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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
16 Results for "
Degron
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "Degron" in MCE Product Catalog:
61
61 Cited Publications
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5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression .
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MRT-2359 is an orally active and selective GSPT1 molecular glue degrader, with a DC50 of 5 nM. MRT-2359 induces CRBN/GSPT1 ternary complex formation to drive CRBN- and degron-dependent proteasomal GSPT1 degradation, with selectivity for wild-type GSPT1 over the GSPT1G575N mutant. MRT-2359 disrupts protein translation, induces ribosome stalling, downregulates MYC family proteins and their transcriptional output, reduces proliferation, and induces apoptosis in cancer cells. MRT-2359 can be used for the research of non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), neuroendocrine lung cancer, high grade neuroendocrine cancers, diffuse large B-cell lymphoma, prostate cancer, and MYC-driven solid tumors .
Cat. No.: HY-160695
CAS No.: 2924858-25-1
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PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms .
Cat. No.: HY-172162
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LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia .
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CC-3060 is a molecular glue modulator targeting Cereblon (CRBN) E3 ubiquitin ligase and ZBTB16 degrader with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 engages structural degrons on ZBTB16’s ZnF1 or ZnF3 domains for fusion protein substrates. CC-3060 can be used for the research of acute promyelocytic leukemia .
Cat. No.: HY-173614
CAS No.: 1061605-35-3
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CC-647 is a molecular glue-type cereblon modulator and ZBTB16 degrader. CC-647 primarily utilizes the C2H2 ZnF3 degron of ZBTB16 to promote CRL4 CRBN-mediated ubiquitination and proteasomal degradation. CC-647 also induces the degradation of the oncogenic RARα-ZBTB16 fusion protein, while exerting a weaker degrading effect on the reciprocal fusion ZBTB16-RARα. CC-647 can be used in studies related to targeted protein degradation and ZBTB16/RARA-rearranged acute promyelocytic leukemia .
Cat. No.: HY-168535
CAS No.: 1010913-79-7
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SJ6145 is a potent ligand for KLHDC2 SBD, with the Kd of 16.9 μM in SPR test, IC50 value of 42 μM in inhibiting KLHDC2 SBD binding to a di-Gly degron peptide test .
Cat. No.: HY-P10360
CAS No.: 2816095-52-8
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Cat. No.: HY-175280
CAS No.: 3095033-62-5
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Lck degrader-1 is a molecular glue degrader that recruits cereblon to target LCK and CK1α. Lck degrader-1 promotes the formation of the LCK/CRBN-DDB1 ternary complex with an EC50 of 77.1 nM, and induces the degradation of LCK and CK1α. LCK degradation induced by Lck degrader-1 depends on the G415-containing helical G-loop degron, and maintains LCK-degrading activity in cells with the LCK T316I gatekeeper mutation. Lck degrader-1 can be used for research related to T-cell acute lymphoblastic leukemia (T-ALL) and LCK inhibitor resistance .
Cat. No.: HY-D2259
CAS No.: 2910938-58-6
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PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .
Cat. No.: HY-P5559
CAS No.: 2582803-80-1
Cat. No.: HY-144314
CAS No.: 2906869-08-5
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PSDalpha is a photoactivatable PS-Degron targeting estrogen receptor α (ERα/ESR1), with a Ki of 72.8 nM for ERα. PSDalpha consists of an ERα-targeting estradiol moiety conjugated via an alkyne bond to triphenylamine-benzothiadiazole (TB), an aggregation-induced emission (AIE) photosensitizer. Upon visible light irradiation, PSDalpha generates singlet oxygen ( 1O2) and induces controllable ERα degradation. PSDalpha also induces G1 phase arrest and apoptosis. PSDalpha can be used in studies related to ERα-positive breast cancer and light-controlled targeted protein degradation .
Cat. No.: HY-134653R
CAS No.: 168649-23-8
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5-Ph-IAA (Standard) is the analytical standard of 5-Ph-IAA (HY-134653). This product is intended for research and analytical applications. 5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression .
Cat. No.: HY-189230
CAS No.: 3108114-67-3
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NEP48 is a small-molecule antagonist targeting the ZER1 (E3 ubiquitin ligase)-E7 oncogenic axis. NEP48 binds to the MHGD/N-degron binding pocket within the ARM repeat domain of ZER1, competitively blocking E7-ZER1 binding and ZER1-mediated substrate degradation. NEP48 disrupts the ZER1-E7 interaction, leading to Rb stabilization and silencing of E2F-driven transcriptional programs. NEP48 inhibits the proliferation of HPV-positive cancer cells and can be used for research on HPV-positive cervical cancer .
Cat. No.: HY-187168
CAS No.: 2407654-72-0
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KAT2A degrader-1 is a molecular glue degrader targeting KAT2A, with a DC50 of 89 nM in Kelly cells. KAT2A degrader-1 recruits KAT2A to cereblon (CRBN) in a degron-independent manner, forms a ternary complex with KAT2A and CRBN, and drives the polyubiquitination and proteasome-dependent degradation of KAT2A. KAT2A degrader-1 reduces the level of histone H3 lysine 9 acetylation (H3K9Ac). KAT2A degrader-1 induces antiproliferative effects in acute myeloid leukemia cells, while enhancing KAT2A-CRBN dimerization activity and eliminating the targeting effect on GSPT1. KAT2A degrader-1 can be used for research related to acute myeloid leukemia .
Cat. No.: HY-180989
Domaines de recherche:
PROTAC PLK1 Degrader-2 is a peptide-based N-end rule PLK1 mini-PROTAC. PROTAC PLK1 Degrader-2 utilizes Arg12 as dual-function cell-permeable N-degron to recruit UBR1/UBR2 E3 ligases, mediates PLK1 ubiquitination and proteasome-dependent degradation. PROTAC PLK1 Degrader-2 suppresses cervical cancer cell proliferation, induces G2/M cell cycle arrest and tumor cell apoptosis, and exerts potent in vivo anti-tumor efficacy in mice and can be applied to research on PLK1-driven cervical carcinoma (PLK1 ligand: POI ligand-3 (HY-180990); E3 ligase ligand: Arg12 (HY-P11631); PROTAC linker: 6-Aminocaproic acid (HY-B0236)) .
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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
