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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
30 Results for "
Heterobifunctional Degrader
" in MedChemExpress (MCE) Product Catalog:
Products (30)
30 Results for "Heterobifunctional Degrader" in MCE Product Catalog:
11
11 Publications Verification
Research Areas:
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression .
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6 Cited Publications
Synonyms: ARV-471; PF-07850327
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Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
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BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .
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1 Cited Publications
dTAG-47 is a heterobifunctional PROTAC degrader that specifically binds to the FKBP12 F36V domain and Cereblon (CRBN). By recruiting the CRBN E3 ubiquitin ligase, dTAG-47 induces ubiquitination and proteasomal degradation of FKBP12 F36V-fused Cas9 and tagged KDM5A. dTAG-47 can induce upregulated expression of some endogenous retrovirus (ERV) genes and is suitable for cancer research .
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CBP/p300 ligand 2 is a ligand for target protein for PROTAC of dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP .
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dTAGV-1-NEG is an inactive FKBP12 F36V PROTAC degrader, the diastereomer of dTAGV-1 (HY-145514D), and a heterobifunctional negative control molecule. dTAGV-1-NEG does not degrade any protein .
Cat. No.: HY-161157
CAS No.: 2451573-90-1
dTAG-13-NEG is a negative control of dTAG-13 (HY-114421). dTAG-13, a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 F36V with expression of FKBP12F36V in-frame with a protein of interest .
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Thalidomide-NH-PEG4-COOH is an E3 ligase ligand-linker conjugate which can be used for synthesizing dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP .
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Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1 (HY-134582). dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP .
Cat. No.: HY-122653A
Purity: 98.02%
CCT367766 formic is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 formic exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 formic reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein .
Cat. No.: HY-161130
CAS No.: 2624336-87-2
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Lenalidomide 4'-PEG3-amine dihydrochloride is a lenalidomide (HY-A0003)-derived immunomodulator and monofunctional synthetic intermediate, as well as a E3 ubiquitin ligase ligand. Lenalidomide 4'-PEG3-amine dihydrochloride can be used for the preparation of small-molecule drug conjugates and heterobifunctional protein degraders .
Cat. No.: HY-138642S
CAS No.: 3025452-07-4
Synonyms: ARV-471-d5 PF-07850327-d5
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Vepdegestrant-d5 (ARV-471-d5) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC50 of about 2 nM .
Cat. No.: HY-175417
VHL-SNAP2-5C is a PROTAC degrader targeting SNAP fusion proteins, with an IC50 of 0.33 μM for binding to VHL. VHL-SNAP2-5C covalently binds to the SNAP-tag target at one end and recruits the VHL ubiquitin E3 ligase at the other end to form a ternary complex, thereby inducing proteasome-dependent ubiquitination and degradation of SNAP fusion proteins through its heterobifunctional structure. VHL-SNAP2-5C can be used in studies of protein homeostasis and degradation mechanisms .
Cat. No.: HY-176130
CAS No.: 3115333-82-6
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MRL828 is a heterobifunctional molecule that targets aggregated tau protein. As an autophagy-targeting chimera (ATTEC), MRL828 selectively labels aggregated tau protein for clearance via the autophagy (autophagy)-lysosome pathway. The activity of MRL828 depends on autophagosomes rather than lysosomes, and it induces autophagosome-dependent secretion. MRL828 acts as an intracellular aggregate inhibitor and a secretory autophagy inducer, reducing intracellular levels of aggregated tau protein through autophagosome-dependent secretory autophagy instead of lysosomal degradation. MRL828 can be used in the research of neurodegenerative diseases such as Alzheimer's disease .
Cat. No.: HY-139996
CAS No.: 2732969-67-2
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Pomalidomide-C5-Dovitinib is a heterobifunctional PROTAC that recruits KEAP1 E3 ligase to degrade BRD4 and BRD3, but not BRD2 .
Cat. No.: HY-168487
CAS No.: 2737222-94-3
PROTAC WDR5 degrader 1 is a heterobifunctional WDR5 PROTAC degrader with a DC50 value of 53 nM and a Kd value of 18 nM, exhibiting selective WDR5 degradation activity and cell permeability. PROTAC WDR5 degrader 1 induces proliferation defects in leukemia cells, with enhanced efficacy in cells overexpressing VHL. PROTAC WDR5 degrader 1 is applicable to research related to acute myeloid leukemia .
Cat. No.: HY-162835
CAS No.: 2409844-88-6
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PROTAC SMARCA2/4 degrader-28 is a heterobifunctional PROTAC degrader targeting SMARCA2 and SMARCA4. PROTAC SMARCA2/4 degrader-28 forms a ternary complex with CRL2VHL E3 ligase and SMARCA2 or SMARCA4, mediating the ubiquitination and degradation of SMARCA2, while acting as a partial degrader of SMARCA4. PROTAC SMARCA2/4-degrader-28 can be used in cancer-related research .
Cat. No.: HY-145514B
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dTAGV-1-NEG TFA is an inactive FKBP12 F36V PROTAC degrader, the diastereomer of dTAGV-1 (HY-145514D), and a heterobifunctional negative control molecule. dTAGV-1-NEG TFA does not degrade any protein .
Cat. No.: HY-138642A
CAS No.: 2229711-08-2
Synonyms: (Rac)-ARV-471; (Rac)-PF-07850327
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(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
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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
