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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
59 Results for "
Rap1
" in MedChemExpress (MCE) Product Catalog:
Products (59)
59 Results for "Rap1" in MCE Product Catalog:
210
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo [1] .
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210 Publications Verification
Synonyms: 1,1-Dimethylbiguanide hydrochloride
Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo [1] .
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9 Cited Publications
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
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1 Cited Publications
Synonyms: 8-CPT-2'-O-Me-cAMP sodium
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8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP) sodium, an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50 >10 μM). 8-pCPT-2′-O-Me-cAMP sodium stimulates Epac-mediated Ca 2+ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP sodium is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP sodium enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration [1] .
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1 Cited Publications
Cat. No.: HY-N0657
CAS No.: 63902-38-5
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1 Cited Publications
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HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP [1].
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1 Cited Publications
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GGTI-2133, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 can be used for the study of eosinophilic airway inflammation such as asthma [1] .
Cat. No.: HY-17471AR
CAS No.: 1115-70-4
Synonyms: 1,1-Dimethylbiguanide hydrochloride (Standard)
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Metformin hydrochloride (Standard) is the analytical standard of Metformin hydrochloride (HY-17471A). This product is intended for research and analytical applications. Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo [1] .
Cat. No.: HY-100876
CAS No.: 180977-44-0
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
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FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity [1].
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AM-001 is a non-competitive inhibitor of Epac1 that blocks the activation of Rap1, a downstream effector of Epac1, in cultured cells. AM-001 can be used in heart disease-related research [1].
Cat. No.: HY-B0627S
CAS No.: 1185512-92-8
Synonyms: 1,1-Dimethylbiguanide-d6
Cat. No.: HY-107544
CAS No.: 1152197-23-3
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8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with PKA pathway [1] .
Cat. No.: HY-132276
CAS No.: 1415684-80-8
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PtdIns-(3,4,5)-P3-biotin sodium is a Biotin-labeled PtdIns-(3,4,5)-P3 (PI(3,4,5)P3). PI(3,4,5)P3 is a substrate of nuclear phosphatidylinositol 5-phosphatase (PIP5Pase). PI(3,4,5)P3 binds to the N-terminus of RAP1 (repressor activator protein 1) and controls its DNA binding activity [1].
Cat. No.: HY-P10038A
Synonyms: Myr-FEEERA-OH TFA
Cat. No.: HY-115489
CAS No.: 171744-11-9
GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM [1] .
Cat. No.: HY-115489A
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GGTI-286 TFA, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 TFA selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 TFA also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM [1] .
Cat. No.: HY-116312
CAS No.: 510774-50-2
Synonyms: 8-CPT-2'-O-Me-cAMP
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8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP), an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50 >10 μM). 8-pCPT-2′-O-Me-cAMP stimulates Epac-mediated Ca 2+ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration [1] .
Cat. No.: HY-169295
CAS No.: 2220208-75-1
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RAP 1 is a reactive affinity probe (RAP) that selectively labels SLC6A8 in the presence of guanine alanine (GPA). RAP 1 can be used as a chemical probe for identifying and studying potential drug binding sites on SLC6A8 [1].
Cat. No.: HY-12369A
CAS No.: 1217480-14-2
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GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma [1] .
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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
