transcriptional

S-23 ((S)-3-(4-chloro-3-fluorophenoxy)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide) is an oral selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.

O6-Benzylguanine is a guanine analog with antineoplastic activity,and is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.

p,p'-DDE (p,p'-dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT

TLX agonist 1 is an orphan nuclear receptor tailless (TLX, NR2E1) modulator

PTGR2-IN-1 is a potent inhibitor of PTGR2 (IC50: 0.7 μM) that enhances 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor that disrupts the [SIX1/EYA2] complex, EMT, and metastasis.

Mifobate (SR-202) is a potent and specific antagonist of PPARγ, exhibiting antiobesity, antidiabetic, and antiatherosclerotic effects[1].

UNC 669 is an effective and specific MBT (malignant brain tumor) inhibitor with IC50 of 4.2/3.1 uM for L3MBTL1/3.

NKL 22 (Histone Deacetylase Inhibitor IV) is an effective Histone Deacetylase Inhibitor.

TED-347 is an irreversible and covalent inhibitor of TEAD4-Yap1 protein-protein interaction(EC50 of 5.9 μM), and inhibits glioblastoma cell viability.

NS-3-008 hydrochloride (NS-3-008 HCl) is a transcriptional G0/G1 switch 2 (G0s2) inhibitor( IC50 of 2.25 μM).

EN4 (EN4 MYC inhibitor) MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC. It is selective for c-MYC over N-MYC and L-MYC, and inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

Transcriptional Intermediary Factor 2 (TIF2) (740-753) is a 14-amino acid peptide coactivator, encompassing residues 740-753 of the TIF-2 protein.

BRD-K98645985 is a BAF transcriptional repression inhibitor (EC50: ~2.37 µM). It binds ARID1A-specific BAF complexes, potently reverses HIV-1 latency and prevents nucleosomal positioning.

BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.

Acolbifene (SCH 57068) is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.

Pifithrin-α, p-Nitro, Cyclic (PFN-α) is a cell-permeable, active-form inhibitor of p53.

JSH-23 is an NF-κB inhibitor that inhibits NF-κB transcriptional activity (IC50=7.1 μM) but does not affect IκBα degradation. JSH-23 is an antioxidant with anti-inflammatory activity.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8/0.8/5.3/16.7 nM for ALK1/2/3/6).

PY-60 can effectively activate YAP transcriptional activity against annexin A2 (ANXA2) (Kd value of 1.4 µM). PY-60 activates a pro-proliferative, YAP-dependent transcriptional program in adult animals that are able to remodel the epidermis through proliferation.

GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

β-Apo-13-carotenone, a naturally occurring apocarotenoid, functions as an antagonist of the retinoid X receptor (RXR). β-Apo-13-carotenone inhibits transactivation of RXRα but does not interfere with coactivator binding to the receptor in the manner observed for the known antagonist UVI3003. β-Apo-13-carotenone induces the formation of a transcriptionally silent RXR tetramer. β-Apo-13-carotenone is therefore relevant for mechanistic investigations involving nuclear receptor signaling, transcriptional regulation, and retinoid-associated cellular processes.

OP-3633 is an effective and selective steroidal glucocorticoid receptor (GR) antagonist (IC50: 29 nM). OP-3633 shows low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism. It also has an inhibition of GR transcriptional activity.