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Ras

Ras inhibitors and related small GTPase modulators act on KRAS and on the Rac, Rho and Cdc42 proteins. Small GTPases of the Ras superfamily work as molecular switches. They cycle between an active form bound to guanosine triphosphate (GTP) and an inactive form bound to guanosine diphosphate (GDP). Oncogenic KRAS mutations such as G12C keep the protein in its signaling state. ARS-853 and KRas G12C inhibitor 4 target the mutant cysteine of KRAS G12C, while Kobe2602 interferes with binding of Ras to Raf. Salirasib, a farnesylcysteine mimetic, disrupts the membrane association of Ras. Rho-family tools include NSC 23766 and EHT 1864, which inhibit Rac, and CASIN, which targets Cdc42.

Cat. No.

A63686

CAS No.

1309252-99-0

Rho GTPase inhibitor 1

Rho GTPase Inhibitor 1 is a selective inhibitor targeting Rho GTPases, with demonstrated high affinity for Cdc42, Rac1, and RhoA, exhibiting KDs of 151, 352, and 232 μM, respectively. This compound effectively reduces cell migration in glioma cell lines, highlighting its potential utility in cancer research and therapeutic development. Its role in modulating Rho GTPase signaling makes it a valuable tool for investigating cellular processes such as motility and invasion.

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Cat. No.

A63688

CAS No.

3074833-87-4

KRAS-IN-48

KRAS-IN-48 is a selective inhibitor targeting KRAS mutations, exhibiting Kd values of 2.58 nM for the KRAS-G12D variant and 5.49 μM for KRAS-G12V. This compound demonstrates significant biological activity against KRAS mutant proteins, making it an important tool in cancer research. KRAS-IN-48 is particularly valuable for studies focused on understanding the role of KRAS mutations in tumorigenesis and therapeutic response.

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Cat. No.

A63689

CAS No.

2821863-70-9

KRAS G12C inhibitor 57

KRAS G12C Inhibitor 57 is a selective and covalent inhibitor targeting the KRAS G12C mutation, exhibiting an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assays. This compound effectively induces apoptosis in cancer cells, making it a valuable tool for studying KRAS-driven malignancies. Its oral bioavailability enhances its suitability for in vivo research applications focused on cancer therapeutics targeting KRAS mutations.

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Cat. No.

A63690

CAS No.

2648552-32-1

KRAS G12D inhibitor 6

KRAS G12D inhibitor 6 is a selective inhibitor targeting the KRAS G12D mutant, a significant oncogenic driver in various cancers. This compound demonstrates strong inhibitory activity that can facilitate the study of KRAS-mediated signaling pathways and tumor progression. It serves as a valuable tool in cancer research, particularly in developing targeted therapies against KRAS-driven malignancies.

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$795.00

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Cat. No.

A63691

CAS No.

3058573-95-5

KRAS inhibitor-37

KRAS Inhibitor-37 targets the KRAS protein, exhibiting high affinity with KDs of 0.004 nM, 0.041 nM, 0.019 nM, and 0.144 nM for KRAS wild type, G12D, G12C, and G12V variants, respectively, as determined by SPR binding assays. This compound demonstrates significant anti-proliferative activity, with IC50 values ranging from

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Cat. No.

A63692

CAS No.

3030078-96-4

KRAS inhibitor-35

KRAS Inhibitor-35 (compound 72) is a potent inhibitor of KRAS with an IC50 of 2 nM. It effectively disrupts KRAS signaling pathways, making it a valuable tool for studying tumor biology and the role of KRAS mutations in cancer research. This compound is suitable for various in vitro and in vivo applications aimed at exploring therapeutic strategies targeting KRAS-driven malignancies.

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25 mg

$2,410.00

50 mg

$3,100.00

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Cat. No.

A63693

CAS No.

2660129-56-4

KRAS G12C inhibitor 38

KRAS G12C inhibitor 38 is a selective inhibitor targeting the mutant form of KRAS G12C, an essential component of intracellular signaling pathways involved in cellular growth and proliferation. This compound exhibits significant anti-cancer activity and is primarily applied in research focused on KRAS G12C-driven malignancies. Its utilization can aid in the exploration and understanding of therapeutic strategies against cancers characterized by KRAS mutations.

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Cat. No.

A63695

CAS No.

2230873-66-0

KRAS inhibitor-18

KRAS inhibitor-18 is a selective inhibitor targeting the KRAS G12C mutation, demonstrating a potent inhibitory effect with an IC50 of 4.74 µM. This compound effectively inhibits phosphorylated ERK in MIA PaCA-2 and A549 cell lines, with IC50 values of 66.4 µM and 11.1 µM, respectively. KRAS inhibitor-18 is valuable for research applications in pancreatic, colorectal, and lung cancer studies, facilitating investigations into KRAS-driven tumorigenesis and potential therapeutic interventions.

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$1,275.00

50 mg

$1,625.00

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Cat. No.

A63698

CAS No.

1009376-10-6

RTIL 13

RTIL 13 is a selective inhibitor of dynamin GTPase, demonstrating an IC50 value of 2.3 μM for dynamin I. Additionally, it interacts with the pleckstrin homology lipid-binding domain. RTIL 13 effectively inhibits receptor-mediated endocytosis and synaptic vesicle endocytosis, with IC50 values of 9.3 μM and 7.1 μM, respectively. This compound is valuable for research focused on vesicle trafficking and cellular uptake mechanisms.

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5 mg

$795.00

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Cat. No.

A63700

CAS No.

3033641-67-4

KRAS-IN-42

KRAS-IN-42 is a covalent inhibitor specifically targeting KRASG12D mutants. This compound exhibits potent activity against KRASG12D-driven cancers, including non-small cell lung cancer and colorectal cancer. It is a valuable tool for researchers studying the molecular mechanisms and therapeutic options for KRASG12D-mutant oncogenesis.

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Cat. No.

A63702

CAS No.

2648808-69-7

KRAS G12C inhibitor 43

KRAS G12C inhibitor 43 is a selective inhibitor targeting the KRAS G12C mutation, a key driver in various cancers. It demonstrates significant anti-migration and anti-proliferative activities, with IC50 values ranging from 0.001 to 1 µM in H358, A549, and HCC cell lines. This compound holds potential for research applications focused on cancer progression and therapeutic development against KRAS-driven malignancies.

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25 mg

$1,275.00

50 mg

$1,625.00

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Cat. No.

A63703

CAS No.

3056974-50-3

KRAS-IN-41

KRAS-IN-41 is a potent inhibitor of the KRAS oncogene, exhibiting IC50 values of less than 0.01 μM against both KRAS G12D and KRAS G12V variants. This compound effectively inhibits the proliferation of RAS mutant cell lines, including GP2D and SW620, demonstrating its potential for therapeutic application. KRAS-IN-41 is suitable for use in cancer research, particularly in studies focused on targeting KRAS mutations.

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Cat. No.

A63705

CAS No.

2760354-12-7

KRAS G12C inhibitor 50

KRAS G12C Inhibitor 50 is a potent small molecule that selectively targets the KRAS G12C mutant protein, exhibiting an IC50 of 46.7 nM. This compound is instrumental in cancer research, particularly in studies focused on KRAS-driven tumors. Its ability to inhibit KRAS G12C activity makes it a valuable tool for investigating therapeutic strategies and potential treatments for malignancies associated with this mutation.

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25 mg

$1,800.00

50 mg

$2,285.00

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Cat. No.

A63706

CAS No.

3079342-05-2

KRAS-IN-47

KRAS-IN-47 is a potent inhibitor of the KRAS protein, specifically targeting the KRAS G12V mutant with an IC50 of less than 50 nM. This compound is valuable for research applications focused on understanding KRAS-driven cancers, providing insights into tumor biology and therapeutic resistance mechanisms. The inhibitor's efficacy in modulating KRAS activity makes it a critical tool for studying the role of this oncogene in cancer progression and treatment response.

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Cat. No.

A63707

CAS No.

2923669-28-5

KRAS G12D inhibitor 28

KRAS G12D inhibitor 28 selectively targets the KRAS G12D mutation, a common oncogenic driver in various cancers. This compound exhibits potent inhibitory activity, making it a valuable tool for studying KRAS-driven tumor biology and developing targeted therapies. Its application in cancer research aids in understanding the molecular mechanisms of KRAS mutations and their role in tumor progression.

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Cat. No.

A63708

CAS No.

2508134-76-5

KRAS G12C inhibitor 55

KRAS G12C inhibitor 55 is a selective inhibitor targeting the KRAS G12C mutant protein. This compound effectively disrupts KRAS signaling pathways, leading to inhibited cell proliferation in cancer models. It is primarily utilized in research focused on the development of targeted therapies for tumors harboring KRAS G12C mutations.

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Cat. No.

A63709

CAS No.

2762632-78-8

KRAS G12C inhibitor 51

KRAS G12C inhibitor 51 is a selective inhibitor targeting the mutant form of the KRAS protein, specifically the G12C variant. This compound exhibits significant biological activity in suppressing KRAS-driven signaling pathways, making it a valuable tool for cancer research, particularly in studies focused on tumors harboring KRAS G12C mutations. Its application extends to investigating therapeutic strategies and screening for potential drug candidates in KRAS-related malignancies.

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$1,800.00

50 mg

$2,285.00

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Cat. No.

A63711

CAS No.

1536470-92-4

SML-8-73-1

SML-8-73-1 is a nucleotide-based inhibitor targeting KRASG12C. This compound demonstrates significant efficacy in inhibiting the activity of KRASG12C, making it a valuable tool for research into non-small cell lung cancer (NSCLC). Its selective inhibition allows for the exploration of KRAS-related signaling pathways and contributes to the understanding of cancer progression and potential therapeutic interventions.

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Cat. No.

A63714

CAS No.

2319939-24-5

(S)-CCG-1423

(S)-CCG-1423 is a selective inhibitor of Rho signaling, effectively blocking the nuclear import of myocardin-related transcription factor A (MRTF-A). This compound reduces the nuclear accumulation of MRTF-A, leading to improved glucose uptake and enhanced glucose tolerance in insulin-resistant mouse models. (S)-CCG-1423 demonstrates superior inhibitory activity compared to its SR- and R-isomers, making it a valuable tool for research in the fields of cancer and diabetes.

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Cat. No.

A63715

CAS No.

2736599-72-5

KRAS G12C inhibitor 22

KRAS G12C inhibitor 22 selectively targets the mutant form of the KRAS protein, specifically the G12C variant. This compound demonstrates potent inhibition of KRAS G12C activity, making it a valuable tool for studying its role in cancer signaling pathways. It is primarily utilized in research focused on developing targeted therapies for KRAS-driven malignancies.

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25 mg

$1,275.00

50 mg

$1,625.00

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Cat. No.

A63716

CAS No.

2923669-20-7

INCB159020

INCB159020 is an orally active inhibitor targeting the KRAS G12D mutation, exhibiting a SPR value of 2.2 nM. It demonstrates significant antitumor activity, making it a valuable compound for research focused on cancers driven by KRAS G12D alterations. This reagent is primarily utilized in studies aimed at understanding the mechanisms of KRAS-related oncogenesis and evaluating potential therapeutic strategies.

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Cat. No.

A63720

CAS No.

2642135-72-4

Pan-RAS-IN-7

Pan-RAS-IN-7 is a pan RAS inhibitor that targets the RAS signaling pathway, crucial in cancer biology. This compound exhibits significant anti-tumor activity and is valuable for cancer research applications, particularly in the development of antibody-drug conjugates (ADCs). Its ability to inhibit various RAS isoforms makes it a versatile tool for studying RAS-mediated oncogenic processes.

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Cat. No.

A63724

CAS No.

2579083-99-9

KARS-IN-1

KARS-IN-1 is a potent inhibitor of lysyl-tRNA synthetase (KARS), specifically dependent on AKR1C3, with an AC50 of 9.1 nM for human KARS. This compound exhibits anti-proliferative effects in H460 cells, featuring high AKR1C3 expression, and in Hara cells, which have low AKR1C3 expression, with AC50 values of 21 nM and 16 nM, respectively. KARS-IN-1 is valuable for research focused on non-small cell lung cancer (NSCLC) and the therapeutic targeting of KARS in cancer biology.

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Cat. No.

A63726

CAS No.

2885961-55-5

pan-KRAS-IN-4

pan-KRAS-IN-4 is a highly potent KRAS inhibitor, demonstrating IC50 values of 0.37 nM for KRAS G12C and 0.19 nM for KRAS G12V. Its specific mechanistic action targets mutated KRAS proteins, making it a valuable tool for studying oncogenic signaling pathways. This compound is particularly relevant for research applications focused on cancer biology, therapeutic development, and the exploration of KRAS-related malignancies.

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Cat. No.

A63727

CAS No.

2749948-26-1

KRAS G12C inhibitor 34

KRAS G12C inhibitor 34 is a selective inhibitor targeting the KRAS G12C mutation, a common driver in various cancers. This compound demonstrates significant anticancer activity by disrupting KRAS signaling pathways, leading to reduced cell proliferation. It is suitable for research applications focusing on cancer biology, particularly in the development and evaluation of targeted therapies for KRAS-driven tumors.

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