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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
227 Results for "
G protein signaling
" in MedChemExpress (MCE) Product Catalog:
Products (227)
227 Results for "G protein signaling" in MCE Product Catalog:
64
64 Publications Verification
Synonyms: MRTX849
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
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62 Cited Publications
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
32
32 Cited Publications
Synonyms: Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium
32
32 Cited Publications
Synonyms: Ursodeoxycholate; Ursodiol; UDCA
19
19 Cited Publications
Target:
12
12 Cited Publications
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IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation .
10
10 Cited Publications
Synonyms: (±)-α-Lipoamide; DL-Lipoamide; DL-6,8-Thioctamide
Category:
Human Gut Microbiota Metabolites Natural Products Other Diseases Endogenous metabolite Disease Research Fields
Target:
7
7 Cited Publications
Cat. No.: HY-18705
CAS No.: 932986-18-0
Research Areas:
Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity .
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5 Cited Publications
BSJ-03-123 is a selective PROTAC degrader of CDK6. BSJ-03-123 degrades CDK6, thereby inhibiting Rb S780 phosphorylation and inducing G1 phase arrest, while remodeling cell cycle and transcriptional signaling, with no effect on CDK4-dependent cancer cells. BSJ-03-123 reduces CDK6 protein levels in mouse ovarian tissues, increases the proportion of primordial follicles, and induces granulosa cell apoptosis, without impairing the ability of oocytes to resume meiosis and mature to the MII stage. BSJ-03-123 alleviates uveitis by blocking the HDACs-CDK6/ID2 axis. BSJ-03-123 can be used in studies related to acute myeloid leukemia, mantle cell lymphoma and autoimmune uveitis .
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3 Cited Publications
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
3
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3
3 Cited Publications
Cat. No.: HY-P2141A
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2
2 Cited Publications
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ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons .
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2 Cited Publications
FzM1.8 is a Wnt/β-catenin signaling pathway agonist and an allosteric agonist of Frizzled 4 (FZD4), with a pEC50 of 6.4 for FZD4 . FzM1.8 stabilizes a conformation with increased affinity for heterotrimeric G proteins, promoting Gβγ release and subsequent PI3K activation. FzM1.8 activates the AKT pathway downstream of FZD4. FzM1.8 does not affect FZD4 maturation or plasma membrane localization and does not induce FZD4 endocytosis. FzM1.8 upregulates the WNT-responsive genes C-myc and Cyclin D1, while leaving lgr5 expression unchanged. FzM1.8 can be used for colon cancer research .
2
Chromeceptin (94G6) is an IGF signaling pathway inhibitor. Chromeceptin suppresses IGF2 expression at mRNA and protein levels in hepatocyte and HCC cells. Chromeceptin inhibits the phosphorylation levels of AKT and mTOR .
2
2 Cited Publications
Cat. No.: HY-70075
CAS No.: 620113-73-7
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CCG-63808 is a selective, reversible RGS4 inhibitor with an IC50 of 10 μM for the Gαo-RGS4 interaction . CCG-63808 enhances the contractile response of lymphatic smooth muscle and potentiates agonist-mediated thoracic duct contraction. CCG-63808 can be used in research related to neuropathic pain and hypertension .
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2 Cited Publications
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CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .
1
1 Cited Publications
BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state. BBO-8520 can be used for the research of cancer .
1
1
1 Cited Publications
Cat. No.: HY-16642A
CAS No.: 1231220-79-3
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LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
