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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
24 Results for "
induced proximity
" in MedChemExpress (MCE) Product Catalog:
Products (24)
24 Results for "induced proximity" in MCE Product Catalog:
Cat. No.: HY-176521
CAS No.: 3083307-42-7
Research Areas:
AR/BRD4 RIPTAC-1 (Compound II-5) is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 holds promise for use in prostate cancer research .
Cat. No.: HY-175452
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MRT-3486 is a molecular glue degrader.MRT-3486 induces ternary complex formation between CRBN and predicted β-hairpin G-loop proteins.MRT-3486 is selected from an internal compound library for proximity-ligation experiments .
Cat. No.: HY-156820
CAS No.: 3077339-82-0
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HLDA-221 is a non-covalent regulated induced proximity targeting chimeras (RIPTAC). The binding of HLDA-221 to BRD4-BD1 is significantly increased after pre-incubation with FKBP. HLDA-221 can be used in cancer research .
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TL13-12 is a CRBN-recruiting ALK PROTAC degrader, with a DC50 of 10 nM in H3122 cells. TL13-12 induces dimerization of CRBN and truncated ALK, which brings the DNA-binding domain and transactivation domain into close proximity, thereby activating the expression of downstream reporter genes, while exhibiting extremely low leaky expression under non-inducing conditions. TL13-12 serves as a tool molecule for the orthogonal PROTAC-CID system, and is applied in research on non-small cell lung cancer, anaplastic large cell lymphoma, and neuroblastoma .
Cat. No.: HY-151071
CAS No.: 2488761-18-6
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TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs) .
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β-NF-JQ1 is a BRD2/3/4 PROTAC degrader. β-NF-JQ1 recruits the AhR E3 ligase complex to BRD2, BRD3 and BRD4, induces AhR-BRD interaction, and mediates AhR-dependent degradation through the proximity effect between the target protein and AhR. β-NF-JQ1 acts as an antiproliferative and cytotoxic agent that induces anticancer activity associated with BRD protein knockdown. β-NF-JQ1 can be used for research on breast cancer and neuroblastoma .
Cat. No.: HY-161794A
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SP3N hydrochloride is a specific degrader of the prolyl isomerase FKBP12. As a prodrug, SP3N hydrochloride is metabolized by Diamine oxidase into the active aldehyde metabolite SP3CHO (HY-161795). SP3N hydrochloride induces the proximity of FKBP12 to the SCF FBXO22 E3 ligase complex, thereby triggering the polyubiquitination and proteasomal degradation of FKBP12. SP3N hydrochloride can be used in cancer research .
Cat. No.: HY-175463
CAS No.: 3095032-50-8
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LCK degrader-2 is a selective CRBN-dependent molecular glue degrader targeting LCK. LCK degrader-2 induces the proximity effect between LCK and CRBN, stabilizes the CRBN-LCK ternary complex, and triggers the ubiquitination and degradation of LCK. LCK degrader-2 can be used for the research of acute lymphoblastic leukemia .
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HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA) .
Cat. No.: HY-164098
CAS No.: 3008612-30-1
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JWZ-7-7-Neg1 is a transcriptional chemical inducers of proximity (TCIP) with negative chemical control. JWZ-7-7-Neg1 reduces the ability to bind to BRD4 or BCL6, so it has less cytotoxicity to DLBCL cells, in compared with JWZ-7-7 .
Cat. No.: HY-161794
Target:
Research Areas:
SP3N is a specific degrader of the prolyl isomerase FKBP12. As a prodrug, SP3N is metabolized by Diamine oxidase into the active aldehyde metabolite SP3CHO (HY-161795). SP3N induces the proximity of FKBP12 to the SCF FBXO22 E3 ligase complex, thereby triggering the polyubiquitination and proteasomal degradation of FKBP12. SP3N can be used in cancer research .
Cat. No.: HY-176521A
Research Areas:
AR/BRD4 RIPTAC-1 (Compound II-5) TFA is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 TFA induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 TFA inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 TFA holds promise for use in prostate cancer research .
Cat. No.: HY-159110
CAS No.: 1947375-16-7
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ABA-DMNB is a photo-caged chemically induced proximity (CIP) inducer. ABA-DMNB is a photo-caged ABA (Abscisic acid (HY-100560)). ABA-DMNB can be uncaged under light irradiation and generate active ABA .
Cat. No.: HY-158905
CAS No.: 2923694-73-7
Synonyms: MTDB-Alk
Target:
MTDB-Alkyne (MTDB-Alk) is a β-coronavirus pseudoknot RNA-binding ligand that binds to the β-coronavirus pseudoknot RNA structure on the SARS-CoV-2 genome. MTDB-Alkyne can be used to synthesize Proximity-Induced Nucleic Acid Degrader (PINAD) for degrading SARS-CoV-2 RNA. MTDB-Alkyne is applicable to research related to the development of SARS-CoV-2-targeted RNA probes .
Cat. No.: HY-132862
CAS No.: 2711006-74-3
ZXH-4-137 is a CRBN PROTAC degrader. ZXH-4-137 brings CRBN and VHL E3 ligase into proximity, induces CRBN ubiquitination and proteasomal degradation, and exhibits high selectivity for CRBN. ZXH-4-137 blocks the degradation of CRBN-dependent target proteins such as GSPT1 and CDK9. ZXH-4-137 serves as a chemical knockdown tool compound for investigating CRBN-dependent biological processes .
Cat. No.: HY-D2477
CAS No.: 1974271-78-7
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Sulfo-QSY21-NHS is an N-hydroxysuccinimide ester derivative fluorescent quencher that reduces the fluorescence intensity of paired fluorophores via proximity effect and relieves quenching after linker extension induced by mechanical force. Sulfo-QSY21-NHS can label streptavidin through NHS ester bioconjugation and be integrated into fluorescence-based molecular tension sensors to map the mechanical forces of cell surface receptors. Sulfo-QSY21-NHS also serves as a quencher for cysteine cathepsin-targeted quenched fluorescent substrate probes, and is widely used in studies related to breast cancer, colorectal cancer and lung adenocarcinoma .
Cat. No.: HY-186126
CAS No.: 3066623-95-5
CDK2 modulator 1 is a CDK2 modulator with an EC50 < 100 nM and an Emax > 100% of positive control in a TR-FRET proximity assay. CDK2 modulator 1 induces ternary complex formation with CDK2/CCNE1 and CRBN. CDK2 modulator 1 can be used for the research of cancer .
Cat. No.: HY-183988
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OICR409946 is a self-dimerization-induced proximity-targeting chimera (SDIPTAC) targeting DCAF1, with a Kd value of 6200 nM. OICR409946 binds to DCAF1, induces head-to-tail homodimerization, sterically blocks the Vpr binding interface, prevents the recruitment of Vpr to the CRL4DCAF1 complex, and inhibits Vpr-dependent HIV replication. OICR409946 can be used in studies related to HIV infection (DCAF1 ligand: (HY-169390); Linker: (HY-130659)) .
Cat. No.: HY-188123
NAMPT ligand-1 is a ligand targeting NAMPT, consisting of a NAMPT-binding domain, a linker, and a maleimide-fused enediyne warhead with a cyclopropane-modified alkyne terminus. NAMPT ligand-1 can be used to synthesize PROTEC NAMPT Degrader-1 (HY-189001). NAMPT ligand-1 induces the degradation of NAMPT via proximity-induced radical oxidation, and this process is independent of endogenous proteolytic mechanisms. NAMPT ligand-1 can be used in ovarian cancer research .
Cat. No.: HY-189495
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CRBN ligand-911 is an E3 ligase ligand that targets CRBN. CRBN ligand-911 forms a stable ternary complex with CRBN to enable proximity-induced co-binding and ubiquitination of LIMK2. CRBN ligand-911 binds directly to CRBN. CRBN ligand-911 is used for the synthesis of the LIMK2-targeting PROTAC degrader THNAN69 (HY-178122) .
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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
