Ras

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.

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.

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.

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.

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.

A63527

CAS No.

10161-87-2

KRA-533

KRA-533 is a potent KRAS agonist that selectively binds to the GTP/GDP binding pocket of the KRAS protein. This interaction inhibits GTP cleavage, leading to the accumulation of constitutively active GTP-bound KRAS. Consequently, KRA-533 induces both apoptotic and autophagic cell death pathways in cancer cells, making it a valuable tool for research into cancer biology and therapeutic strategies targeting KRAS signaling.

Cat. No.

A63539

CAS No.

868145-09-9

I942

I942 is a selective non-cyclic nucleotide (NCN) agonist of EPAC1. It effectively modulates proinflammatory cytokine signaling pathways associated with various cardiovascular diseases. This compound serves as a valuable tool in research focused on understanding EPAC1-related mechanisms and developing therapeutic strategies for inflammatory cardiovascular conditions.

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.

A63669

CAS No.

905794-70-9

K-Ras-IN-2

K-Ras-IN-2 is a selective antagonist of the K-Ras protein. It has demonstrated significant biological activity in inhibiting K-Ras-driven signaling pathways, making it a valuable tool for researchers studying tumor biology and oncogenic signaling. This compound is particularly useful in cancer research applications focused on K-Ras-related malignancies.

Cat. No.

A63730

CAS No.

3097973-97-9

(R)-ACBI-4

(R)-ACBI-4 is a selective PROTAC degrader targeting the GTP-loaded active state of KRAS (KRAS(on)). It exhibits notable anti-proliferative activity and effectively degrades various KRAS mutants, including KRASG12R, in cancer cell lines. This compound is utilized in research focused on understanding KRAS-driven oncogenesis and therapeutic interventions in KRAS-related cancers.

Cat. No.

A63794

CAS No.

612513-15-2

8-pHPT-2'-O-Me-cAMP

Synonyms: 8-(4-Hydroxyphenylthio)-2'-O-Me-cAMP

8-pHPT-2'-O-Me-cAMP is a cAMP analog that acts as an Epac agonist, specifically enhancing the activity of the exchange protein activated by cyclic AMP (Epac). This compound is utilized in cardiac research to explore signaling mechanisms and cellular responses associated with cardiac function and pathophysiology. Its ability to modulate Epac pathways makes it a valuable tool for investigating the roles of cAMP in cardiac health and disease.

Cat. No.

A63809

CAS No.

1801911-86-3

NY-0173

NY-0173 is an antagonist of exchange proteins directly activated by cAMP (EPAC), demonstrating IC50 values of 3.5 μM for EPAC2 and 4.0 μM for EPAC1. This reagent serves as a valuable tool for investigating the biological roles and pathways mediated by EPAC. Researchers can utilize NY-0173 to explore its impact on cellular processes influenced by EPAC signaling.