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Results for "

transcriptional regulation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) AP-1 (1) Apoptosis (6) Autophagy (3) c-Myc (2) CDK (2) Cytochrome P450 (2) DNA/RNA Synthesis (1) Endogenous Metabolite (1) HDAC (1) Histone Methyltransferase (1) IKZF Family (1) Influenza Virus (1) Mitochondrial Metabolism (1) MMP (1) NF-κB (2) NO Synthase (2) Notch (1) Orphan Receptor (2) PKC (1) PPAR (5) PROTACs (2) REV-ERB (1) Serpin (1) TRP Channel (1) TSH Receptor (1)
By Research Areas:	Cancer (18) Cardiovascular Disease (3) Endocrinology (2) Infection (1) Inflammation/Immunology (5) Metabolic Disease (6) Neurological Disease (1)
Oligonucleotides:	Nucleotides and their Analogs (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-115728

PROTAC CDK9 degrader-4	PROTACs	Cancer
PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.

HY-N6747

Stauprimide	c-Myc Autophagy	Cancer
Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription .

HY-12270

T-5224 Maximum Cited Publications 73 Publications Verification	AP-1 MMP	Others
T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription .

HY-P0312

c-Myc Peptide TFA 1 Publications Verification	c-Myc	Cancer
c-Myc Peptide (TFA) is a synthetic peptide corresponding to the C-terminal amino acids (410-419) of human c-myc protein, and participates in regulation of growth-related gene transcription.

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-103691A

ARN5187 trihydrochloride 1 Publications Verification	Autophagy Apoptosis	Cancer
ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis .

HY-112721

FDI-6 3 Publications Verification	DNA/RNA Synthesis	Cancer
FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.

HY-144175

CDK7-IN-12	CDK	Cancer
CDK7-IN-12 is a potent inhibitor of CDK7. CDK7-IN-12 plays a key role in transcriptional regulation and cell cycle regulation. CDK7-IN-12 effectively inhibit malignant tumor proliferation in vitro and in vivo. CDK7-IN-12 has the potential for the research of cancer disease (extracted from patent WO2021249417A1, compound 43) .

HY-120106

BG14	HDAC	Others
BG14 is a chemical optical modulation of epigenetic regulation of transcription (COMET) probe. BG14 enables high-resolution optical control of epigenetic mechanisms using visible light and can photochromically inhibit human histone deacetylases (HDACs). BG14 can be used to study the dynamic regulation of the human genome .

HY-103691

ARN5187	Autophagy Apoptosis	Cancer
ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis .

HY-14414

GSK4112 5+ Cited Publications SR6452	REV-ERB Apoptosis	Metabolic Disease
GSK4112 (SR6452) is a Rev-erbα agonist with an EC₅₀ value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways .

HY-N0292

Oleuropein 2 Publications Verification	Cytochrome P450 PPAR Apoptosis	Cardiovascular Disease Inflammation/Immunology Cancer
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .

HY-143862

Pparδ agonist 7	PPAR	Metabolic Disease
Pparδ agonist 7 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 7 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2019105234A1, compound TM4) .

HY-143863

PPARδ agonist 8	PPAR	Metabolic Disease
Pparδ agonist 8 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 8 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2021169769A1, compound TM2) .

HY-151379

EM127	Histone Methyltransferase	Cancer
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (K_D=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .

HY-N0292R

Oleuropein (Standard)	Cytochrome P450 PPAR Apoptosis	Cardiovascular Disease Inflammation/Immunology Cancer
Oleuropein (Standard) is the analytical standard of Oleuropein. This product is intended for research and analytical applications. Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .

HY-103484

GATA4-NKX2-5-IN-1	IKZF Family	Cardiovascular Disease
GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC₅₀ of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression .

HY-107916

Thyrotropin 1 Publications Verification TSH; Pretiron	TSH Receptor PKC Apoptosis	Metabolic Disease Inflammation/Immunology Endocrinology Cancer
Thyrotropin (TSH, Pretiron) is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid. Thyrotropin induces transcriptional regulation of TH-gatekeeper genes in tanycytes through the Tshr/Gαq/PKC pathway. Thyrotropin prevents Apoptosis. Thyrotropin has an association of low levels with increased bone remodeling, reduced bone mass and a high fracture risk in mice. Thyrotropin is promising for research of skeletal remodeling, hyperthyroidism .

HY-N1445

Isoquercitrin 4 Publications Verification Isoquercetin; Quercetin 3-glucoside	NF-κB NO Synthase	Inflammation/Immunology Cancer
Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .

HY-P99925

Enoticumab REGN421	Notch	Metabolic Disease Cancer
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .

HY-N10612

Petasin	AMPK PPAR TRP Channel Mitochondrial Metabolism	Metabolic Disease Cancer
Petasin inhibits adipogenesis in cell 3T3-F442A with an IC₅₀ of 0.95 μM. Petasin inhibits the expression of lipid synthesis factors ACC1, FAS and SCD1 by inhibiting transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels . Petasin inhibits mitochondrial complex I, thereby inhibiting tumor growth and metastasis. Petasin activates AMPK signaling pathway, participating in regulation of glucose and lipid metabolism. Petasin is orally active .

HY-156190

NR2F2-IN-1	Orphan Receptor	Cancer
NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .

HY-156190A

NR2F2-IN-1 free base	Orphan Receptor	Cancer
NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .

HY-N1445R

Isoquercitrin (Standard) Isoquercetin (Standard); Quercetin 3-glucoside (Standard)	NF-κB NO Synthase	Inflammation/Immunology Cancer
Isoquercetin (Standard) is the analytical standard of Isoquercetin. This product is intended for research and analytical applications. Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .

HY-P10336

Serpinin	Serpin	Neurological Disease Endocrinology
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function . Serpinin is a selective agonist for β-adrenergic receptors. Serpinin interacts with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .

HY-N0086R

N6-Methyladenosine (Standard)	Influenza Virus Endogenous Metabolite	Infection
N6-Methyladenosine (Standard) is the analytical standard of N6-Methyladenosine. This product is intended for research and analytical applications. N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities. In Vitro: N6-methyladenosine (m6A) is selectively recognized by the human YTH domain family 2 (YTHDF2) protein to regulate mRNA degradation. N6-methyladenosine (m6A), a prevalent internal modification in the messenger RNA of all eukaryotes, is post-transcriptionally installed by m6A methyltransferase (e.g., MT-A70) within the consensus sequence of G(m6A)C (70%) or A(m6A)C (30%). N6-methyladenosine (m6A)-containing RNAs are greatly enriched in the YTHDF-bound portion and diminished in the flow-through portion . N6-methyladenosine (m6A), the most abundant internal RNA modification, functions in diverse biological processes, including regulation of embryonic stem cell self-renewal and differentiation. N6-methyladenosine (m6A) is a large protein complex, consisting in part of methyltransferase-like 3 (METTL3) and methyltransferase-like 14 (METTL14) catalytic subunits .

Cat. No.	Product Name

HY-L090

Transcription Factor-Targeted Library	1,757 compounds
Transcription is the essential first step in the conversion of the genetic information in the DNA into protein and the major point at which gene expression is controlled. Transcription of protein-coding genes is accomplished by the multi-subunit enzyme RNA polymerase II and an ensemble of ancillary proteins, called transcription factors (TFs). Transcription factors play an important role in the long-term regulation of cell growth, differentiation and responses to environmental cues. Deregulated transcription factors contribute to the pathogenesis of a plethora of human diseases, ranging from diabetes, inflammatory disorders and cardiovascular disease to many cancers, and thus these proteins hold great therapeutic potential. MCE offers a unique collection of 1,757 compounds with validated transcription factor targets modulating properties. MCE transcription factor-targeted compound library is an effective tool for researching transcription factors as drug targets as well as modulation of TFs for different therapeutic applications.

Transcription Factor-Targeted Library

1,757 compounds

Transcription is the essential first step in the conversion of the genetic information in the DNA into protein and the major point at which gene expression is controlled. Transcription of protein-coding genes is accomplished by the multi-subunit enzyme RNA polymerase II and an ensemble of ancillary proteins, called transcription factors (TFs). Transcription factors play an important role in the long-term regulation of cell growth, differentiation and responses to environmental cues. Deregulated transcription factors contribute to the pathogenesis of a plethora of human diseases, ranging from diabetes, inflammatory disorders and cardiovascular disease to many cancers, and thus these proteins hold great therapeutic potential.

MCE offers a unique collection of 1,757 compounds with validated transcription factor targets modulating properties. MCE transcription factor-targeted compound library is an effective tool for researching transcription factors as drug targets as well as modulation of TFs for different therapeutic applications.

HY-L088

Angiogenesis-Related Compound Library	2,645 compounds
Angiogenesis is the physiological process through which new blood vessels are formed from pre-existing vessels. It occurs in various physiological processes e.g. embryonic development, menstrual cycle, exercise and wound healing etc. Angiogenesis is regulated by both endogenous activators and inhibitors. Some key activators of angiogenesis include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), angiogenin, TGF-β, etc. whereas angiogenesis inhibitors are angiostatin, endostatin, interferon, platelet factor 4, etc. The loss of balance between these opposing signals leads to life threatening diseases like cancer, cardiovascular and ischemic diseases etc. which are thus controlled by exogenous angiogenesis activators (for cardiovascular/ischemic disorders) and inhibitors (for cancer). MCE offers a unique collection of 2,645 compounds with validated angiogenesis targets modulating properties. MCE angiogenesis-related compound library is an effective tool for angiogenesis research and discovery of angiogenesis-related drugs.

Angiogenesis-Related Compound Library

2,645 compounds

Angiogenesis is the physiological process through which new blood vessels are formed from pre-existing vessels. It occurs in various physiological processes e.g. embryonic development, menstrual cycle, exercise and wound healing etc. Angiogenesis is regulated by both endogenous activators and inhibitors. Some key activators of angiogenesis include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), angiogenin, TGF-β, etc. whereas angiogenesis inhibitors are angiostatin, endostatin, interferon, platelet factor 4, etc. The loss of balance between these opposing signals leads to life threatening diseases like cancer, cardiovascular and ischemic diseases etc. which are thus controlled by exogenous angiogenesis activators (for cardiovascular/ischemic disorders) and inhibitors (for cancer).

MCE offers a unique collection of 2,645 compounds with validated angiogenesis targets modulating properties. MCE angiogenesis-related compound library is an effective tool for angiogenesis research and discovery of angiogenesis-related drugs.

HY-L045

Oxygen Sensing Compound Library	3,360 compounds
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 3,360 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Oxygen Sensing Compound Library

3,360 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 3,360 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

HY-L014

NF-κB Signaling Compound Library	1,159 compounds
Nuclear factor-κB (NF-κB)/Rel proteins include NF-κB2 p52/p100, NF-κB1 p50/p105, c-Rel, RelA/p65, and RelB. These proteins function as dimeric transcription factors that regulate the expression of genes and influence a broad range of biological processes including innate and adaptive immunity, inflammation, stress responses, B-cell development, and lymphoid organogenesis. NF-κB plays a key role in regulating the immune response to infection. In addition, activation of the NF-κB pathway is involved in the pathogenesis of chronic inflammatory diseases, such as asthma, rheumatoid arthritis, and inflammatory bowel disease. Incorrect regulation of NF-κB has been linked to cancer, inflammatory and autoimmune diseases, septic shock, viral infection, and improper immune development. MCE owns a unique collection of 1,159 small molecule compounds that can be used in the research of NF-κB signaling pathway or high throughput screening (HTS) related drug discovery.

NF-κB Signaling Compound Library

1,159 compounds

Nuclear factor-κB (NF-κB)/Rel proteins include NF-κB2 p52/p100, NF-κB1 p50/p105, c-Rel, RelA/p65, and RelB. These proteins function as dimeric transcription factors that regulate the expression of genes and influence a broad range of biological processes including innate and adaptive immunity, inflammation, stress responses, B-cell development, and lymphoid organogenesis. NF-κB plays a key role in regulating the immune response to infection. In addition, activation of the NF-κB pathway is involved in the pathogenesis of chronic inflammatory diseases, such as asthma, rheumatoid arthritis, and inflammatory bowel disease. Incorrect regulation of NF-κB has been linked to cancer, inflammatory and autoimmune diseases, septic shock, viral infection, and improper immune development.

MCE owns a unique collection of 1,159 small molecule compounds that can be used in the research of NF-κB signaling pathway or high throughput screening (HTS) related drug discovery.

HY-L018

TGF-beta/Smad Compound Library	317 compounds
The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc. MCE designs a unique collection of 317 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.

TGF-beta/Smad Compound Library

317 compounds

The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.

MCE designs a unique collection of 317 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.

Cat. No.	Product Name	Target	Research Area