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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
33 Results for "
TMD8
" in MedChemExpress (MCE) Product Catalog:
Products (33)
33 Results for "TMD8" in MCE Product Catalog:
3
3 Cited Publications
Synonyms: NX-5948; BTK-IN-24
Research Areas:
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTK C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies .
Cat. No.: HY-P99349
CAS No.: 1879918-31-6
Synonyms: Loncastuximab tesirine-lpyl; ADCT-402
Research Areas:
NRX-0492 is an orally active BTK PROTAC degrader, with a binding IC50 of 1.2 nM for both wild-type BTK and BTK T474I, and 2.7 nM for BTK C481S, and exhibits cellular DC50 values of 0.1 nM and 0.2 nM against wild-type BTK and BTK C481S, respectively. NRX-0492 catalyzes the ubiquitination and proteasomal degradation of wild-type and drug-resistant mutant BTK by recruiting the CRBN E3 ubiquitin ligase complex. NRX-0492 inhibits the BCR signaling pathway and its downstream NF-κB/MYC transcriptional program, achieves rapid and sustained degradation in primary CLL cells, and exhibits extremely low cytotoxicity. NRX-0492 degrades BTK, inhibits tumor cell proliferation and activation, and significantly suppresses tumor growth in xenograft models. NRX-0492 can be used in research related to chronic lymphocytic leukemia and diffuse large B-cell lymphoma .
Cat. No.: HY-160142
CAS No.: 2884554-45-2
UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .
Cat. No.: HY-157763
Target:
Research Areas:
Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 is a cleavable linker-payload conjugate and cereblon-binding BTK bifunctional degrader. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 induces BTK degradation and exerts cytotoxic effects when delivered via CD79b monoclonal antibody. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1, when formulated as a CD79b antibody-drug conjugate, achieves sustained in vivo BTK degradation in tumor-bearing mice with reduced systemic payload exposure. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ADC linker: (HY-130944); PROTAC: (HY-163295)) .
KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .
Cat. No.: HY-174850
CAS No.: 2941611-57-8
CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27 nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
PROTAC BTK Degrader-1 is a selective, orally active BTK PROTAC degrader with a DC50 of 5.8 nM. PROTAC BTK Degrader-1 induces ubiquitination and degradation of wild-type and mutant (C481S, T316) BTK proteins via the CRBN-mediated pathway. PROTAC BTK Degrader-1 exhibits anticancer activity against diffuse large B-cell lymphoma. PROTAC BTK Degrader-1 can be used in lymphoma-related research .
Research Areas:
PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease .
Cat. No.: HY-175541
CAS No.: 2926610-43-5
TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma .
Cat. No.: HY-163295
CAS No.: 2377645-56-0
Target:
Research Areas:
BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect .
Cat. No.: HY-153220A
CAS No.: 3024312-52-2
Synonyms: (R)-NX-2127
Research Areas:
(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTK C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies .
Cat. No.: HY-177750
CAS No.: 2417647-40-4
Target:
Research Areas:
TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .
Cat. No.: HY-172217
CAS No.: 2982511-19-1
Target:
Research Areas:
DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
Cat. No.: HY-156746
DBt-10 is a PROTAC degrader that targets and degrades BTK by recruiting DCAF1. It degrades BTK in TMD8 BTK-GFP/mCherry cells with a DC50 of 137 nM. DBt-10 induces CRL4 DCAF1-dependent ubiquitination and proteasomal degradation of BTK, and retains BTK-degrading and antiproliferative activities in TMD8 cells that are resistant to CRBN-BTK PROTACs due to loss of CRBN expression. DBt-10 has a high survival window and exhibits extremely weak apoptosis-inducing effects on lymphoma cells. DBt-10 can be used for research on diffuse large B-cell lymphoma .
Cat. No.: HY-150593
CAS No.: 1812188-83-2
IRAK4-IN-16 (compound 4) is a potent IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor, with an IC50 of 2.5 nM. IRAK4-IN-16 shows cytotoxicity activity against OCI-LY10, TMD8, Ramos and HT cells, with IC50 values of 0.2, 0.2, 0.6, and 2.7 μM, respectively .
Cat. No.: HY-174129
CAS No.: 2649008-95-5
TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTK WT), >40,000 nM (BTK C481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis .
Cat. No.: HY-173143
BTK-IN-42 (Compound 11a) is a Btk inhibitor. BTK-IN-42 can effectively inhibit the growth and migration of tumor cells TMD8, with IC50 values of 2.61 and 5.34 μM for TMD8 and T9 cells respectively. It shows promise for research in the field of anti-cancer .
Cat. No.: HY-153321A
CAS No.: 2649400-33-7
Synonyms: (R,R)-NX-5948; (R,R)-BTK-IN-24
Target:
Research Areas:
(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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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
