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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
57 Results for "
IRAK4 degrader
" in MedChemExpress (MCE) Product Catalog:
Products (57)
57 Results for "IRAK4 degrader" in MCE Product Catalog:
13
13 Publications Verification
Synonyms: Dexamethasone 21-phosphate disodium
Research Areas:
Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease) .
13
13 Publications Verification
Synonyms: Dexamethasone 21-phosphate
Research Areas:
Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease) .
3
3 Cited Publications
Synonyms: KYM-001; PROTAC IRAK4 degrader-7
Research Areas:
KT-474 (KYM-001; PROTAC IRAK4 degrader-7) is an orally active PROTAC IRAK4 degrader with anti-tumor effects. KT-474 inhibits the cell cycle and induces apoptosis. KT-474 induces tumor regression in a xenograft model of MYD88-mutated ABC DLBCL .
3
3 Cited Publications
Cat. No.: HY-145483A
CAS No.: 2751703-31-6
Synonyms: KYM-001 hydrochloride; PROTAC IRAK4 degrader-7 hydrochloride
Research Areas:
KT-474 (KYM-001; PROTAC IRAK4 degrader-7) hydrochloride is an orally active PROTAC IRAK4 degrader with anti-tumor effects. KT-474 inhibits the cell cycle and induces apoptosis. KT-474 induces tumor regression in a xenograft model of MYD88-mutated ABC DLBCL .
1
Research Areas:
Zomiradomide (KT-413) is an orally active IRAK4 PROTAC degrader with a DC50 of 6 nM. Zomiradomide inhibits the NF-κB signaling pathway, while its molecular glue function mediates the degradation of Ikaros and Aiolos (with a DC50 of 1 nM for both), activates the IFN-I signaling pathway, and selectively degrades IMiD substrates. Zomiradomide inhibits cancer cell proliferation and tumor growth. Zomiradomide can be used in research related to B-cell non-Hodgkin's lymphoma and diffuse large B-cell lymphoma .
1
Cat. No.: HY-41547
CAS No.: 835616-60-9
Synonyms: Cereblon ligand 4; E3 ligase Ligand 4
Target:
Research Areas:
Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966) .
Research Areas:
PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau .
Cat. No.: HY-W087383
CAS No.: 835616-61-0
Target:
Research Areas:
Thalidomide 5-fluoride is a thalidomide-based Cereblon ligand used to recruit Cereblon protein. Thalidomide 5-fluoride can be linked to target protein ligands (e.g. IRAK4) through a linker to form PROTAC molecules (e.g. PROTAC IRAK4 degrader-1). PROTAC IRAK4 degrader-1 caused <20%, >20-50%, and >50% IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, respectively .
JNJ-1013 is a potent and selective IRAK1 PROTAC degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) (Pink: ligand for target protein (HY-138834); black: linker (HY-Y1760); Blue: E3 ligase ligand (HY-112078)) .
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 .
KTX-951 is an orally active PROTAC degrader of IRAK4 and IMiD (Ikaros/Aiolos) substrates (Kd = 3.5 nM). KTX-951 induces IRAK4 degradation, and the degradation efficiency is independent of IRAK4 binding affinity. The DC50 values of KTX-951 for IRAK4, Ikaros and Aiolos are 18 nM, 14 nM and 13 nM, respectively. The IC50 of KTX-951 against OCl-Ly10 CTG is 35 nM. KTX-951 exhibits antitumor activity .
Cat. No.: HY-175022
CAS No.: 2432992-21-5
Research Areas:
PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research . Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker
Cat. No.: HY-153673
CAS No.: 2911615-06-8
Research Areas:
PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC degrader that targets IRAK4 by recruiting cereblon. PROTAC IRAK4 degrader-8 inhibits IRAK4 kinase activity with an IC50 of 15.5 nM. PROTAC IRAK4 degrader-8 suppresses IL-6 production in immune cells. PROTAC IRAK4 degrader-8 can be used in the research of inflammatory diseases, immune diseases and cancers .
Cat. No.: HY-174455
CAS No.: 3065494-66-5
Target:
Research Areas:
APH02174 is an orally effective and selective IRAK4 PROTAC degrader with a DC50 of 4.01 nM in THP-1 cells. APH02174 inhibits LPS (HY-D1056)-induced IL-6 release by degrading IRAK4 and blocking TLR/IL-1R downstream signaling. APH02174 exhibits favorable anti-inflammatory activity in both Imiquimod (HY-B0180)-induced psoriasis-like skin inflammation and collagen-induced arthritis models. APH02174 is useful for research on inflammatory diseases such as psoriasis and rheumatoid arthritis .
Cat. No.: HY-175764
CAS No.: 3091132-73-6
Research Areas:
FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis .
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88 MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model .
Cat. No.: HY-135382
CAS No.: 2374122-27-5
Target:
Research Areas:
PROTAC IRAK4 degrader-2 is a PROTAC degrader targeting IRAK4. PROTAC IRAK4 degrader-2 induces proteasome-dependent degradation of IRAK4 by recruiting the VHL E3 ligase. PROTAC IRAK4 degrader-2 inhibits multiple cytokines in peripheral blood mononuclear cells. PROTAC IRAK4 degrader-2 can be used in the research of autoimmune diseases, inflammatory diseases and neoplastic diseases .
Cat. No.: HY-46871
CAS No.: 93004-48-9
Target:
Research Areas:
3,9-Dimethyl-3,9-diazaspiro[5.5]undecane is a rigid PROTAC linker can be used in the synthesis of PROTACs, such as FIP22 (HY-175764). FIP22 is a potent and selective IRAK4 PROTAC degrader with anti- atopic dermatitis activity .
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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
