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Results for "

transactivation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (2) Antibiotic (3) Apoptosis (6) Autophagy (1) Bacterial (1) c-Myc (1) Cytochrome P450 (2) Epigenetic Reader Domain (1) Fungal (3) FXR (1) Glucocorticoid Receptor (3) HDAC (2) Histone Acetyltransferase (1) HIV (1) IKK (1) MDM-2/p53 (3) NF-κB (2) PDGFR (1) PKA (1) PPAR (3) STAT (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (12) Cardiovascular Disease (1) Endocrinology (4) Infection (4) Inflammation/Immunology (8) Metabolic Disease (3) Neurological Disease (1)

Inhibitors & Agonists

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12702

10058-F4 Maximum Cited Publications 34 Publications Verification	c-Myc Autophagy	Cancer
10058-F4 is a c-Myc inhibitor that prevents c-Myc-Max dimerization and transactivation of c-Myc target gene expression.

HY-100348

EPI-001
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .

HY-10074

TPCA-1 20+ Cited Publications	IKK STAT Apoptosis	Inflammation/Immunology Cancer
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC₅₀ of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

HY-10678

BMS-687453 2 Publications Verification	PPAR	Cardiovascular Disease
BMS-687453 is a potent and selective PPARα agonist, with an EC₅₀ and IC₅₀ of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.

HY-125265

JTP-117968	Glucocorticoid Receptor	Metabolic Disease
JTP-117968, a novel selective glucocorticoid receptor modulator (a non-steroidal SGRM, IC₅₀ of 6.8 nM), exhibits improved transrepression/transactivation dissociation .

HY-100348R

EPI-001 (Standard)	Androgen Receptor PPAR Apoptosis	Cancer
EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .

HY-108639

MIRA-1 NSC 19630	MDM-2/p53 Apoptosis	Cancer
MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity .

HY-19337

Ketodarolutamide 1 Publications Verification BAY 1896953; ORM-15341	Androgen Receptor	Endocrinology
Ketodarolutamide (ORM-15341) is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.

HY-108470

Ro5-3335 3 Publications Verification	Others	Cancer
Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation .

HY-110267

DY268	FXR	Metabolic Disease
DY268 is a farnesoid X receptor (FXR) antagonist (IC₅₀=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC₅₀ value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI) .

HY-126428

ZL0580	HIV Epigenetic Reader Domain	Infection Inflammation/Immunology
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter .

HY-N2273

Gymnestrogenin
Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br . Gymnestrogenin is a LXR antagonist with IC₅₀s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression .

HY-115539

Windorphen	Wnt β-catenin Histone Acetyltransferase	Cancer
Windorphen is a Wnt/β-catenin signal inhibitor that specifically targets the function of the c-terminal transactivation domain of β-catenin-1 but not β-catenin-2. Windorphen selectively targets p300, disrupting the association of the mammalian β-catenin with p300 but not CBP .

HY-123352

ZK 216348 (+)-ZK 216348	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC₅₀ of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC₅₀s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects .

HY-135046

MTOB sodium 1 Publications Verification	Others	Neurological Disease Inflammation/Immunology Cancer
MTOB sodium is a potent C-terminal binding protein (CtBP) inhibitor. MTOB sodium attenuates repetitive head injury-elicited neurologic dysfunction and neuroinflammation via inhibition of the transactivation activity of CtBP1 and CtBP2. MTOB sodium antagonizes the transcriptional regulatory activity of CtBP1 and CtBP2 by eviction from their target promoters in breast cancer cell lines .

HY-123352A

(-)-ZK 216348	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
(-)-ZK 216348 is the enantiomer of (+)-ZK 216348 (HY-123352). (+)-ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist with an IC₅₀ of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC₅₀s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects .

HY-146564

R-HP210	NF-κB	Inflammation/Immunology
R-HP210 acts on the NF-κB mediated tethered transrepression function (IC₅₀=3.80 μM). R-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. R-HP210 does not induce the transactivation functions of Glucocorticoids (GCs) .

HY-B1324A

Oxiconazole Ro 13-8996 free base	Fungal Cytochrome P450 Antibiotic	Infection Cancer
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .

HY-B1324

Oxiconazole nitrate 1 Publications Verification Ro 13-8996	Fungal Cytochrome P450 Antibiotic	Infection Cancer
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .

HY-121542

PPARδ agonist 10	PPAR	Metabolic Disease
PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC₅₀ values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research .

HY-N6727

Gliotoxin Aspergillin	Apoptosis PKA NF-κB Bacterial Fungal Antibiotic	Infection Inflammation/Immunology Cancer
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis . Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells . Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells .

HY-160053

Gint4.T aptamer sodium	PDGFR	Cancer
Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM). Gint4.T aptamer sodium inhibits PDGFRβ heterodimerization and EGFR transactivation. It can significantly inhibit cell migration and proliferation, induce differentiation and prevent tumor growth in vivo. Gint4.T aptamer sodium specifically inhibits PDGFRβ-mediated tropism of mesenchymal stem cells (MSCs) toward the tumor microenvironment .

HY-16138

Ivaltinostat CG-200745	HDAC MDM-2/p53 Apoptosis	Cancer
Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects .

HY-16138A

Ivaltinostat formic CG-200745 formic	HDAC MDM-2/p53 Apoptosis	Inflammation/Immunology Endocrinology
Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects .

Gliotoxin Aspergillin	Structural Classification Anti-inflammation/Immunoregulatory Classification of Application Fields Source classification Antibacterial Disease Research Other Antibiotics Biological Pesticide Research Agricultural Research Infection Microorganisms Antibiotics Inflammation/Immunology Disease Research Fields	Apoptosis PKA NF-κB Bacterial Fungal Antibiotic
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis . Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells . Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells .

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transactivation

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