Estrogen Receptor/ERR Degrader

Estrogen Receptor/ERR Degraders (46):

Cat. No.	Product Name	Effect	Purity

HY-12870

AZD9496	Degrader	99.28%
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC₅₀ of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).

HY-145572

Imlunestrant	Degrader	98.02%
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).

HY-133017

Amcenestrant	Degrader	99.79%
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC₅₀ of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER⁺ breast cancer.

HY-136242

UT-34	Degrader	98.09%
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

HY-111486

LSZ-102	Degrader	99.94%
LSZ-102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with an IC₅₀ value of 0.2 nM.

HY-149295

PROTAC ERα Degrader-4	Degrader	99.06%
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (K_i: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER⁺ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

HY-111846

PROTAC ERα Degrader-2	Degrader	98.92%
PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)).

HY-149480

ERD-3111	Degrader	98.72%
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC₅₀: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer.

HY-141551

GNE-274	Degrader	98.00%
GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.

HY-147402A

Taragarestrant meglumine	Degrader	99.33%
Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models.

HY-145572A

Imlunestrant tosylate	Degrader	98.54%
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).

HY-125263

OP-1074	Degrader	99.77%
OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC₅₀ values of 1.6 and 3.2 nM, respectively.

HY-157765

PROTAC ERα Degrader-6	Degrader
PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC₅₀ of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation.

HY-161740

PHTPP-1304	Degrader	99.96%
PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC₅₀ ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ.

HY-101119

GLL398	Degrader
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC₅₀ value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC₅₀=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.

HY-111484A

GDC-0927 Racemate	Degrader
GDC-0927 Racemate (SRN-927 Racemate) is an estrogen receptor (ER) degrader that can effectively inhibit the activity of ER-α with an IC₅₀ value of 0.2 nM and can be used in diseases related to estrogen receptors.

HY-147402

Taragarestrant	Degrader
Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models.

HY-175260

ZN-c5	Degrader
ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC₅₀ = 0.3 nM) and binds with high affinity to ERα and ERβ (IC₅₀ = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer.

HY-174131

PVTX-321	Degrader
PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC₅₀=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC₅₀=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer.

HY-161692

ERα degrader 8	Degrader
ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC₅₀ value of 0.15 μM.

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