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Results for "

KRAS G12 mutant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (4) AMPK (1) Apoptosis (14) Autophagy (1) Bcl-2 Family (1) Caspase (1) ERK (15) Galectin (1) IFNAR (4) Isotope-Labeled Compounds (4) MEK (2) Mitochondrial Metabolism (1) mTOR (3) p38 MAPK (4) PARP (1) PERK (4) Phosphatase (1) PI3K (3) PROTACs (4) Proton Pump (1) Raf (2) Ras (68) Reactive Oxygen Species (ROS) (3) Ribosomal S6 Kinase (RSK) (1) SOS1 (2) Tim3 (1) TNF Receptor (1)
By Research Areas:	Cancer (82) Inflammation/Immunology (3)
Click Chemistry:	Alkynes (6)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156819

Zoldonrasib 5 Publications Verification RMC-9805; KRAS G12D inhibitor 18	Ras Apoptosis	Cancer
Zoldonrasib (RMC-9805) is a potent and orally active **KRAS G12D inhibitor.Zoldonrasib induces apoptosis** in KRAS G12D mutant cancer cells. Zoldonrasib has the potential for the research of KRAS G12D mutant cancer .

HY-134813

MRTX1133 45+ Cited Publications	Ras	Cancer
MRTX1133 is a noncovalent, potent, and selective alkyne-based **KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D** against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .

HY-156498

RMC-7977 10+ Cited Publications	Ras ERK Raf Ribosomal S6 Kinase (RSK) AMPK Apoptosis PARP	Cancer
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (K_d = 195 nM) and KRAS (G12V) (K_d = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS ^G12C cancer models, and demonstrates good tolerability across various RAS cancer models .

HY-153724

BI-2865 10+ Cited Publications	Ras	Cancer
BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with K_Ds of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC₅₀: roughly 140 nM) .

HY-153346

Elironrasib 2 Publications Verification RMC-6291	Ras ERK Apoptosis	Cancer
Elironrasib is an orally active and covalent inhibitor of KRAS ^G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS ^G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS ^G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS ^G12C mutant cells with a median IC₅₀ of 0.11 nM .

HY-173629

RMC-5127	Ras Apoptosis	Cancer
RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS ^G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS ^G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS ^G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS ^G12V tumors .

HY-132844

Tunlametinib HL-085	MEK	Cancer
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC₅₀=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .

HY-176523

KRAS G12D-IN-29	Ras	Cancer
KRAS G12D inhibitor 29 (Compound Formula (I)) is an orally active and selective KRAS ^G12D mutant inhibitor. KRAS G12D inhibitor 29 blocks downstream signaling pathways mediated by KRAS ^G12D, suppressing tumor cell proliferation. KRAS G12D inhibitor 29 is promising for research of KRAS ^G12D mutation-related cancers (such as pancreatic cancer, lung cancer, colorectal cancer) .

HY-114277A

Sotorasib racemate 1 Publications Verification AMG-510 racemate	Ras p38 MAPK	Cancer
Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of **KRAS G12C mutant which induces adaptive feedback activation of MAPK** pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .

HY-162960

pan-KRAS-IN-18	Ras	Cancer
pan-KRAS-IN-18 is a panKRAS inhibitor that inhibits KRAS WT and **KRAS G12V with IC₅₀*s of 29 and 9 nM, respectively. pan-KRAS-IN-18 exhibits antiproliferative activity in KRAS-mutant* cell lines. pan-KRAS-IN-18 can be used for lung cancer research .

HY-128522

ARS-1323-alkyne	Ras	Cancer
ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .

HY-160023

Elisrasib D3S-001	Ras PERK	Cancer
Elisrasib (D3S-001) is an orally active and selective inhibitor for *KRAS. Elisrasib inhibits the proliferation of KRAS* ^G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .

HY-164315

KRAS G12C inhibitor 67	Ras PERK	Cancer
KRAS G12C inhibitor 67 (Example 35) is an orally active **KRAS G12C** inhibitor. KRAS G12C inhibitor 67 inhibits pERK and active KRas. KRAS G12C inhibitor 67 selectively inhibits the growth of various KRAS G12C mutant tumor cell lines. KRAS G12C inhibitor 67 exhibits anticancer activity against esophageal cancer, bladder cancer, colorectal cancer, lung cancer, and pancreatic cancer .

HY-156671

RMC-4998	Ras PI3K ERK mTOR Apoptosis	Cancer
RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS ^G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS ^G12C mutant, with an IC₅₀ value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS ^G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .

HY-161176

PROTAC KRAS G12D degrader 1	PROTACs Ras ERK	Cancer
PROTAC KRAS G12D degrader 1 is a selective PROTAC KRAS ^G12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRAS ^G12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRAS ^G12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)) .

HY-154959

AZD4747	Ras	Cancer
AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS ^G12C inhibitor. AZD4747 has the potential to study cancer .

HY-19706

ARS-853 5 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-176954

RSC-1255	Proton Pump Ras Autophagy Apoptosis	Cancer
RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a K_d = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRAS ^G13D and KRAS ^G12V cells. RSC-1255 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers .

HY-177511

KRAS G12D-IN-30	Ras p38 MAPK Raf MEK ERK	Cancer
KRAS G12D-IN-30 (Compound 4) is a *KRAS* inhibitor. KRAS G12D-IN-30 inhibits the activation of the downstream MAPK signaling cascade (Raf1-MEK-ERK) by blocking the activity of the KRAS G12 mutant. KRAS G12D-IN-30 can be used for the research of cancer .

HY-153663

TH-Z827	Ras	Cancer
TH-Z827 is a mutant selective *KRAS(G12D)* inhibitor with an IC₅₀ of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC₅₀ value of 42 μM .

HY-175870

Eras-4001	Ras	Cancer
Eras-4001 (Compound 14-1) is a pan-KRAS inhibitor. Eras-4001 has potent antitumor activities and significantly inhibits the proliferation of wild-type and mutant (such as KRAS ^G12D, KRAS ^G12V and KRAS ^G12C) cancer cells. Eras-4001 effectively inhibits tumor growth in GP2D and Panc0403 xenograft mouse models .

HY-176792

ACBI-4	PROTACs Ras	Cancer
ACBI-4 is a selective GTP-loaded active state of *KRAS* (KRAS(on)) PROTAC degrader, with K_d values of 141 nM against KRAS ^G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .

HY-146243

TH-Z835	Ras Apoptosis	Cancer
TH-Z835 is a mutant selective **KRAS (G12D) inhibitor with an IC₅₀** of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange .

HY-122862

RAS inhibitor Abd-7 3 Publications Verification	Ras	Cancer
RAS inhibitor Abd-7, a potent RAS-binding compound (K_d=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .

HY-151523

KRas G12R inhibitor 1	Ras	Cancer
KRas G12R inhibitor 1 is a covalent inhibitor targeting the common oncogenic mutant **KRas G12R** with selectivity for the mutant arginine. KRas G12R inhibitor 1 possesses an α,β-diketoamide and exploits strong nucleophilicity of the mutant cysteine and irreversibly binds in the Switch II region of KRas. KRas G12R inhibitor 1 can be researched for K-Ras (G12R)-driven cancer such as pancreatic ductal adenocarcinoma (PDAC) .

HY-156529

pan-KRAS-IN-2	Ras	Cancer
pan-KRAS-IN-2 (Compound 6) is a pan-inhibitor with IC₅₀s ≤ 10 nM for KRAS WT and mutants (G12D, *G12C, G12V, G12S, G12A* and Q61H); and an IC₅₀ > 10 μM for KRAS G13D. pan-KRAS-IN-2 can be used to study various KRAS-mediated cancers, such as pancreatic cancer and colorectal cancer .

HY-122914

KRAS inhibitor-3 1 Publications Verification	Ras	Cancer
KRAS inhibitor-3 is an inhibitor of *KRAS* inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (K_D: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .

HY-178042

SS-3091	Ras Akt ERK	Cancer
SS-3091 is a pan-KRas inhibitor active across KRas ^G12D, KRas ^G12C, KRas ^G12V, KRas ^G12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRas ^G12 mutations. SS-3091 can be used for the research of KRas-driven cancers .

HY-U00416

ARS-1323	Ras	Cancer
ARS-1323 is a **KRAS G12C** inhibitor. ARS-1323 specifically binds to the cysteine residue on the mutant K-Ras protein, locks it in the GDP-bound conformation, thereby blocking K-Ras activation and downstream signaling pathways. ARS-1323 can be used to investigate the signal transduction mechanisms and growth characteristics of tumor cells driven by K-Ras G12C .

HY-P2265A

SAH-SOS1A TFA	SOS1 Ras	Cancer
SAH-SOS1A TFA is a peptide-based *SOS1/KRAS* protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-P5192

KRAS G12D(8-16)	Ras	Cancer
KRAS G12D 8-16 is a mutant KRAS G12D 8-16 peptide .

HY-156671A

RMC-4998 formic	Ras PI3K ERK mTOR Apoptosis	Cancer
RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS ^G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS ^G12C mutant, with an IC₅₀ value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS ^G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for non-small cell lung cancer (NSCLC) research .

HY-159591

YK-8S	Ras Akt ERK	Cancer
YK-8S is a dual-targeted **K-Ras (G12D/G12C)** covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .

HY-175025

CH091138	PROTACs Ras Apoptosis	Cancer
CH091138 is a potent and selective KRASG12D PROTAC degrader with DC₅₀s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS ^WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .

HY-P11356

KRAS G12V Peptide	IFNAR	Cancer
KRAS G12V Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12V oncogenic mutation. KRAS G12V Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12V Peptide can be used for the study of immune responses against KRAS G12V-mutant tumors .

HY-P11357A

KRAS G12C Peptide TFA	IFNAR	Cancer
KRAS G12C Peptide TFA is the trifluoroacetate salt of KRAS G12C Peptide (HY-P11357). KRAS G12C Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12C oncogenic mutation. KRAS G12C Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12C Peptide can be used for the study of immune responses against KRAS G12C-mutant tumors .

HY-P11356A

KRAS G12V Peptide TFA	IFNAR	Cancer
KRAS G12V Peptide TFA is the trifluoroacetate salt of KRAS G12V Peptide (HY-P11355). KRAS G12V Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12V oncogenic mutation. KRAS G12V Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12V Peptide can be used for the study of immune responses against KRAS G12V-mutant tumors .

HY-179300A

KRAS-IN-48	Ras	Cancer
KRAS-IN-48 (Compound 1-01) is a *KRAS* mutant inhibitor, with K_d values of 2.58 nM and 5.49 μM for KRAS-G12D and KRAS-G12V, respectively. KRAS-IN-48 can be used in the research of cancer .

HY-174261

KRAS-IN-5	Ras	Cancer
KRAS-IN-5 (Compound Ex 6) is an orally active and selective inhibitor targeting *KRAS* mutants (including KRAS ^G12D, KRAS ^G12V, KRAS ^WT) with a GNE IC₅₀ value of 1.3 nM against KRAS ^G12D. KRAS-IN-5 blocks tumor cell proliferation by inhibiting KRAS-mediated signaling pathways (e.g., reducing ERK phosphorylation). KRAS-IN-5 is promising for research of KRAS mutation-related cancers, such as pancreatic cancer, colorectal cancer, lung cancer .

HY-P2265

SAH-SOS1A	SOS1 Ras	Cancer
SAH-SOS1A is a peptide-based *SOS1/KRAS* protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-179403

KRASG12C IN-17	Ras	Cancer
KRASG12C IN-17 is an orally active covalent KRAS ^G12C inhibitor, showing strong inhibitory activity in KRAS ^G12C-mutant cancer cells (NCI-H23 IC₅₀ = 0.7 nM; NCI-H358 IC₅₀ = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRAS ^G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .

HY-U00417

ARS-1630 1 Publications Verification	Ras	Cancer
ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of **mutant K-ras G12C** extracted from patent WO 2015054572 A1.

HY-178497

ZJK-807	PROTACs Ras p38 MAPK TNF Receptor	Inflammation/Immunology Cancer
ZJK-807 is a highly effective and selective PROTAC degrader targeting KRAS^G12D (DC₅₀ = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type *KRAS* or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRAS^G12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506) .

HY-154959A

(9R,12aR)-AZD4747	Ras	Cancer
(9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRAS ^G12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer .

HY-176870

KRAS-IN-42	Ras	Cancer
KRAS-IN-42 (Compound Z1063) is a covalent **KRAS ^G12D mutants** inhibitor. KRAS-IN-42 is promising for research of KRAS ^G12D-mutant cancers (e.g., non-small cell lung cancer, colorectal cancer) .

HY-18606

K-Ras G12C-IN-3	Ras	Cancer
K-Ras G12C-IN-3 (Compound VI-5) is an irreversible small molecule inhibitor of mutant **K-Ras G12C*. K-Ras* G12C-IN-3 can be used in the research of cancers .

HY-18604

K-Ras G12C-IN-1 1 Publications Verification	Ras	Cancer
K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.

HY-173329

KRAS-IN-41	Ras	Cancer
KRAS-IN-41 is an inhibitor of *KRAS* with IC₅₀ values of <0.01 μM for KRAS G12D and KRAS G12V. KRAS-IN-41 inhibits RAS mutant cell lines, GP2D (KRAS-G12D) and SW620 (KRAS-G12V). KRAS-IN-41 can be used in cancer research .

HY-P11357

KRAS G12C Peptide	IFNAR	Cancer
KRAS G12C Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12C oncogenic mutation. KRAS G12C Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12C Peptide can be used for the study of immune responses against KRAS G12C-mutant tumors .

HY-162440

pan-KRAS-IN-7	Ras	Cancer
pan-KRAS-IN-7 (Compound 25) is an inhibitor for in human tumor mutated genes *KRAS, which inhibits proliferation of KRAS* mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC₅₀ of 0.35 and 0.51 nM, respectively .

Cat. No.	Product Name

HY-L260

KRAS Targeted Compound Library

0 compounds

KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) is one of the most important oncogenic driver genes in oncology, with high mutation frequencies in pancreatic cancer, non‑small cell lung cancer, and colorectal cancer. For a long time, KRAS was considered "undruggable" due to the lack of suitable small‑molecule binding pockets on its protein surface. In recent years, with the discovery of the switch‑II pocket and the successful approval of KRAS G12C inhibitors, KRAS‑targeted research has achieved groundbreaking progress, which has also spurred a wave of development targeting non‑G12C mutants such as G12D and G12V, as well as upstream and downstream regulatory factors including SOS1 and SHP2.

MCE KRAS Targeted Compound Library contains 0 small‑molecule compounds targeting the KRAS, serving as high‑quality research tools for mechanistic studies of KRAS‑mutant tumors, combination therapy development, resistance mechanism exploration, and high‑throughput drug screening, thereby providing robust support for KRAS‑targeted drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-P2265A

SAH-SOS1A TFA	SOS1 Ras	Cancer
SAH-SOS1A TFA is a peptide-based *SOS1/KRAS* protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-P5192

KRAS G12D(8-16)	Ras	Cancer
KRAS G12D 8-16 is a mutant KRAS G12D 8-16 peptide .

HY-P3488

GADGVGKSA	Peptides	Inflammation/Immunology Cancer
GADGVGKSA is a mutant KRAS G12D 9mer peptide. GADGVGKSA can be used as an immunogenic neoantigen for cancer immunotherapy research .

HY-P11356

KRAS G12V Peptide	IFNAR	Cancer
KRAS G12V Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12V oncogenic mutation. KRAS G12V Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12V Peptide can be used for the study of immune responses against KRAS G12V-mutant tumors .

HY-P11357A

KRAS G12C Peptide TFA	IFNAR	Cancer
KRAS G12C Peptide TFA is the trifluoroacetate salt of KRAS G12C Peptide (HY-P11357). KRAS G12C Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12C oncogenic mutation. KRAS G12C Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12C Peptide can be used for the study of immune responses against KRAS G12C-mutant tumors .

HY-P11356A

KRAS G12V Peptide TFA	IFNAR	Cancer
KRAS G12V Peptide TFA is the trifluoroacetate salt of KRAS G12V Peptide (HY-P11355). KRAS G12V Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12V oncogenic mutation. KRAS G12V Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12V Peptide can be used for the study of immune responses against KRAS G12V-mutant tumors .

HY-P2265

SAH-SOS1A	SOS1 Ras	Cancer
SAH-SOS1A is a peptide-based *SOS1/KRAS* protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-P3486

GADGVGKSAL	Peptides	Inflammation/Immunology Cancer
GADGVGKSAL is a mutant KRAS G12D 10mer peptide. GADGVGKSAL can be used as an immunogenic neoantigen for cancer immunotherapy research .

HY-P11357

KRAS G12C Peptide	IFNAR	Cancer
KRAS G12C Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12C oncogenic mutation. KRAS G12C Peptide induces responses like IFN-γ secretion and cytotoxicity. KRAS G12C Peptide can be used for the study of immune responses against KRAS G12C-mutant tumors .

Cat. No.	Product Name	Target	Research Area	Image

HY-P992366

HFB200901	Galectin Tim3	Cancer
HFB200901 is a galectin LGALS9 inhibitor and immunostimulant that can be used in studies related to pancreatic adenocarcinoma, pancreatic intraepithelial neoplasia, KRAS ^G12C-mutant colon cancer, and prostate cancer. HFB200901 disrupts the LGALS9/TIM-3 axis, while blocking the internalization and vacuolization of recombinant LGALS9. HFB200901 reduces the proportion of regulatory T cells (Treg) and enhances dendritic cell activation, thereby inducing polyfunctional and memory CD8 ⁺ T cell responses. HFB200901 inhibits the progression of pancreatic neoplastic lesions and effectively improves the efficacy of PSMA-based vaccination .

Cat. No.	Product Name	Chemical Structure

HY-176358S

KRAS 2B G12C mutant, Arg-13C6,15N4, Lys-13C6,15N2
KRAS 2B G12C mutant, Arg- ¹³C₃₆, ¹⁵N₄, Lys- ¹³C₆, ¹⁵N₂ is the ¹³C- and ¹⁵N-labeled KRAS 2B G12C mutant.

HY-176359S

KRAS 2B G12D mutant, Arg-13C6,15N4, Lys-13C6,15N2
KRAS 2B G12D mutant, Arg- ¹³C₃₆, ¹⁵N₄, Lys- ¹³C₆, ¹⁵N₂ is the ¹³C- and ¹⁵N-labeled KRAS 2B G12D mutant.

HY-176354S

KRAS 2B G12V mutant, Arg-13C6,15N4, Lys-13C6,15N2
KRAS 2B G12V mutant, Arg- ¹³C₃₆, ¹⁵N₄, Lys- ¹³C₆, ¹⁵N₂ is the ¹³C- and ¹⁵N-labeled KRAS 2B G12V mutant.

HY-176357S

KRAS 2B G12R mutant, Arg-13C6,15N4, Lys-13C6,15N2
KRAS 2B G12R mutant, Arg- ¹³C₃₆, ¹⁵N₄, Lys- ¹³C₆, ¹⁵N₂ is the ¹³C- and ¹⁵N-labeled KRAS 2B G12R mutant.

HY-180885S

KRAS G12D-IN-35

KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .

Cat. No.	Product Name		Classification

HY-134813

MRTX1133 45+ Cited Publications		Alkynes
MRTX1133 is a noncovalent, potent, and selective alkyne-based **KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D** against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .

HY-128522

ARS-1323-alkyne		Alkynes
ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .

HY-179300A

KRAS-IN-48		Alkynes
KRAS-IN-48 (Compound 1-01) is a *KRAS* mutant inhibitor, with K_d values of 2.58 nM and 5.49 μM for KRAS-G12D and KRAS-G12V, respectively. KRAS-IN-48 can be used in the research of cancer .

HY-179403

KRASG12C IN-17		Alkynes
KRASG12C IN-17 is an orally active covalent KRAS ^G12C inhibitor, showing strong inhibitory activity in KRAS ^G12C-mutant cancer cells (NCI-H23 IC₅₀ = 0.7 nM; NCI-H358 IC₅₀ = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRAS ^G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .

HY-176870

KRAS-IN-42		Alkynes
KRAS-IN-42 (Compound Z1063) is a covalent **KRAS ^G12D mutants** inhibitor. KRAS-IN-42 is promising for research of KRAS ^G12D-mutant cancers (e.g., non-small cell lung cancer, colorectal cancer) .

HY-179300

KRAS-IN-48 free base		Alkynes
KRAS-IN-48 free base (Compound 1-01) is a mutant *KRAS* inhibitor, with K_d values of 2.58 nM and 5.49 μM for KRAS G12D and KRAS G12V, respectively. KRAS-IN-48 free base affects pERK expression in cells harboring KRAS G12D and KRAS G12V mutations, with IC₅₀ values of 1.1 μM and 1.51 μM, respectively. KRAS-IN-48 free base can be used in the research of cancer .

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