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GEFs

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Acyltransferase (1) Apoptosis (4) Autophagy (1) DOCK (1) EGFR (1) ERK (1) JNK (1) PI3K (1) Ras (13) ROCK (1) Src (1) STAT (1)
By Research Areas:	Cancer (15) Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (1)

Inhibitors & Agonists

Peptides

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Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P1382A

Rac1 Inhibitor W56 TFA	Ras	Cancer
Rac1 Inhibitor W56 TFA is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 TFA inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam .

HY-110100

CPYPP 2 Publications Verification	DOCK	Inflammation/Immunology
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 ^DHR-2 for Rac1 in a dose-dependent manner with an IC₅₀ of 22.8 μM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9 .

HY-117656

ESI-05 3 Publications Verification NSC 116966	Acyltransferase	Neurological Disease Metabolic Disease
ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC₅₀ of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders .

HY-12649

Y16 5 Publications Verification	Ras	Cancer
Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a K_d value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP .

HY-102078

ZINC69391 1 Publications Verification	Ras Apoptosis	Cancer
ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects .

HY-12646

Rhosin hydrochloride Maximum Cited Publications 24 Publications Verification	Ras Apoptosis	Cancer
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a K_d of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .

HY-19539

NSC-658497	Ras	Cancer
NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation .

HY-P1382

Rac1 Inhibitor W56	Ras	Cancer
Rac1 Inhibitor W56 is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam .

HY-124161

SCH54292	Ras	Cancer
SCH54292 is a potent *Ras-GEF* interaction inhibitor with IC₅₀ of 0.7 μM .

HY-151461

CHNQD-01255	Others	Cancer
CHNQD-01255 is an orally active *Arf-GEFs* inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy .

HY-12646A

Rhosin	Ras Apoptosis	Cancer
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a K_d of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .

HY-108016

Peruvoside Encordin	Src PI3K JNK STAT EGFR Apoptosis Autophagy	Cancer
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .

HY-16663

ITX3 2 Publications Verification	ROCK Others	Others
ITX3 is a specific and nontoxic inhibitor of TrioN (N-terminal GEF domain of the multidomain Trio protein) with an IC₅₀ value of 76 μM. ITX3 can be used for the research of agent .

HY-117958

HJC0197 1 Publications Verification	Ras	Cardiovascular Disease Metabolic Disease Cancer
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 .

HY-114398

BAY-293 1 Publications Verification	Ras	Cancer
BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC₅₀ of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS .

HY-126247

BI-2852	Ras	Cancer
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

HY-107543

8-CPT-2Me-cAMP sodium	Ras	Others
8-CPT-2Me-cAMP sodium is a selective activator of exchange proteins activated by cAMP (Epac), the cAMP sensitive guanine nucleotide exchange factors (GEFs) for the small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium activates Epac1 (EC₅₀ = 2.2 μM), but not PKA (EC₅₀> 10 μM) . 8-CPT-2Me-cAMP sodium stimulates Epac-mediated Ca ²⁺ release in pancreatic β-cells in vitro .

HY-156002

LUNA18	Ras ERK	Cancer
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .

HY-126247B

(R)-BI-2852	Others	Cancer
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

Cat. No.	Product Name	Target	Research Area

HY-P1382A

Rac1 Inhibitor W56 TFA	Ras	Cancer
Rac1 Inhibitor W56 TFA is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 TFA inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam .

HY-156002

LUNA18	Ras ERK	Cancer
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .

HY-P1382

Rac1 Inhibitor W56	Ras	Cancer
Rac1 Inhibitor W56 is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam .

HY-P1383

Rac1 Inhibitor F56, control peptide	Peptides	Others
Rac1 Inhibitor F56, control peptide is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor F56, control peptide contains a Trp ⁵⁶ to Phe ⁵⁶ mutation. Rac1 Inhibitor F56, control peptide has no effect on Rac1 interaction with its guanine nucleotide exchange factors (GEFs) .

HY-P1383A

Rac1 Inhibitor F56, control peptide TFA	Peptides	Others
Rac1 Inhibitor F56, control peptide TFA is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor F56, control peptide TFA contains a Trp ⁵⁶ to Phe ⁵⁶ mutation. Rac1 Inhibitor F56, control peptide TFA has no effect on Rac1 interaction with its guanine nucleotide exchange factors (GEFs) .

Peruvoside Encordin	Apocynaceae Triterpenes Structural Classification Terpenoids Source classification Thevetia peruviana (Pers.) K. Schum. Plants	Src PI3K JNK STAT EGFR Apoptosis Autophagy
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .

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