Btk Degrader
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PROTAC DDa-1
0 ImagesCat. No.: HY-156745CAS No.: 3036944-98-3PROTAC DDa-1 is a multi-targeted DCAF1-recruiting tyrosine kinase PROTAC degrader. PROTAC DDa-1 mediates the degradation of TNK2, CSK, LIMK2, TEC, and BTK, with a DC50 of 90 nM for BTK. PROTAC DDa-1 reduces the viability of BTK-dependent diffuse large B-cell lymphoma cells. PROTAC DDa-1 can be used for the research of diffuse large B-cell lymphoma.
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PROTAC BTK Degrader-5
0 ImagesCat. No.: HY-155072CAS No.: 3049086-75-8PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research.
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BCPyr
0 ImagesCat. No.: HY-142621CAS No.: 2669844-82-8BCPyr is a PROTAC degrader targeting cIAP1 and BTK, with a Kd of 262 nM for human cIAP1, and Kd values of 262 nM and 692 nM for human BTK. BCPyr binds to the Bir3 domain of cIAP1, recruits BTK to cIAP1, and mediates the ubiquitination and degradation of BTK. BCPyr acts as a degrader, ternary complex stabilizer, cooperative binder, and higher-order assembly inducer. BCPyr can be used in studies related to leukemia and lymphoma.
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(R,R)-Bexobrutideg
0 ImagesSynonyms: (R,R)-NX-5948; (R,R)-BTK-IN-24(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker).
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PROTAC BTK Degrader-12
0 ImagesCat. No.: HY-170413CAS No.: 2736508-65-7PROTAC BTK Degrader-12 is a BTK PROTAC degrader that recruits CRBN, with a DC50 of 0.72 nM. PROTAC BTK Degrader-12 achieves ubiquitin-proteasome pathway degradation of BTK by conjugating a BTK inhibitor domain with an E3 ubiquitin ligase ligand domain. PROTAC BTK Degrader-12 can be used in cancer research.
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TQ-3959
0 ImagesCat. No.: HY-175541CAS No.: 2926610-43-5
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BTK ligand 1
0 ImagesCat. No.: HY-150885CAS No.: 330785-90-5BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting Btk can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies.
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PROTAC BTK/IKZF1/3 Degrader-1
0 ImagesCat. No.: HY-179077CAS No.: 2416130-49-7PROTAC BTK/IKZF1/3 Degrader-1 is an orally active PROTAC-IMiD bifunctional protein degrader that selectively degrades BTK, IKZF1 and IKZF3. PROTAC BTK/IKZF1/3 Degrader-1 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, mediating ubiquitination and proteasome-dependent degradation of target proteins, with no obvious degrading effect on GSPT1. PROTAC BTK/IKZF1/3 Degrader-1 inhibits cancer cell proliferation, induces cancer cell apoptosis, and suppresses tumor growth. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of diffuse large B-cell lymphoma.
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PROTAC BTK Degrader-4
0 ImagesCat. No.: HY-128408CAS No.: 2893795-12-3PROTAC BTK Degrader-4 (compound 15) is a potent PROTAC Bruton's tyrosine kinases (BTK) degrader (DC50 < 100 nM) with little immunomodulatory imide drug (IMiD) activity (DC50 = 0.345 μM, Dmax = 27.4%). PROTAC BTK Degrader-4 can be used for cancers, autoimmune diseases, and inflammatory diseases that are mediated by BTK.
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PROTAC BTK Degrader-3
0 ImagesCat. No.: HY-153536CAS No.: 2563861-90-3
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ISM-PR44
0 ImagesCat. No.: HY-189442ISM-PR44 is an orally active PROTAC degrader targeting BTK, with a DC50 of 0.05 nM in BTK-HiBiT Ramos cells. ISM-PR44 recruits CRBN E3 ligase to induce ubiquitination and proteasomal degradation of BTK. ISM-PR44 exhibits antiproliferative and cytotoxic activities in B-cell lymphoma cells. ISM-PR44 can be used for research on B-cell lymphoma.
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PROTAC BTK Degrader-9
0 ImagesCat. No.: HY-162280CAS No.: 3034024-77-3PROTAC BTK Degrader-9 is a potent BTK PROTAC degrader with a DC50 of 1.29 nM (in Mino cells at 4 h). PROTAC BTK Degrader-9 induces the formation of a stable ternary complex with BTK and the CRBN E3 ubiquitin ligase, thereby mediating proteasomal degradation of BTK in a CRBN-dependent manner. PROTAC BTK Degrader-9 downregulates the RANKL-activated BTK-PLCγ2-Ca2+-NFATc1 signaling pathway. PROTAC BTK Degrader-9 alleviates alveolar bone resorption in periodontitis models of Mus musculus (house mouse). PROTAC BTK Degrader-9 can be used in research related to periodontitis.
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PROTAC BTK Degrader-13
0 ImagesCat. No.: HY-168963PROTAC BTK Degrader-13 is a reagent targeting BTK, with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 degrades BTK in a proteasome-dependent manner and inhibits BTK-mediated downstream signaling pathways by reducing the phosphorylation levels of BTK and p38 MAPK. PROTAC BTK Degrader-13 exerts selective cytotoxic effects on BTK-overexpressing lymphoma cells and ITK-positive cells. PROTAC BTK Degrader-13 can be used in studies related to B-cell lymphoma.
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