glucocorticoid receptor

Glucocorticoid receptor agonist is an effective glucocorticoid receptor agonist.

Glucocorticoid receptor/IL-6-IN-1 (Compound 35) is a selective dual inhibitor of the glucocorticoid receptor (GR) and the IL-6 signaling pathway, with IC50 values of 120 nM and 59 nM, respectively. It suppresses IL-6-induced phosphorylation of JAK/STAT3, thereby blocking the transcription of inflammatory cytokines. This compound holds potential for research into inflammatory diseases such as rheumatoid arthritis and asthma.

Glucocorticoid receptor/IL-6-IN-2 (Compound 36) is a selective dual inhibitor of the glucocorticoid receptor (GR) and the IL-6 signaling pathway, with IC50 values of 120 nM and 59 nM, respectively. It shows potential for research in inflammatory diseases such as rheumatoid arthritis and asthma.

Glucocorticoid receptoragonist-6 (Compound A) is a glucocorticoid receptor (GR) agonist. It can be utilized as a cytotoxic payload in the synthesis of antibody-drug conjugates (ADCs).

Glucocorticoid receptor-IN-2 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. IC50: 0.171 nM) and also has some transcriptional activating effect on MMTV (EC50: 0.94 nM).

Glucocorticoid receptor-IN-1 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. glucocorticoid receptor-IN-1 has good transcriptional repression, acting on hMMP1 ( IC50: 2.11 nM) and also has a transcriptional activating effect on MMTV (EC50: 5.59 nM).

Glucocorticoid receptor modulator 1 is a highly effective and orally administered NF-κB and AP-1 inhibitor with IC50 values of 9 nM and 130 nM, respectively. It can downregulate the expression of inflammatory factors IL-6, IL-1β, TNF-α, and MMP-13, thereby alleviating skin inflammation.

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88), a glucocorticosteroid and glucocorticoid receptor agonist, can be conjugated with Adalimumab to formulate an ADC [1].

Glucocorticoid receptor agonist-2 (compound 21), a glucocorticoid receptor agonist with an IC50 value of 6.6 nM, serves as an active reference for ABBV-3373 [1] and is instrumental in the synthesis of anti-inflammatory ADC molecules.

Glucocorticoid Receptor Agonist-1 Phosphate Ala-Ala-Mal functions as a glucocorticoid receptor agonist, utilized in the formulation of anti-CD40 antibody agent conjugates (ADC). It serves as a research tool for exploring inflammation and immune regulation [1].

Glucocorticoid Receptor Agonist-1 Phosphate Ala-Ala-Br is a drug-linker conjugate for antibody-drug conjugates (ADCs), serving as a reaction reagent in the creation of anti-CD40 antibody agent conjugates [1].

Glucocorticoid Receptor Agonist-3 (Preparation 6) acts as a glucocorticoid receptor agonist [1].

Glucocorticoid Receptor Agonist-4 (Compound Preparation 5) serves as an agonist for glucocorticoid receptors and can be conjugated with TNF-α antibodies, facilitating research into autoimmune and inflammatory diseases [1].

Glucocorticoid Receptor Agonist-4 Ala-Ala-Mal (Compound Preparation 9) is a conjugate of anti-human TNFα antibody and glucocorticoid receptor agonist (GC). It is applicable in the research of autoimmune and inflammatory diseases [1].

Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Mal functions as a glucocorticoid receptor agonist and serves as a drug-linker conjugate for ADC. This compound is instrumental in the synthesis of anti-CD40 antibody agent conjugates (WO2019106608A1; example 9) [1].

Glucocorticoid receptor modulator3 (Payload 6) is a thioester-based modulator of the glucocorticoid receptor, exhibiting a potent IC50 value of 0.6 nM. This compound is deactivated through rapid hepatic metabolism, minimizing systemic exposure of its unconjugated active payload. Glucocorticoid receptor modulator3 is suitable for development in antibody-drug conjugates (ADCs) targeted at autoimmune diseases.

Compound DL5, also known as Glucocorticoid receptor modulator 4, acts as a conjugate of linkers and glucocorticoid receptor regulators. It demonstrates GRE reporter activity in K562 cells expressing mTNF with an EC50 of 40 μM. Additionally, Compound DL5 binds to anti-tumor necrosis factor (TNF) antibodies and exhibits anti-inflammatory properties in combating arthritis in mouse models.

Glucocorticoid Receptoragonist-5 (compound 4) is an effective glucocorticoid molecule acting as a potent agonist for glucocorticoid receptors. It exhibits anti-inflammatory and immunosuppressive activities and serves as an ADC cytotoxin.

Glucocorticoid receptor agonist-1, a potent glucocorticoid receptor agonist, has an IC50 of 2.8 nM[1].

Glucocorticoid Receptor Agonist-3 Ala-Ala-Mal (Compound Preparation 8) is a conjugate of an anti-human TNFα antibody and a glucocorticoid receptor agonist (GC). It is utilized in researching autoimmune and inflammatory diseases [1].

Glucocorticoid Receptor Activator 1, a phenyl nitrogen-heterocyclic precursor, acts as an activator of the glucocorticoid receptor (GR). By activating GR, it downregulates the expression of pro-inflammatory genes stimulated by TNF, making it useful for inflammation research.

Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. It prevents degradation of glucocorticoid receptor (GR) mRNA and GR protein and inhibits the activation of the NF-κB signaling pathway. Additionally, it reduces levels of nitric oxide (NO), interleukin (IL-6), and tumor necrosis factor-alpha (TNF-α), and improves sepsis in mice.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Dexamethasone is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory, immunosuppressive, and apoptosis-inducing activities. It inhibits the production of inflammatory miRNA-155 exosomes in macrophages, significantly reduces inflammatory cytokine expression in neutrophils and monocytes, suppresses LPS-induced macrophage inflammation, and induces autophagy. It is commonly used to induce animal models of depression, muscle atrophy, and hypertension, and holds potential in COVID-19 research.