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ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character .
SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
MCB-613 is a potent Steroid receptor coactivatorSRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity.
MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS).
MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program .
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1 .
Transcriptional Intermediary Factor 2 (TIF2) (740-753) is a TIF-2 coactivator peptide composed of 14 amino acids and covers the residue range 740-753 of TIF-2 protein .
SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
SR-18292-d9 is the deuterium labeled SR-18292 (HY-101491). SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes .
SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
Ethacridine is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor and an activator of the transcriptional coactivator. Ethacridine induces thyroid cancer cells apoptosis and promotes differentiation in thyroid follicular cells .
EPZ0025654 (GSK3536023) is an inhibitor for protein arginine methyltransferases 4 (PRMT4) (which is also known as coactivator associated arginine methyltransferase 1 CARM1), with IC50 of 3 nM .
MLS000389544 is a selective and potent methylsulfonylnitrobenzoate thyroid hormone receptor β (TRβ) antagonist that blocks the association of TRβ with steroid receptor coactivator 2 (SRC2) .
CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
(E)-SI-2 is an isomer of SI-2, an inhibitor of the steroid receptor coactivator SRC-3. SI-2 has anticancer activity and increases the number of cytotoxic immune cells in mice with breast cancer .
SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor .
KG-655 is a small molecule compound that binds to the β-folded surface and internal cavity of ARNT PAS-B and interferes with its binding to the transcriptional coactivator TACC3. KG-655 can promote the homodimerization of ARNT PAS-B and has the potential to regulate multiple ARNT-mediated signaling pathways .
DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5 .
R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
(E/Z)-MCB-613 is a pan-Steroid Receptor Coactivator (SRC) stimulator. (E/Z)-MCB-613 overstimulates SRC activity in cancer cells resulting in excessive generation of reactive oxygen species (ROS), leading to cell stress and death by a process called paraptosis. (E/Z)-MCB-613 is a cytotoxic molecule that plays an important role in cancer .
AdipoR agonist 1 (Compound 112254) is an agonist for adiponectin receptor (AdipoR), which activates the transcriptional regulators like peroxisome proliferator-activated receptors (PPARs), peroxisome proliferator-activated receptor gamma coactivator 1α (PGC-1α), sirtuin 1 (SIRT1), and adenylate-activated protein kinase (AMPK). AdipoR agonist 1 is utilized in preventive doping research .
SRC-3-IN-1 (compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor (IC50=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research .
LG190178 is a non-steroidal vitamin D receptor (VDR) ligand that can induce the formation of heterodimer complexes between VDR and retinoid X receptor (RXR), stabilizing the agonistic conformation of the VDR ligand-binding domain and promoting its interaction with co-activators. LG190178 has functions in regulating calcium homeostasis, bone mineralization, as well as cell proliferation, differentiation, and apoptosis, making it useful for research in psoriasis, osteoporosis, and cancer .
Tanaproget is an orally effective, selective nonsteroidal progesterone receptor (PR) agonist targeting human PR with an IC50 of 1.7 nM. Tanaproget promotes the interaction between PR receptors and coactivators (such as SRC-1), thereby inhibiting the secretion of matrix metalloproteinases (MMP-3/MMP-7) and reducing endometrial tissue invasion and angiogenesis. Tanaproget can be used for contraception and endometriosis inhibition research .
ESI1 is a small molecule epigenetic silencing inhibitor. ESI1 can trigger the formation of nuclear condensates of key lipid metabolism regulators SREBP1/2, concentrating transcriptional co-activators to drive lipid/cholesterol biosynthesis. ESI1 can promote myelin regeneration in demyelinated animal models and facilitate de novo myelination on regenerating CNS axons, reversing age-related declines in cognitive abilities .
Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability .
15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2), a metabolite of PGD2 (HY-101988), is an agonist of prostaglandin receptor 2 (DP2). 15-deoxy-Δ12,14-Prostaglandin D2 binds to DP2 (Ki=50 nM) and induces eosinophil activation (EC50=8 nM). 15-deoxy-Δ12,14-Prostaglandin D2 also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), inducing PPARγ-mediated transcription. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is cytotoxic to L1210 murine leukemia cells (IC50=0.3 μg/ml) and inhibits ADP-induced platelet aggregation (IC50=320 ng/mL).
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activatorBRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN .
PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC50=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC50 of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration .
C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivatorsYAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
Transcriptional Intermediary Factor 2 (TIF2) (740-753) is a TIF-2 coactivator peptide composed of 14 amino acids and covers the residue range 740-753 of TIF-2 protein .
SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
The PC4/SUB1 protein acts as a multifunctional coactivator that cooperates with TAF to promote functional interactions between upstream activators and the general transcription machinery. Its role extends to the potential stability of multiprotein transcription complexes. PC4/SUB1 Protein, Human (His) is the recombinant human-derived PC4/SUB1 protein, expressed by E. coli , with N-His labeled tag. The total length of PC4/SUB1 Protein, Human (His) is 127 a.a., with molecular weight of ~19 kDa.
CARM1 Protein, Human (His) is the recombinant human-derived CARM1, expressed by E. coli , with C-10*His labeled tag. The total length of CARM1 Protein, Human (His) is 607 a.a.,
RBM14; SIP; RNA-binding protein 14; Paraspeckle protein 2; PSP2; RNA-binding motif protein 14; RRM-containing coactivator activator/modulator; Synaptotagmin-interacting protein; SYT-interacting protein
The RBM14 protein has different isoforms with multiple functions. Isoform 1 enhances transcription as a nuclear receptor coactivator, interacting with NCOA6 and CITED1. RBM14 Protein, Human (His-SUMO) is the recombinant human-derived RBM14 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of RBM14 Protein, Human (His-SUMO) is 669 a.a., with molecular weight of ~85.5 kDa.
GAPDH, a multifunctional protein, acts as a key enzyme in glycolysis, catalyzing the conversion of G3P. It also functions as a nitrosylase, impacting nuclear processes. In addition, it influences cytoskeleton organization, associates with CHP1, participates in transcript-selective translation inhibition, contributes to immune responses, and mediates nuclear events through S-nitrosylation of target proteins. GAPDH Protein, Human (His-SUMO) is the recombinant human-derived GAPDH protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag.
TGS1 protein catalyzes the conversion of the 7-monomethylguanosine (m(7)G) cap of small nuclear RNA (snRNA) and small nucleolar RNA (snoRNA) into 2, 2,7-trimethylguanosine (m( 2,2,7)G) Cap structure. The enzyme shows specificity for guanine, with N7 methylation occurring before N2 methylation during the modification process. TGS1 Protein, Human (His-SUMO) is the recombinant human-derived TGS1 protein, expressed by E. coli , with N-His, N-SUMO labeled tag. The total length of TGS1 Protein, Human (His-SUMO) is 141 a.a., with molecular weight of ~31.6 kDa.
SR-18292-d9 is the deuterium labeled SR-18292 (HY-101491). SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes .
PGC1 alpha+beta Antibody (YA3458) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3458), targeting PGC1 alpha+beta , with a predicted molecular weight of 91/113 kDa (observed band size:110 kDa). PGC1 alpha+beta Antibody (YA3458) can be used for WB experiment in human, mouse, rat background.
PGC1 alpha Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 91 kDa, targeting to PGC1 alpha. It can be used for WB assays with tag free, in the background of Human, Mouse, Rat.
CREB Regulated Transcription Coactivator 2 Antibody (YA3279) is a non-conjugated IgG antibody, targeting CREB Regulated Transcription Coactivator 2, with a predicted molecular weight of 73 kDa (observed band size: 80 kDa). CREB Regulated Transcription Coactivator 2 Antibody (YA3279) can be used for WB experiment in human background.
Aly Antibody (YA2079) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2079), targeting Aly, with a predicted molecular weight of 27 kDa (observed band size: 27 kDa). Aly Antibody (YA2079) can be used for WB, IHC-F, IHC-P, ICC/IF, IP experiment in human, mouse, rat background.
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