Ras

Cat. No.

A15925

CAS No.

878978-76-8

ML-098

Synonyms: CID-7345532

ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM).

Cat. No.

A16231

CAS No.

2002381-25-9

APS-2-79

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.

Cat. No.

A20067

CAS No.

143703-25-7

CE3F4

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.

Cat. No.

A20284

CAS No.

292168-79-7

KY1220

KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.

Cat. No.

A23920

CAS No.

2378258-52-5

PROTAC K-Ras Degrader-1

PROTAC K-Ras Degrader-1 (Compound 518) is a cereblon-based PROTAC that selectively degrades K-Ras, achieving ≥70% degradation efficiency in SW1573 cells. It serves as a valuable tool for studying K-Ras-driven signaling pathways and potential therapeutic strategies in cancer research.

Cat. No.

A23933

CAS No.

2502156-03-6

LC-2

LC-2 is a first-in-class, VHL-based PROTAC designed to degrade endogenous KRAS G12C. Incorporating a MRTX849-derived covalent warhead, LC-2 binds KRAS G12C and recruits the VHL E3 ligase, inducing rapid and sustained degradation with DC₅₀ values between 0.25 and 0.76 μM. It effectively suppresses MAPK signaling in both homozygous and heterozygous KRAS G12C mutant cell lines, making it a valuable tool for targeted cancer research.

Cat. No.

A23987

PROTAC SOS1 degrader-1 TFA

PROTAC SOS1 Degrader-1 (TFA) is a potent PROTAC molecule targeting SOS1, with a DC₅₀ of 98.4 nM. It exhibits antiproliferative activity in cancer cells harboring various KRAS mutations and demonstrates antitumor efficacy with low toxicity, making it a promising candidate for targeted cancer therapy research.

Cat. No.

A24225

CAS No.

496775-95-2

ML-099 (CID-888706)

Synonyms: CID-888706

ML-099 (CID-888706) is a pan Ras-related GTPase activator that promotes the activation of multiple small GTPases, including Rac1, Cdc42, Ras, Rab7, and Rab2A. It serves as a useful tool for studying the regulation and function of Ras-related GTPase signaling pathways.

Cat. No.

A24569

CAS No.

2245237-53-8

VUBI1 (SOS1 activator 1)

Synonyms: SOS1 activator 1

VUBI1 (SOS1 Activator 1) is a benzimidazole-derived small molecule that acts as a potent activator of the guanine nucleotide exchange factor SOS1, with a dissociation constant (Kᴅ) of 44 nM. It promotes RAS activation by enhancing RAS-GTP formation and modulates downstream ERK phosphorylation, thereby influencing RAS–MAPK signaling. In addition, VUBI1 serves as a functional ligand for the development of PROTAC-based degraders, such as PROTAC SOS1 Degrader-1, to induce targeted SOS1 degradation. VUBI1 is a valuable compound for studying RAS pathway regulation and its role in cancer biology.

Cat. No.

A24573

CAS No.

301177-43-5

ESI-08

ESI-08 is a potent and selective antagonist of exchange proteins directly activated by cAMP (EPACs). It inhibits both EPAC1 and EPAC2 with an IC₅₀ of 8.4 μM, effectively blocking cAMP-induced EPAC activation while sparing cAMP-mediated protein kinase A (PKA) signaling. By selectively disrupting EPAC-dependent pathways, ESI-08 serves as a valuable tool compound for dissecting cAMP signaling mechanisms and studying EPAC-related physiological and pathological processes.

Cat. No.

A24683

CAS No.

1383539-73-8

HJC0197

HJC0197 is a selective antagonist of Epac1 and Epac2, exhibiting an IC50 of 5.9 μM for Epac2. This compound effectively inhibits cAMP-induced activation of Epac, demonstrating a capacity to block Epac1-mediated Rap1-GDP exchange activity at a concentration of 25 μM in the presence of a corresponding concentration of cAMP. HJC0197 serves as a valuable tool for investigating the role of Epac proteins in cellular signaling pathways and cAMP-mediated biological processes.

Cat. No.

A24693

CAS No.

2821793-99-9

Setidegrasib

Synonyms: ASP-3082; KRAS G12D inhibitor 17

Setidegrasib is a PROTAC degrader specifically targeting the KRAS G12D mutation with a DC50 of 37 nM. This compound effectively induces the degradation of KRAS G12D protein, leading to the suppression of key signaling molecules such as p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates significant anti-tumor activity across various cancer xenograft models, making it a valuable tool for studying KRAS(G12D)-mutated solid tumors.

Cat. No.

A24695

CAS No.

2938169-76-5

ACBI3

ACBI3 is a PROTAC designed to target KRAS, employing a unique mechanism to induce degradation of this oncogenic protein. It comprises a pan-KRAS degrader linked to an E3 ligase ligand through a specialized linker, facilitating the recruitment of the proteasome for degradation. ACBI3 has demonstrated significant biological activity by achieving durable modulation of signaling pathways and promoting tumor regression in KRAS mutant xenograft mouse models, making it a valuable tool for research into cancer therapeutics aimed at KRAS-driven malignancies.

Cat. No.

A24723

CAS No.

3033583-54-6

PROTAC KRAS G12D degrader 1

PROTAC KRAS G12D degrader 1 functions as a selective PROTAC targeting the KRAS G12D mutant by promoting its degradation. This compound effectively inhibits the proliferation of KRAS G12D-mutant cell lines and suppresses phosphorylation of ERK, a critical pathway in cancer signaling. In vivo studies demonstrate its ability to impede tumor growth in mice with AsPC-1 xenografts, making it a valuable tool for research into KRAS G12D-driven cancers.

Cat. No.

A24805

CAS No.

74805-91-7

Methylophiopogonanone B

Methylophiopogonanone B is a homoisoflavonoid that serves as a Ras activator. Isolated from the root of Ophiopogon japonicus, it exhibits potent antioxidant properties. This compound enhances GTP-Rho levels and activates the Rho signaling pathway, thereby inducing morphological changes in cells, such as actin cytoskeletal reorganization, dendrite retraction, and stress fiber formation. It is a valuable reagent for research into cellular signaling and structural dynamics.

Cat. No.

A24811

CAS No.

743456-83-9

ML-097

Synonyms: CID-2160985

ML-097 is a potent activator of Ras-related GTPases, specifically targeting Rac1, CDC42, Ras, and Rab7. It plays a critical role in modulating cellular signaling pathways associated with proliferation, migration, and cytoskeletal organization. This compound is valuable for research applications focusing on cancer biology, neurobiology, and cellular communication mechanisms.

Cat. No.

A24815

CAS No.

634207-53-7

8-pCPT-2′-O-Me-cAMP sodium

Synonyms: 8-CPT-2'-O-Me-cAMP sodium

8-pCPT-2′-O-Me-cAMP sodium is an analog of cyclic AMP that serves as a selective activator of exchange proteins activated by cAMP (Epac). This compound demonstrates effective activation of Epac1 with an EC50 value of 2.2 μM, while showing minimal activity towards protein kinase A (EC50 >10 μM). In vitro studies highlight its role in stimulating Epac-mediated Ca2+ release in pancreatic β-cells, and it functions as an activator of Rap1. Additionally, 8-pCPT-2′-O-Me-cAMP sodium has been shown to strengthen the barrier of retinal pigment epithelium against pathological choroidal endothelial cell invasion, contributing to research on macular degeneration.

Cat. No.

A24830

CAS No.

2984236-79-3

PROTAC KRAS G12C degrader-1

PROTAC KRAS G12C degrader-1 is a Cereblon-based PROTAC targeting the KRAS G12C mutant. This compound promotes the formation of a dimer between Cereblon and KRAS G12C, leading to the degradation of GFP-tagged KRAS G12C in reporter cell systems. It serves as a valuable tool for research on targeted degradation strategies in KRAS-driven cancers.

Cat. No.

A36686

CAS No.

3052745-16-8

PROTAC K-Ras Degrader-5

PROTAC K-Ras Degrader-5 is a cereblon-based PROTAC specifically designed to target KRASG12D, achieving a DC50 of less than 100 nM. This reagent facilitates the recruitment of KRASG12D to the cereblon E3 ubiquitin ligase complex, leading to its ubiquitination and proteasomal degradation. As a result, it effectively reduces pERK levels and inhibits the proliferation of cancer cells. PROTAC K-Ras Degrader-5 also enhances caspase 3/7 activity and cleaved PARP levels, indicative of apoptosis, in pancreatic cancer models. This compound is a valuable tool for researching both pancreatic and colorectal cancer.

Cat. No.

A37215

CAS No.

59212-44-1

8-HA-cAMP

Synonyms: 8-Hexylamino-cAMP

8-HA-cAMP is a membrane-permeable analogue of cyclic adenosine monophosphate (cAMP) that acts as an activator of cAMP-dependent protein kinase (PKA). Its structure confers metabolic stability against mammalian phosphodiesterases that respond to cyclic nucleotides. This compound is useful in studying PKA signaling pathways and their associated biological processes.

Cat. No.

A40763

CAS No.

3104382-00-2

MCB-36

MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment.

Cat. No.

A63557

CAS No.

2378257-72-6

PROTAC KRAS G12C degrader-2

PROTAC KRAS G12C degrader-2 is a bifunctional molecule that targets the KRAS G12C mutant protein for degradation via the proteasome. It features a cereblon inhibitor that modulates the activity of inhibitors of apoptosis proteins (IAPs) to facilitate the targeted destruction of KRAS. This reagent is valuable for research applications aimed at elucidating the role of KRAS in cancer biology and developing effective targeted therapies for KRAS-driven malignancies.

Cat. No.

A63602

CAS No.

2706637-43-4

(Rac)-D3S-001

(Rac)-D3S-001 is a racemic mixture of the compound D3S-001, which serves as a potent modulator of specific biological pathways. This compound exhibits significant activity in regulating cellular processes, making it a valuable tool for investigating the underlying mechanisms of disease. It is particularly useful in pharmacological studies and in the development of therapeutic strategies targeting related biological systems.

Cat. No.

A63619

CAS No.

663941-66-0

8-CPT-cAMP-AM

Synonyms: 8-(4-Chlorophenylthio)-cAMP-AM

8-CPT-cAMP-AM is a membrane-permeant analogue of cyclic adenosine monophosphate (cAMP) that acts as an activator of cAMP- and cGMP-dependent protein kinases. It also stimulates exchange protein directly activated by cAMP (Epac), making it a valuable tool for investigating cAMP signaling pathways. This compound is useful in research applications studying cellular processes influenced by cAMP, such as cell proliferation, differentiation, and effects on various physiological responses.

Cat. No.

A63650

CAS No.

1579978-17-8

RAS activator compound 1

RAS Activator Compound 1 is a specific activator targeting the guanine nucleotide exchange factor, son of sevenless homologue 1 (SOS1). This compound effectively facilitates the nucleotide exchange process, leading to increased levels of active RAS-GTP in HeLa cells. RAS Activator Compound 1 is valuable for research focused on RAS-driven tumors, providing insights into the mechanisms of RAS activation and its role in cancer biology.