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KRAS mutants

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Acyltransferase (1) Akt (2) AMPK (1) Apoptosis (7) ATTECs (1) Autophagy (3) EGFR (1) ERK (5) Farnesyl Transferase (2) Ferroptosis (1) GLUT (1) Isotope-Labeled Compounds (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (1) MAPKAPK2 (MK2) (1) MDM-2/p53 (1) MEK (1) Molecular Glues (1) mTOR (1) p38 MAPK (1) PARP (1) PDK-1 (1) Phosphatase (3) Phosphodiesterase (PDE) (3) PI3K (1) Polo-like Kinase (PLK) (1) PROTAC Linkers (1) PROTACs (3) Raf (9) Ras (52) Ribosomal S6 Kinase (RSK) (1) SHP2 (1)
By Research Areas:	Cancer (84) Inflammation/Immunology (2)
Click Chemistry:	Azide (1) Alkynes (1)

Inhibitors & Agonists

Fluorescent Dye

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153724

BI-2865 1 Publications Verification	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-122914

KRAS inhibitor-3	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-19706

ARS-853 4 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-134813

MRTX1133 10+ Cited Publications	Ras	Cancer
MRTX1133 is a noncovalent, potent, and selective 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-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-124761

Poloppin	Polo-like Kinase (PLK) Autophagy	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-108887

Anticancer agent 124	Raf	Cancer
Anticancer agent 124 is an orally active, highly selective and potent pan RAF inhibitor. Anticancer agent 124 inhibits MAPK signalling in BRAF V600E, NRAS and KRAS mutant tumor cells .

HY-157458

PDEδ autophagic degrader 1	ATTECs Phosphodiesterase (PDE) Autophagy	Cancer
PDEδ autophagic degrader 1 (compound 12c) 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-168514

SOS1/EGFR-IN-2	EGFR	Cancer
SOS1/EGFR-IN-2 (Compound 4) is a SOS1 and EGFR dual inhibitor with IC₅₀s of 8.3 and 14.6 nM, respectively. SOS1/EGFR-IN-2 exhibits significant antiproliferative effect on the cancer cells haboring various KRAS mutants .

HY-161654

PROTAC SOS1 degrader-10	PROTACs Ras	Cancer
PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC₅₀s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC₅₀s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))

HY-122862

RAS inhibitor Abd-7 1 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-132920

KRAS mutant protein inhibitor 1	Ras	Cancer
KRAS mutant protein inhibitor 1 is a *KRAS* mutant protein inhibitor for potential research in 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-114491A

Rineterkib hydrochloride	ERK Raf	Cancer
Rineterkib hydrochloride (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-154313

Spiclomazine Clospirazine	Ras	Cancer
Spiclomazine (Clospirazine) is a potent mutant *KRAS*(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .

HY-151287

KRAS inhibitor-20	Ras	Cancer
KRAS inhibitor-20 is a small molecular inhibitor of *KRas* ^G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits *KRas* ^G12C with the IC50 value <10 nM .

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 .

HY-162441

pan-KRAS-IN-8	Ras	Cancer
pan-KRAS-IN-8 (Compound 38) 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 0.07 and 0.18 nM, respectively .

HY-162442

pan-KRAS-IN-9	Ras	Cancer
pan-KRAS-IN-9 (Compound 52) 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 0.24 and 0.30 nM, respectively .

HY-162443

pan-KRAS-IN-10	Ras	Cancer
pan-KRAS-IN-10 (Compound 58) 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 0.7 and 0.24 nM, respectively .

HY-18606

K-Ras G12C-IN-3	Ras	Cancer
K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.

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-164315

KRAS G12C inhibitor 67	Ras	Cancer
KRAS G12C inhibitor 67 (example 35) is a KRAS G12C inhibitor that selectively inhibits the growth of many KRAS G12C mutant tumor cell lines .

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 in cancer research .

HY-159476

KRAS inhibitor-26	Ras	Cancer
KRAS inhibitor-26 (compound 194a) is a potent KRAS G12V inhibitor (IC₅₀: ≤100 nM). KRAS inhibitor-26 can be used for cancer research .

HY-151523

KRas G12R inhibitor 1	Ras	Cancer
KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research .

HY-164513

NHTD	Ras Phosphodiesterase (PDE)	Cancer
NHTD is a KRAS-PDEδ inhibitor. NHTD targets the prenyl-binding pocket of PDEδ, altering the cellular localization of *KRAS, thereby inhibiting the proliferation of KRAS-mutant* cancer cells and inducing apoptosis. NHTD can be used for research on KRAS-driven non-small cell lung cancer (NSCLC) .

HY-18604

K-Ras G12C-IN-1	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-151999

KRAS G12C inhibitor 65	Ras	Cancer
KRAS G12C inhibitor 65 is a potent and covalent KRAS ^G12C inhibitor that traps KRAS ^G12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer .

HY-145022

KRAS G12C inhibitor 25	Ras	Cancer
KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC₅₀=0.48 nM). From WO2021216770A1 compound 3 .

HY-156819

RMC-9805 KRAS G12D inhibitor 18	Ras	Cancer
RMC-9805 (KRAS G12D inhibitor 18) is a KRAS G12D inhibitor. RMC-9805 is orally active. RMC-9805 inhibits RAS signaling to induce apoptosis in KRAS G12D mutant cancer cells .

HY-156529

pan-KRAS-IN-2	Ras	Cancer
pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC₅₀s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively .

HY-168055

(S)-Deoxy-thalidomide	Ligands for E3 Ligase	Cancer
(S)-Deoxy-thalidomide is an E3 ubiquitin ligase ligand. (S)-Deoxy-thalidomide can be linked to the target protein ligand through a linker to form PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can target KRAS mutant proteins for degradation .

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-112929

DT-061 10+ Cited Publications	Phosphatase	Cancer
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .

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-128350A

FGTI-2734 mesylate	Farnesyl Transferase	Cancer
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC₅₀s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .

HY-153346

RMC-6291 1 Publications Verification	Ras ERK Apoptosis	Cancer
RMC-6291 is an orally active and covalent inhibitor of KRAS ^G12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRAS ^G12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRAS ^G12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRAS ^G12C mutant cells with a median IC₅₀ of 0.11 nM .

HY-U00416

ARS-1323	Ras	Cancer
ARS-1323, the racemate of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.

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-159163

KRASG12C IN-12	Ras	Cancer
KRASG12C IN-12 (compound-1) is a KRAS ^G12C inhibitor. KRASG12C IN-12 (compound-1) can form a ternary complex with intracellular CYPA and the activated KRAS ^G12C mutant .

HY-161906

SD-066-4	Acyltransferase	Cancer
SD-066-4 is an orally active acyltransferase inhibitor. SD-066-4 can be used in cancer research .

HY-P2265

SAH-SOS1A	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-128350

FGTI-2734	Farnesyl Transferase	Cancer
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC₅₀s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .

HY-U00417

ARS-1630	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-141807

MS21	PROTACs Akt	Cancer
MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.

HY-146223

AZD4625	Ras	Cancer
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS ^G12C. AZD4625 has high oral bioavailability .

HY-120885

(+)-Oxanthromicin	Ras	Cancer
(+)-Oxanthromicin (Compound 1) mislocalizes the oncogenic mutant K-Ras from the plasma membrane of intact Madin-Darby canine kidney (MDCK) cells, and exhibits thereby antitumor efficacy .

HY-114277A

Sotorasib racemate 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-139047

SW157765	GLUT	Cancer
SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs .

Cat. No.	Product Name	Type

HY-114491

Rineterkib

Fluorescent Dyes/Probes

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 .

Cat. No.	Product Name	Target	Research Area

HY-P2265A

SAH-SOS1A TFA	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-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 .

HY-P5192

KRAS G12D(8-16)	Peptides	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-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 .