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Results for "

KRAS mutant cancer

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (10) AMPK (1) Apoptosis (17) ATTECs (1) Autophagy (6) Bcl-2 Family (1) c-Myc (1) Calcium Channel (3) Caspase (2) CDK (2) Cyclophilin (1) Discoidin Domain Receptor (1) Drug Isomer (1) Early 2 Factor (E2F) (1) EGFR (3) ERK (21) Galectin (1) Isotope-Labeled Compounds (1) Ligands for Target Protein for PROTAC (1) MAPKAPK2 (MK2) (1) MDM-2/p53 (1) MEK (4) Mitochondrial Metabolism (2) Mitosis (1) Molecular Glues (1) mTOR (3) NAMPT (1) NEKs (1) p38 MAPK (6) PARP (2) PDK-1 (1) PERK (6) Phosphatase (1) Phosphodiesterase (PDE) (4) PI3K (7) Polo-like Kinase (PLK) (1) PROTACs (7) Proton Pump (1) Raf (9) Ras (79) Reactive Oxygen Species (ROS) (4) Reference Standards (1) Ribosomal S6 Kinase (RSK) (1) SHP2 (1) SOS1 (6) STING (3) Tim3 (1) TNF Receptor (2) ULK (1) β-catenin (1)
By Research Areas:	Cancer (108) Cardiovascular Disease (3) Infection (3) Inflammation/Immunology (3)
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106

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: BCRP

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-156498

RMC-7977 Maximum Cited Publications 14 Publications Verification	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-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-158115

NST-628	Molecular Glues Raf MEK	Cancer
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant 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-162960

pan-KRAS-IN-18	Ras	Cancer
pan-KRAS-IN-18 is a panKRAS inhibitor that inhibits KRAS WT and KRAS G12V with IC₅₀s 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-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-173405

VVD-699	Ras PI3K Akt	Cancer
VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC₅₀: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer .

HY-114491

Rineterkib	ERK Raf	Cancer
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .

HY-114436

MRTX-1257 5 Publications Verification	Ras	Cancer
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

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-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-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-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-B0984

Fendiline hydrochloride 3 Publications Verification	Calcium Channel Ras STING Autophagy	Infection Cardiovascular Disease Cancer
Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC₅₀ of 17 µM). Fendiline hydrochloride is also a selective *K-Ras* inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC₅₀ of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .

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-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-162809

XMU-MP-9	Ras	Cancer
XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of *K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1* and *K-Ras, induces conformational changes in the Nedd4-1/K-Ras* complex, promotes the ubiquitination and degradation of multiple *K-Ras* mutants, and inhibits the proliferation of cells carrying *K-Ras* mutants. XMU-MP-9 can be used for the study of colon, lung and pancreatic cancer .

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-B0984A

Fendiline 3 Publications Verification	Calcium Channel Ras STING Autophagy	Infection Cardiovascular Disease Cancer
Fendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC₅₀ of 17 µM). Fendiline is also a selective *K-Ras* inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC₅₀ of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .

HY-159190

HRX-0233	MAPKAPK2 (MK2)	Cancer
HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .

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-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-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-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-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-142160

GNE-9815	Raf	Cancer
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits K_i values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of *KRAS* mutant cancers .

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-W998345

SMART1	PROTACs PDK-1 Akt	Cancer
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .

HY-124761

Poloppin	Polo-like Kinase (PLK) Autophagy Mitosis	Cancer
Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC₅₀=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (K_d= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors .

HY-B0984R

Fendiline hydrochloride (Standard)	Calcium Channel Ras STING Autophagy Reference Standards	Infection Cardiovascular Disease Cancer
Fendiline (hydrochloride) (Standard) is the analytical standard of Fendiline (hydrochloride). This product is intended for research and analytical applications. Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .

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-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-163299

pan-KRAS-IN-5 1 Publications Verification	Ras Apoptosis PI3K Akt p38 MAPK	Cancer
pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research .

HY-P991571

GC1118 GC-1118A	EGFR PERK Akt	Cancer
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (K_D) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .

HY-135865

KRAS inhibitor-7	Ras	Cancer
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B .

HY-157458

PDEδ autophagic degrader 1	ATTECs Phosphodiesterase (PDE) Autophagy	Cancer
PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells .

HY-P10436

Braftide	Raf	Cancer
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF ^G469A with IC₅₀ of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC₅₀ is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer 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-162445

KRASG12D-IN-3	Ras PERK	Cancer
KRASG12D-IN-3 is an orally active KRAS ^G12D inhibitor. KRASG12D-IN-3 inhibits the growth of gastric cancer and pancreatic cancer cells. KRASG12D-IN-3 inhibits the activity of p-ERK in gastric cancer cells. KRASG12D-IN-3 can be used for the research of gastric cancer and pancreatic 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-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-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-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-125199

ULK-100	ULK	Cancer
ULK-100 is a highly selective and potent ULK1 kinase inhibitor with an IC₅₀ value of 1.6 nM. ULK-100 is promising for research of autophagy-related diseases (e.g., KRAS-mutant lung cancer, glioblastoma) .

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-172237

Sosimerasib	Ras	Cancer
Sosimerasib is an orally active KRAS ^G12C inhibitor. Sosimerasib can be used in research related to non-small cell lung cancer .

Cat. No.	Product Name

HY-L260

KRAS Targeted Compound Library

32 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 32 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-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-P10436

Braftide	Raf	Cancer
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF ^G469A with IC₅₀ of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC₅₀ is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research .

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-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 .

Cat. No.	Product Name	Target	Research Area	Image

HY-P991571

GC1118 GC-1118A	EGFR PERK Akt	Cancer
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (K_D) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .

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	Category	Target	Chemical Structure

HY-137971

(±)-Spiro-oxanthromicin A	Microorganisms Ketones, Aldehydes, Acids Source Classification	Ras
(±)-Spiro-oxanthromicin A (Compound 4), a polyketide, is a *K-Ras* inhibitor with an IC₅₀ of 26.7  μM. (±)-Spiro-oxanthromicin A can be isolated from soil-derived Streptomyces sp. (±)-Spiro-oxanthromicin A can mislocalize oncogenic mutant K-Ras from the plasma membrane of intact MDCK cells. (±)-Spiro-oxanthromicin A can be used for cancers research .

Cat. No.	Product Name	Chemical Structure

HY-114436S

MRTX-1257-d6
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

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-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 .

HY-180200

RNK08954		Alkynes
RNK08954 is an orally active KRAS^G12D inhibitor with a K_d of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRAS^G12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRAS^G12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .

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