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Heterobifunctional Degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Androgen Receptor (1) Apoptosis (2) Autophagy (1) CDK (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (4) Estrogen Receptor/ERR (2) FKBP (5) Isotope-Labeled Compounds (1) Ligands for Target Protein for PROTAC (2) PI3K (1) PROTAC Linkers (1) PROTACs (19) RET (1) Tau Protein (1)
By Research Areas:	Cancer (22) Neurological Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-134592

Piperidine-GNE-049-N-Boc	Ligands for Target Protein for PROTAC	Cancer
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 .

HY-134582

dCBP-1 5 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
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 .

HY-145514A

dTAGV-1-NEG	PROTACs FKBP	Cancer
dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12 ^F36V-selective degrader .

HY-161157

dTAG-13-NEG	PROTACs	Cancer
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 .

HY-138539

CBP/p300 ligand 2	Ligands for Target Protein for PROTAC	Cancer
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 .

HY-138642

Vepdegestrant 3 Publications Verification ARV-471	PROTACs Estrogen Receptor/ERR	Cancer
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 .

HY-114421

FKBP12 PROTAC dTAG-13 Maximum Cited Publications 7 Publications Verification dTAG-13	PROTACs FKBP	Cancer
FKBP12 PROTAC dTAG-13 (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. FKBP12 PROTAC dTAG-13 effectively engages FKBP12 ^F36V and CRBN, thereby selectively degrading FKBP12 ^F36V .

HY-161157A

dTAG-13-NEG TFA	PROTACs	Cancer
dTAG-13-NEG TFA 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 .

HY-145514B

dTAGV-1-NEG TFA	PROTACs FKBP	Cancer
dTAGV-1-NEG TFA is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1-NEG TFA is an FKBP12 ^F36V-selective degrader .

HY-138642A

(Rac)-Vepdegestrant (Rac)-ARV-471	Estrogen Receptor/ERR PROTACs	Cancer
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) 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 .

HY-158101

BMS-986365 CC-94676	PROTACs Androgen Receptor	Cancer
BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader, 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 significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. (Blue: HY-W247437; Black: linker (HY-W126831); Pink: HY-168697) .

HY-W190796A

Mal-PEG3-NH2 TFA	PROTAC Linkers	Cancer
Mal-PEG3-NH2 TFA is a linear heterobifunctional PEG crosslinker with Maleimide (HY-W007324) and amine. Mal-PEG3-NH2 TFA is a non-degradable (non-cleavable) PROTAC linker .

HY-134591

Thalidomide-NH-PEG4-COOH	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
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 .

HY-168664

CPD-39	PROTACs CDK	Cancer
CPD-39 is a potent and orally active CCND1 and CDK4 heterobifunctional PROTAC degrader. CPD-39 shows anti-proliferation. (Pink: ligand for target protein (HY-50767); black: linker (HY-20240); Blue: E3 ligase ligand (HY-168667)) .

HY-138642S

Vepdegestrant-d5 ARV-471-d₅	Isotope-Labeled Compounds	Cancer
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 .

HY-147098

dTAG-47	PROTACs FKBP	Cancer
dTAG-47 is a FKBP12F36V PROTAC degrader. dTAG-47 efficiently degrades FKBP12F36V-MELK(sg3R) in MELK ^⁻/⁻ MDA-MB-468-FKBP12F36V-MELK(sg3R) cells. dTAG-47 can be used for the research of basal-like breast cancers (BBC). (Pink: FKBP12F36V ligand (HY-114420), Blue: CRBN Ligand (HY-W087383), Black: Linker (HY-42773), E3 ligase ligand-linker conjugate (HY-175952)) .

HY-123941

FKBP12 PROTAC dTAG-7 3 Publications Verification dTAG-7	PROTACs FKBP Epigenetic Reader Domain	Others
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional PROTAC degrader. FKBP12 PROTAC dTAG-7 targets FKBP12 ^F36V and BET BRD4. FKBP12 PROTAC dTAG-7 enables rapid and selective degradation of target proteins, and is suitable for cellular and in vivo studies to analyze protein functions and validate targets . (Pink: target protein ligand (HY-114420); Black: linker (HY-128844); Blue: CRBN Ligand (HY-103597); CRBN Ligand+linker: (HY-W722323))

HY-178964

PROTAC RET Degrader 1	PROTACs RET	Cancer
PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC₅₀ values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .

HY-122653

CCT367766	PROTACs	Cancer
CCT367766 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 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC₅₀ value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with K_d values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein .

HY-163677

ARM165	PROTACs PI3K Akt	Cancer
ARM165 is a heterobifunctional molecule. ARM165 degrades the PIK3CG proteins, inhibits PI3Kγ-Akt signaling pathway, and thus exhibits antileukemia efficacy. ARM165 inhibits proliferations of AML cells, with IC₅₀ <1 μM. (Pink: ligand for target protein PI3Kγ inhibitor AZ2 (HY-111570); Black: linker; Blue: ligand for E3 ligase Pomalidomide (HY-10984))

HY-122653A

CCT367766 formic	PROTACs	Cancer
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 K_d values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein .

HY-134850

QC-01–175	PROTACs Tau Protein	Neurological Disease
QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau. QC-01-175 reduces the levels of A152T and P301L mutant tau protein and protects neurons from tau-mediated toxicity and improve cell survival (Pink: ligand for target protein Aberrant tau ligand 1 (HY-W453397); Black: linker NH2-PEG3 (HY-W007545); Blue: ligand for E3 ligase Pomalidomide (HY-10984)) .

HY-161769

HL435	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC₅₀ of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))

HY-145925B

CFT8634 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor) .

Cat. No.	Product Name	Chemical Structure

HY-138642S

Vepdegestrant-d5
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 .

Vepdegestrant-d5

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 .

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