; TA-KRP; Kelch Repeat And BTB (POZ) domain Containing 8; T-Cell Activation Kelch Repeat Protein; TAKRP
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P701577
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: KBTBD6; Kelch Repeat And BTB (POZ) domain Containing 6; Kelch Repeat And BTB domain Containing 6; DKFZp547E1912; Kelch Repeat And BTB domain-Containing Protein 6; Alternative Protein KBTBD6
Species:
Human
Source:
Sf9 insect cells
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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
