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Results for "

GDP-bound

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Arf Family GTPase (1) Isotope-Labeled Compounds (2) JNK (1) p38 MAPK (1) Ras (10) α-synuclein (1)
By Research Areas:	Cancer (11) Neurological Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-130149

Adagrasib 35+ Cited Publications MRTX849	Ras	Cancer
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 .

HY-114277

Sotorasib Maximum Cited Publications 72 Publications Verification AMG-510	Ras	Cancer
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

HY-19706

ARS-853 4 Publications Verification	Ras Apoptosis	Cancer
ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC₅₀ of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .

HY-145928

Divarasib 3 Publications Verification GDC-6036	Ras	Cancer
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

HY-12873

RBC8	Ras p38 MAPK JNK	Cancer
RBC8 is a selective and allosteric RALA and RALB inhibitor. RBC8 stabilizes the inactive GDP-bound state of Ral, preventing its activation. RBC8 promotes the phosphorylation of proteins related to the MAPK/JNK pathway. RBC8 has the activity of inhibiting tumor cell proliferation, migration and invasion. RBC8 is used in the study of various cancers such as lung cancer, gastric cancer, and multiple myeloma .

HY-114277S

Sotorasib-d7 AMG-510-d₇	Isotope-Labeled Compounds Ras	Cancer
Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

HY-145928B

Divarasib adipate GDC-6036 adipate	Ras	Cancer
Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state .

HY-151999

KRAS G12C inhibitor 65	Ras	Cancer
KRAS G12C inhibitor 65 is a potent and covalent KRAS ^G12C inhibitor that traps KRAS ^G12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer .

HY-13868

SCH-53870	Ras	Cancer
SCH-53870 is a Ras activation inhibitor that binds to the Ras-GDP complex, keeping the Ras protein in an inactive GDP-bound state and preventing it from switching to an active GTP-bound state. SCH-53870 affects cell signaling and cell proliferation by preventing the activation of Ras protein. SCH-53870 can be used in cancer research .

HY-173350

Ran-IN-1	Arf Family GTPase	Cancer
Ran-IN-1 (Compound M36) is an orally active and selective Ran GTPase inhibitor. Ran-IN-1 binds to the GDP-bound form of Ran (RanGDP) at the allosteric switch II pocket with high specificity, stabilizing the inactive state and reducing the active Ran-GTP population. Ran-IN-1 induces apoptosis and represses DNA repair pathways like HR and NHEJ in epithelial ovarian cancer (EOC) cells. Ran-IN-1 is promising for research of EOC, particularly high-grade serous carcinoma .

HY-114277S2

Sotorasib-d3 AMG-510-d₃	Isotope-Labeled Compounds Ras	Cancer
Sotorasib-d₃ (AMG-510-d₃) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .

HY-110174

NAB2	α-synuclein	Neurological Disease
NAB2 is a neuroprotectant that targets the small GTPase Rab1a. NAB2 selectively binds to the GDP-bound form of Rab1a and protects multiple cell types from α-synuclein toxicity by increasing Rab1a expression. Rab1a regulates ER-to-Golgi trafficking and mediates endosomal trafficking events of the E3 ubiquitin ligase Rsp5/Nedd4. NAB2 stimulates ubiquitination of related proteins in a Nedd4-dependent manner and rescues α-synuclein-associated trafficking defects associated with early-onset Parkinson's disease .

Cat. No.	Product Name	Chemical Structure

HY-114277S

Sotorasib-d7
Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

Sotorasib-d7

Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

HY-114277S2

Sotorasib-d3
Sotorasib-d₃ (AMG-510-d₃) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .

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