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Results for "

KRAS mutant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (5) ATTECs (1) Autophagy (3) ERK (3) Farnesyl Transferase (2) Ferroptosis (1) GLUT (1) Isotope-Labeled Compounds (1) MDM-2/p53 (1) MEK (1) Molecular Glues (1) p38 MAPK (1) Phosphatase (2) Phosphodiesterase (PDE) (1) Polo-like Kinase (PLK) (1) PROTACs (1) Raf (5) Ras (41) SHP2 (1)
By Research Areas:	Cancer (64) Inflammation/Immunology (2)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Fluorescent Dye

Peptides

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153724

BI-2865	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 2 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-132920

KRAS mutant protein inhibitor 1

Ras Cancer

KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential research in cancer.

KRAS mutant protein inhibitor 1	Ras	Cancer
KRAS mutant protein inhibitor 1 is a *KRAS* mutant protein inhibitor for potential research in cancer.

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-134813

MRTX1133 3 Publications Verification	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-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-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-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-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 .

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.

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	Cancer
RMC-4998 is a molecular glue compound with good antitumor activity. RMC-4998 is able to form a ternary complex with CYPA and an activated KRAS G12C mutant. Furthermore, CYPA binding to KRAS G12C blocks the interaction between activated KRAS mutants and downstream effector proteins, thereby inhibiting signaling that promotes cell proliferation .

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-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.

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-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-151999

KRASG12C IN-1	Ras	Cancer
KRASG12C IN-1 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-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-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 5+ 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-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	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 .

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.

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

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 .

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.

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.

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-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 .

HY-W451275

HG106	Others	Cancer
HG106 is a potent SLC7A11 inhibitor. HG106 markedly decreased cystine uptake and intracellular glutathione biosynthesis. HG106 can be used for the research of KRAS-mutant lung adenocarcinoma .

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-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-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-156498

RMC-7977	Ras	Cancer
RMC-7977 is a reversible, tri-complex RAS inhibitor with broad spectrum activity for both mutant and wild-type (WT) KRAS, NRAS, and HRAS variants.RMC-7977 can lead to tumor regressions and was well tolerated in diverse RAS-addicted preclinical cancer models. RMC-7977 also can inhibit the growth of KRAS ^G12C cancer models .

HY-126247

BI-2852	Ras	Cancer
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

HY-N6674

Diazepinomicin ECO-4601; TLN-4601; BU 4664L	Ras Apoptosis	Cancer
Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models .

HY-150927

G12Si-2

Ras Cancer

G12Si-2, an analog of G12Si-1 (HY-150926), is a negative control tool. G12Si-2 is not a covalent inhibitor of the G12S mutant of K-Ras .

HY-154959A

(9R,12aR)-AZD4747	Others	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-126247B

(R)-BI-2852	Others	Cancer
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

HY-146223A

(3R,10R,14aS)-AZD4625	Others	Cancer
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS ^G12C. AZD4625 has high oral bioavailability .

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