Search Result

Pathways Recommended:	Vitamin D Related/Nuclear Receptor

Results for "

nuclear degradation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	NF-κB (14) ADC Linker (1) Akt (3) AMPK (1) Amyloid-β (1) Androgen Receptor (5) Apolipoprotein (1) Apoptosis (8) AUTACs (1) Autophagy (6) AUTOTACs (3) Calcineurin (1) Caspase (2) COX (1) CRM1 (3) CXCR (1) DNA/RNA Synthesis (3) Drug Derivative (1) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (2) Ferroptosis (2) FKBP (3) GABA Receptor (2) HDAC (1) Hexokinase (1) HIF/HIF Prolyl-Hydroxylase (2) Histone Methyltransferase (6) HMG-CoA Reductase (HMGCR) (1) HSP (1) IAP (1) IKK (2) Influenza Virus (3) Interleukin Related (2) Isotope-Labeled Compounds (1) Keap1-Nrf2 (1) Molecular Glues (4) mTOR (1) NO Synthase (5) NOD-like Receptor (NLR) (2) Parasite (4) PI3K (3) Prostaglandin Receptor (1) PROTACs (8) Pyroptosis (2) RAR/RXR (1) Ras (3) Reactive Oxygen Species (ROS) (1) Reference Standards (3) SARS-CoV (3) SNIPERs (1) Survivin (2) Tau Protein (1) TNF Receptor (2) YAP (1)
By Research Areas:	Cancer (41) Cardiovascular Disease (1) Infection (6) Inflammation/Immunology (18) Metabolic Disease (5) Neurological Disease (3)

By Targets:

NF-κB (14)

ADC Linker (1)

Akt (3)

AMPK (1)

Amyloid-β (1)

Androgen Receptor (5)

Apolipoprotein (1)

Apoptosis (8)

AUTACs (1)

Autophagy (6)

AUTOTACs (3)

Calcineurin (1)

Caspase (2)

COX (1)

CRM1 (3)

CXCR (1)

DNA/RNA Synthesis (3)

Drug Derivative (1)

E1/E2/E3 Enzyme (1)

Epigenetic Reader Domain (2)

Ferroptosis (2)

FKBP (3)

GABA Receptor (2)

HDAC (1)

Hexokinase (1)

HIF/HIF Prolyl-Hydroxylase (2)

Histone Methyltransferase (6)

HMG-CoA Reductase (HMGCR) (1)

HSP (1)

IAP (1)

IKK (2)

Influenza Virus (3)

Interleukin Related (2)

Isotope-Labeled Compounds (1)

Keap1-Nrf2 (1)

Molecular Glues (4)

mTOR (1)

NO Synthase (5)

NOD-like Receptor (NLR) (2)

Parasite (4)

PI3K (3)

Prostaglandin Receptor (1)

PROTACs (8)

Pyroptosis (2)

RAR/RXR (1)

Ras (3)

Reactive Oxygen Species (ROS) (1)

Reference Standards (3)

SARS-CoV (3)

SNIPERs (1)

Survivin (2)

Tau Protein (1)

TNF Receptor (2)

YAP (1)

By Research Areas:

Cancer (41)

Cardiovascular Disease (1)

Infection (6)

Inflammation/Immunology (18)

Metabolic Disease (5)

Neurological Disease (3)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Orphan Nuclear Receptor NF-κB Nuclear Factor of activated T Cells (NFAT) Nuclear Hormone Receptor 4A/NR4A

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0191

Andrographolide 30+ Cited Publications Andrographis	NF-κB SARS-CoV Influenza Virus Autophagy Parasite	Infection Inflammation/Immunology Cancer
Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.

HY-13982

JSH-23 Maximum Cited Publications 141 Publications Verification	NF-κB	Metabolic Disease Inflammation/Immunology Cancer
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC₅₀ of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .

HY-170430

HGC652	Molecular Glues E1/E2/E3 Enzyme	Cancer
HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (K_a=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death .

HY-19979

RCM-1 5+ Cited Publications	DNA/RNA Synthesis	Cancer
RCM-1 is a forkhead box M1 (FOXM1) inhibitor with an EC₅₀ of 0.72 μM in U2OS cells. RCM-1 blocks the nuclear localization and increased the proteasomal degradation of FOXM1. RCM-1 can be used for asthma and other chronic airway diseases research .

HY-138280

DTHIB 5+ Cited Publications	HSP	Cancer
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a K_d of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research .

HY-119264

PRLX-93936	Molecular Glues Ras Apoptosis HIF/HIF Prolyl-Hydroxylase	Cancer
PRLX-93936 is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 inhibits HIF-1 under hypoxic conditions (IC₅₀ = 0.09 μM in cell-based reporter gene assay). PRLX-93936 suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 is applicable to research related to pancreatic cancer and multiple myeloma .

HY-108716

Felezonexor CBS9106; SL-801	CRM1 Apoptosis	Cancer
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells .

HY-N0696

Sipeimine 4 Publications Verification Imperialine	PI3K NF-κB Akt NOD-like Receptor (NLR) Pyroptosis Ferroptosis	Inflammation/Immunology
Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases .

HY-168016

PROTAC YAP degrader-1	PROTACs YAP	Cancer
PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC₅₀=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma .

HY-158420

STL001	Autophagy	Cancer
STL001 is potent and selective FOXM1 inhibitor. STL001 induces the translocation of nuclear FOXM1 to the cytoplasm and promotes its autophagic degradation. STL001 sensitizes human cancers to a broad-spectrum of cancer therapies .

HY-N0191R

Andrographolide (Standard) Andrographis (Standard)	Reference Standards NF-κB SARS-CoV Influenza Virus Autophagy Parasite	Infection Inflammation/Immunology Cancer
Andrographolide (Standard) is the analytical standard of Andrographolide. This product is intended for research and analytical applications. Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.

HY-125740

Malvidin-3-glucoside chloride Malvidin-3-O-glucoside chloride; Oenin chloride	NF-κB TNF Receptor NO Synthase Interleukin Related	Inflammation/Immunology
Malvidin-3-glucoside (Malvidin-3-O-glucoside; Oenin) chloride is an orally active inhibitor of the NF-κB pathway, which blocks inflammatory responses induced by TNF-α, reduces IκB-α degradation and p65 nuclear translocation, and upregulates endothelial nitric oxide synthase eNOS to increase NO production. Malvidin-3-glucoside chloride exerts anti-inflammatory and antioxidant effects by inhibiting pro-inflammatory molecules such as MCP-1, ICAM-1, and IL-6, and regulating intestinal microorganisms and metabolites, while protecting endothelial cells and improving intestinal microecological dysbiosis under inflammatory conditions. Malvidin-3-glucoside chloride can be used to study chronic inflammatory-related diseases such as atherosclerosis and inflammatory bowel disease, and has the potential to prevent vascular inflammation and improve intestinal health .

HY-129610

KB02-SLF	PROTACs FKBP	Cancer
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF .

HY-161574

LLC0424	PROTACs Histone Methyltransferase	Cancer
LLC0424 is a potent and selective cereblon-based *PROTAC nuclear* receptor-binding SET domain-containing 2 (NSD2)** degrader. LLC0424 effectively degraded NSD2 with a DC₅₀ of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .

HY-157251

UNC8153 TFA	Histone Methyltransferase	Cancer
UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a K_d of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC₅₀ in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .

HY-119264A

PRLX-93936 dihydrochloride	Molecular Glues Apoptosis Ras HIF/HIF Prolyl-Hydroxylase	Cancer
PRLX-93936 dihydrochloride is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 dihydrochloride binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 dihydrochloride induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 dihydrochloride inhibits HIF-1 under hypoxic conditions (IC₅₀ = 0.09 μM in cell-based reporter gene assay). PRLX-93936 dihydrochloride suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 dihydrochloride is applicable to research related to pancreatic cancer and multiple myeloma .

HY-159834

Progerinin SLC-D011	DNA/RNA Synthesis	Others
Progerinin (SLC-D011) is an orally active progerin-lamin A binding inhibitor. Progerinin selectively binds to the C-terminal region of progerin, disrupting its interaction with lamin A and promoting progerin degradation while sparing wild-type lamin A, B, and C. Progerinin ameliorates nuclear deformation, increases H3K9me3 levels, and reduces progerin expression in HGPS patient-derived fibroblasts. Progerinin extends lifespan in Lmna ^G609G/G609G mice and Lmna ^G609G/+ mice, improves body weight, hair morphology, cardiac function, and histological phenotypes. Progerinin can be used for the study of Hutchinson-Gilford progeria syndrome (HGPS) .

HY-135700

Mevalonolactone	Calcineurin Ras HMG-CoA Reductase (HMGCR)	Metabolic Disease Inflammation/Immunology
Mevalonolactone is an intermediate metabolite in the eukaryotic mevalonate pathway, serving as the stable δ-lactone form of mevalonate with oral activity. Mevalonolactone exhibits binding affinity for ZNF384 (K_a = 12.6 μM) and inhibitory activity against aconitase (aconitase). Mevalonolactone promotes the nuclear localization of ZNF384 and enhances its binding to the GGPPS promoter. Mevalonolactone induces insulin resistance, disrupts glucose and lipid metabolism, enhances the isoprenylation of K-Ras, and inhibits the activation of the insulin signaling pathway. Mevalonolactone inhibits polypeptide synthesis of HMG-CoA reductase in isolated rat hepatocytes, promotes its degradation, and reduces its enzymatic activity. Mevalonolactone impairs mitochondrial function in rat brains. Mevalonolactone promotes the development of metabolically unhealthy obesity. Mevalonolactone can be used in research related to metabolically abnormal obesity, mevalonic aciduria, HMGCR-related limb-girdle myopathy, and statin-induced myopathy .

HY-111844

PROTAC RAR Degrader-1	PROTACs SNIPERs RAR/RXR	Neurological Disease Metabolic Disease Cancer
PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) .

HY-157251A

UNC8153	Histone Methyltransferase	Cancer
UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a K_d of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC₅₀ in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 .

HY-177454

Basivarsen linker	ADC Linker	Others
Basivarsen linker is a linker used in HY-177452 Zeleciment basivarsen for coupling a TfR1-binding Fab (HY-P990780 Zeleciment) and an antisense oligonucleotide. Zeleciment basivarsen is an antibody-oligonucleotide conjugate (AOC) designed to target mutant nuclear myotonic dystrophy protein kinase (DMPK) RNA for RHase H-mediated degradation to correct splicing. It is used for the study of myotonic dystrophy type 1 (DM1).

HY-P11208C

mNLS-CPP-WSTF TFA	GABA Receptor	Inflammation/Immunology
mNLS-CPP-WSTF TFA is the trifluoroacetate salt of mNLS-CPP-WSTF (HY-P11208). mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .

HY-169387

YT 6-2-PEG3-C2-NH2	AUTOTACs	Cancer
YT 6-2-PEG3-C2-NH2 is the p62/SQSTM1 targeting, autophagy-targeting ligand-linker conjugate of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa .

HY-P11208

mNLS-CPP-WSTF	GABA Receptor	Inflammation/Immunology
mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .

HY-118160

PPM-18 NSC 73233	NO Synthase Drug Derivative IKK NF-κB HDAC Reactive Oxygen Species (ROS) AMPK mTOR PI3K Akt Autophagy Apoptosis	Cardiovascular Disease Infection Neurological Disease Inflammation/Immunology Cancer
PPM-18 (NSC 73233) is a Vitamin K (HY-B2172) analog. PPM-18 prevents LPS-induced IκBα degradation, thereby inhibiting NF-κB activation and nuclear translocation of NF-κB. PPM-18 inhibits LPS-induced nitrite production and iNOS expression. PPM-18 inhibits HDAC6. PPM-18 induces ROS accumulation, activates AMPK, inhibits the mTORC1 and PI3K/AKT pathways, initiates Autophagy, and induces Apoptosis. PPM-18 suppresses seizures in zebrafish and mouse epilepsy models. PPM-18 prevents LPS-induced lethal toxicity and delayed hypotension. PPM-18 exhibits anticancer activity against leukemia and bladder cancer. PPM-18 can be used in research related to septic shock, bladder cancer and atherosclerosis .

HY-125740R

Malvidin-3-glucoside chloride (Standard) Malvidin-3-O-glucoside chloride (Standard); Oenin chloride (Standard)	Reference Standards Interleukin Related NO Synthase NF-κB TNF Receptor	Metabolic Disease Inflammation/Immunology
Malvidin-3-glucoside (Malvidin-3-O-glucoside; Oenin) chloride (Standard) is the analytical standard of Malvidin-3-glucoside chloride (HY-125740). This product is intended for research and analytical applications. Malvidin-3-glucoside chloride is an orally active inhibitor of the NF-κB pathway, which blocks inflammatory responses induced by TNF-α, reduces IκB-α degradation and p65 nuclear translocation, and upregulates endothelial nitric oxide synthase eNOS to increase NO production. Malvidin-3-glucoside chloride exerts anti-inflammatory and antioxidant effects by inhibiting pro-inflammatory molecules such as MCP-1, ICAM-1, and IL-6, and regulating intestinal microorganisms and metabolites, while protecting endothelial cells and improving intestinal microecological dysbiosis under inflammatory conditions. Malvidin-3-glucoside chloride can be used to study chronic inflammatory-related diseases such as atherosclerosis and inflammatory bowel disease, and has the potential to prevent vascular inflammation and improve intestinal health .

HY-175354

PROTAC BET Degrader-13	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader targeting BET. PROTAC BET Degrader-13 significantly degrades PML-eGFP-BRD4 fusion protein with a near-complete loss of EGFP+ nuclear puncta with an EC₅₀ of 1.4 μM . Pink: BET ligand (HY-13030); Blue: E3 ligase ligand (HY-W1125585); Black: linker

HY-155972

CRM1-IN-1	CRM1	Cancer
CRM1-IN-1 (Compound KL1) is a noncovalent CRM1 inhibitor. CRM1-IN-1 induces nuclear CRM1 degradation (IC₅₀: 0.27 μM). CRM1-IN-1 inhibits CRM1-mediated nuclear export and cell proliferation, and triggers apoptosis in colorectal cancer cells .

HY-155816

PROTAC NSD3 degrader-1	PROTACs	Cancer
PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.

HY-130073

Amorfrutin A	NF-κB Apoptosis	Cancer
Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis .

HY-169388

YT 6-2	AUTACs	Cancer
YT 6-2 is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa .

HY-147196

KB03-SLF	PROTACs FKBP	Cancer
KB03-SLF (compound 6) is an electrophilic PROTAC degrader that binds to DCAF16 to degrade the nuclear protein FKBP12. KB03-SLF can be used in cancer research . (Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-W040168); Blue: Ligand for E3 ligase (HY-169968)).

HY-170983

MC-25B	FKBP	Cancer
MC-25B is a specific FKBP12 PROTAC degrader. MC-25B degrades FKBP12 with a DC₅₀ of 0.35 μM and a D_max of 89%. MC-25B facilitates the degradation of nuclear-localized FKBP12 through a DCAF16-dependent mechanism. (Pink: FKBP12 ligand (HY-170988); Blue: E3 ligase ligand HY-170986); Black: linker (HY-128844); FKBP12 ligand+ linker (HY-170987)) .

HY-179123

ZC9	Androgen Receptor Apoptosis	Cancer
ZC9 is a novel androgen receptor (AR) degrader. ZC9 directly binds to AR and inhibits Dihydrotestosterone-induced nuclear translocation of AR. ZC9 promotes AR degradation via the ubiquitin-proteasome system and suppresses AR transcriptional activity. ZC9 significantly decreases the mRNA levels of other AR downstream genes, including PSA, TMPRSS2, and PMEPA1. ZC9 promotes Apoptosis. ZC9 exhibits anticancer activity against prostate cancer .

HY-13982R

JSH-23 (Standard)	NF-κB	Metabolic Disease Inflammation/Immunology Cancer
JSH-23 (Standard) is the analytical standard of JSH-23. This product is intended for research and analytical applications. JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .

HY-178321

UNC10088	Molecular Glues Histone Methyltransferase	Cancer
UNC10088 is a molecular glue targeting NSD2. UNC10088 mediates the formation of a stable ternary complex between SCFFBXO22 and the NSD2 PWWP1 domain. UNC10088 promotes ubiquitination of the SCFFBXO22-dependent NSD2 PWWP1 domain through reversible covalent bonding with the C326 region of FBXO22. UNC10088 could be used in cancer research .

HY-169385

ATC-324	AUTOTACs Androgen Receptor	Cancer
ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa . ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).

HY-169355

TrimTAC1	PROTACs Epigenetic Reader Domain	Cancer
TrimTAC1 is a TRIM21-based PROTAC targeting BRD4. TrimTAC1 selectively degrads NUP98 ^FG-mEGFP-BRD4 ^BD2 nuclear condensates. TrimTAC1 does not degrade soluble mEGFP-BRD4 ^BD2 in A549 cells. (Pink: target protein ligand (+)-JQ-1 (HY-13030); Blue:E3 ligase ligand Acepromazine-OTs (HY-169356); Black: PROTAC linker (HY-W088456); E3 ligase ligand + linker: HY-169357) .

HY-146384

CRM1 degrader 1	CRM1	Cancer
CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer agent target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer .

HY-170674

ND-L11B free base	Histone Methyltransferase	Cancer
ND-L11B is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC₅₀ of 1.48 and 0.8 μM, the D_max is closed to 80 % .

HY-170674A

ND-L11B TFA	Histone Methyltransferase	Cancer
ND-L11B TFA is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC₅₀ of 1.48 and 0.8 μM, the D_max is closed to 80 % .

HY-169386

YT 6-2 analog-1	AUTOTACs	Cancer
YT 6-2 analog-1 (compound 2-3) is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa .

HY-123870

MX107	Survivin IAP NF-κB	Inflammation/Immunology Cancer
MX107 is a selective and potent survivin inhibitor that suppresses triple-negative breast cancer (TNBC) cell proliferation. MX107 induces degradation of survivin and inhibitor-of-apoptosis proteins (IAPs), which inhibits nuclear factor κB (NF-κB) activation induced by DNA damage. MX107 enhances tumoricidal efficacy of genotoxic treatments synergized with chemotherapeutic drugs .

HY-P11502

COG112	Apolipoprotein NO Synthase CXCR NF-κB IKK	Infection
COG112 is an antennapedia-linked apoE-mimetic peptide. COG112 attenuates induction of NO production, inhibits CXC chemokines KC and MIP-2. COG112 reduces nuclear translocation of NF-κB. COG112 inhibits phosphorylation of IκB-α and prevents the degradation of IκB-α. COG112 inhibits the inflammatory response to Citrobacter rodentium .

HY-403733A

(–)-JJ-450	Androgen Receptor	Cancer
(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR ^F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .

HY-168070

COX-2-IN-48	COX NF-κB NO Synthase	Inflammation/Immunology
COX-2-IN-48 (5-25), a COX-2 inhibitor with an IC₅₀ of 51.7 nM for human COX-2, exerts anti-inflammatory and analgesic effects in various rodent models by inhibiting NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, the phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS .

HY-174287

Keap1-IN-2	Keap1-Nrf2	Inflammation/Immunology
Keap1-IN-2 (Compound 164) is a KEAP1 inhibitor (IC₅₀: 2 nM). Keap1-IN-2 indirectly activates Nrf2 by inhibiting KEAP1, thereby enhancing the antioxidant capacity of cells. Keap1-IN-2 promotes the accumulation and nuclear translocation of Nrf2 by blocking KEAP1-mediated Nrf2 degradation. Keap1-IN-2 can be used to study diseases associated with oxidative stress, such as inflammatory bowel disease, Crohn's disease, and immune diseases such as ulcerative colitis .

HY-403733B

(+)-JJ-450	Androgen Receptor Prostaglandin Receptor	Cancer
(+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003) .

HY-403733C

JJ-450	Androgen Receptor	Cancer
JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR ^F876L. JJ-450 has an IC₅₀ of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR ^F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .

HY-N0696R

Sipeimine (Standard) Imperialine (Standard)	Reference Standards PI3K NF-κB Akt NOD-like Receptor (NLR) Pyroptosis Ferroptosis	Inflammation/Immunology
Sipeimine (Standard) is the analytical standard of Sipeimine (HY-N0696R). Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases .

Cat. No.	Product Name	Target	Research Area