Search Result

Results for "

Orally bioavailable degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (3) Apoptosis (1) CDK (2) Cholinesterase (ChE) (1) Environmental Pollutants (3) Epigenetic Reader Domain (2) Estrogen Receptor/ERR (7) Herbicide (3) IAP (1) Isotope-Labeled Compounds (1) MAP4K (1) PD-1/PD-L1 (1) Phosphodiesterase (PDE) (1) PROTACs (9) Reference Standards (1) RET (1) STING (1)
By Research Areas:	Cancer (18) Neurological Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-163410

AU-24118 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .

HY-12864

Brilanestrant 5+ Cited Publications ARN-810; GDC-0810	Estrogen Receptor/ERR	Cancer
Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable *selective estrogen receptor degrader* (SERD) with IC₅₀** of 0.7 nM.

HY-13208

Xevinapant hydrochloride 10+ Cited Publications AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride	IAP Apoptosis	Cancer
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with K_is of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .

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) .

HY-168162

ZLC491	PROTACs CDK	Cancer
ZLC491 is an orally active PROTAC degrader that selectively targets CDK12/CDK13 and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of CDK12 and CDK13. ZLC491 inhibits the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer .

HY-156751A

GDC-2992 RO7656594	PROTACs Androgen Receptor	Cancer
GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC₅₀ value of 2.7 nM and inhibits proliferation with an IC₅₀ valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study. (Structure Note: Pink: target protein ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189A); Black: linker (HY-169975); E3 ligase ligand +linker (HY-169976A)) .

HY-111486

LSZ-102 1 Publications Verification	Estrogen Receptor/ERR	Cancer
LSZ-102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with an IC₅₀ value of 0.2 nM.

HY-145479

PROTAC AR-V7 degrader-1 1 Publications Verification	PROTACs Androgen Receptor	Cancer
PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC₅₀ of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer .(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))

HY-132292

ARD-2128	PROTACs Androgen Receptor	Cancer
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .

HY-168518

PROTAC CDK9 degrader-9	PROTACs CDK	Cancer
PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research .

HY-145341

GNE-149	Estrogen Receptor/ERR	Cancer
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC₅₀=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .

HY-12870A

AZD9496 maleate Maximum Cited Publications 28 Publications Verification	Estrogen Receptor/ERR	Cancer
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC₅₀ of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

HY-B1849

Hexazinone	Environmental Pollutants Herbicide	Others
Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .

HY-B1849R

Hexazinone (Standard)	Reference Standards Environmental Pollutants Herbicide	Others
Hexazinone (Standard) is the analytical standard of Hexazinone. This product is intended for research and analytical applications. Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .

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-146267

ERα degrader 5	Estrogen Receptor/ERR	Cancer
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC₅₀ of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .

HY-B1849S

Hexazinone-d6	Isotope-Labeled Compounds Environmental Pollutants Herbicide	Others
Hexazinone-d₆ is the deuterium labeled Hexazinone. Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .

HY-101119

GLL398	Estrogen Receptor/ERR	Cancer
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-114770

(E,E)-GLL398	Estrogen Receptor/ERR	Cancer
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC₅₀ = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC₅₀ = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .

HY-162816

PROTAC HPK1 Degrader-3	PROTACs MAP4K	Cancer
PROTAC HPK1 Degrader-3 (compound C3) is an orally effective PROTAC targeting HPK1 (DC₅₀=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC HPK1 Degrader-3 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC HPK1 Degrader-3 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC HPK1 Degrader-3 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841) ^{[1] ^.}

HY-14795

Mimopezil ZT-1	Cholinesterase (ChE)	Neurological Disease
Mimopezil (ZT-1) is an cholinesterase (ChE) inhibitor that rapidly degrades into the active metabolite Huperzine A (HY-17388) in water or aqueous organic solvents. After oral administration, Mimopezil is rapidly absorbed but has low bioavailability (0.37%) in rats. However, after metabolism, it is converted into Huperzine A, which accumulates in the blood and exhibits strong activity. Following intravenous administration, Mimopezil reaches higher blood concentrations and is also rapidly metabolized into Huperzine A .

HY-168491

Enpp-1-IN-25	Phosphodiesterase (PDE) STING PD-1/PD-L1	Cancer
Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC₅₀ of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy .

Cat. No.	Product Name	Chemical Structure

HY-B1849S

Hexazinone-d6
Hexazinone-d₆ is the deuterium labeled Hexazinone. Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .

Hexazinone-d6

Hexazinone-d₆ is the deuterium labeled Hexazinone. Hexazinone is a triazinone herbicide with high mobility and persistence in soil. Hexazinone is mainly degraded by soil microorganisms, and its degradation and mineralization processes are significantly affected by soil texture (faster in clay loam) and application method (mixed application can improve its bioavailability and mineralization rate). Hexazinone exhibits mild to moderate acute oral toxicity and has significant eye irritation .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Name
Email *

	Sorry, but the email address you supplied was invalid.