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Results for "

KRas inhibitor

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (435) Cardiovascular Disease (3) Endocrinology (1) Infection (9) Inflammation/Immunology (11) Metabolic Disease (2) Neurological Disease (5)
Click Chemistry:	Azide (3) Alkynes (30)

444

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-137497

KRAS inhibitor-9	Ras Apoptosis	Cancer
KRAS inhibitor-9, a potent *KRAS* inhibitor (K_d=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung 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-159652

KRAS inhibitor-31 1 Publications Verification	Ras	Cancer
KRAS inhibitor-31 (compound 33) is a *KRAS* inhibitor, with K_D (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRas G12V, respectively .

HY-144661

KRAS G12D inhibitor 14	Ras Apoptosis	Cancer
KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a K_D of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D .

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-164350

KRAS inhibitor-27	Ras ERK p38 MAPK	Cancer
KRAS inhibitor-27 (Compound 15h) is the inhibitor for *KRAS. KRAS* inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC₅₀ of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC₅₀ in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway .

HY-138295

KRAS inhibitor-10	Ras	Cancer
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1 .

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-171255

KRAS G12D inhibitor 26	Ras	Cancer
KRAS G12D inhibitor 26 is a modulator of *Kras, targeting Kras(G12D) with an IC₅₀* ≤ 100 nM .

HY-115880A

KRAS G12D inhibitor 3 TFA	Ras	Cancer
KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC₅₀ of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-159474

KRAS inhibitor-24	Ras	Cancer
KRAS inhibitor-24 (compound 115c) is a pyridopyrimidine *KRAS* inhibitor, with an IC₅₀ of < 100 nM for KRas G12V, KRas WT and KRas G12R .

HY-139911

KRAS G12D inhibitor 7	Ras	Cancer
KRAS G12D inhibitor 7 is an inhibitor of KRAS G12D. KRAS G12D inhibitor 7 can be used for the research of cancer .

HY-169311

KRAS inhibitor-37	Ras	Cancer
KRAS inhibitor-37 (compound 2) is a potent *KRAS* inhibitor with K_Ds of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC₅₀s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .

HY-135865

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

HY-172626

KRAS G12D inhibitor 28	Ras	Cancer
KRAS G12D inhibitor 28 (Compound 1) is a KRAS G12D inhibitor. KRAS G12D inhibitor 28 (Compound 1) can be used in the cancer research .

HY-125872

KRAS G12C inhibitor 14	Ras	Cancer
KRas G12C inhibitor 14 (Compound 17) is a potent KRAS G12C inhibitor (IC₅₀ = 18 nM).

HY-143607

KRAS G12D inhibitor 13	Ras	Cancer
KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142) .

HY-115880

KRAS G12D inhibitor 3	Ras	Cancer
KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC₅₀ of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-146544

KRAS inhibitor-14	Ras	Cancer
KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC₅₀s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .

HY-134811

KRAS G12D inhibitor 1	Ras PERK	Cancer
KRAS G12D inhibitor 1 is a KRAS ^G12D inhibitor with an IC₅₀ value of 0.4 nM. KRAS G12D inhibitor 1 inhibits KRas ^G12D-mediated ERK phosphorylation. KRAS G12D inhibitor 1 can be used for cancer research .

HY-143592

KRAS G12C inhibitor 39	Ras	Cancer
KRAS G12C inhibitor 39 is a potent inhibitor of KRAS G12C. KRas is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494) .

HY-139894

KRAS G12D inhibitor 5	Ras	Cancer
KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential research of pancreatic cancer.

HY-172626A

*(R)-KRAS* G12D inhibitor 28 hydrochloride dihydrate**	Ras	Cancer
(R)-KRAS G12D inhibitor 28 hydrochloride dehydrate is the hydrochloride dehydrate of (R)-KRAS G12D inhibitor 28 (HY-172626). KRAS G12D inhibitor 28 (Compound 2) is a KRAS G12D inhibitor. KRAS G12D inhibitor 28 (Compound 2) can be used in the cancer research .

HY-143606

KRAS G12D inhibitor 12	Ras	Cancer
KRAS G12D inhibitor 12 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 134) .

HY-143604

KRAS G12D inhibitor 11	Ras	Cancer
KRAS G12D inhibitor 11 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 11 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 52) .

HY-143599

KRAS G12D inhibitor 8	Ras	Cancer
KRAS G12D inhibitor 8 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 8 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021107160A1, compound 2) .

HY-160445

KRAS G12D inhibitor 19	Ras	Cancer
KRAS G12D inhibitor 19 (Compound 7) is a KRAS G12D inhibitor. KRAS G12D inhibitor 19 can be used for the research of cancer .

HY-142460

KRAS G12C inhibitor 28	Ras	Cancer
KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC₅₀ of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1) .

HY-151288

KRAS inhibitor-21	Ras	Cancer
KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC₅₀ value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research .

HY-153412

KRAS inhibitor-22	Ras	Cancer
KRAS inhibitor-22 (compound FB9/6B9) is a potent inhibitor of *K-Ras. KRAS* inhibitor-22 targets to Kras 4B(G12D) and (G12C), which can be used for cancer research .

HY-130260

KRAS inhibitor-4	Ras	Cancer
KRAS inhibitor-4 (compound F12) is a potent *KRAS* inhibitor and developed as anticancer agents .

HY-159474A

*(1R)-KRAS* inhibitor-24**	Ras	Cancer
(1R)-KRAS inhibitor-24 (compound 115c) is a pyridopyrimidine *KRAS* inhibitor, with an IC₅₀ of < 100 nM for KRas G12V, KRas WT and KRas G12R .

HY-135864

KRAS inhibitor-6	Ras	Cancer
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A .

HY-146543

KRAS inhibitor-13	Ras	Cancer
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC₅₀s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers .

HY-146533

KRAS inhibitor-12	Ras	Cancer
KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC₅₀s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .

HY-146476

KRAS inhibitor-18	Ras	Cancer
KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC₅₀ of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC₅₀s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers .

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-162366

KRAS G12D inhibitor 20	Ras	Cancer
KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor. KRAS G12D inhibitor 20 has antitumor activity .

HY-162444

KRAS G12D inhibitor 22	Ras	Cancer
KRAS G12D inhibitor 22 (compound 6) is a inhibitor of *KRAS* mutation. KRAS G12D inhibitor 22 has high activity (IC₅₀＜100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research .

HY-148260

KRAS G12D inhibitor 16	Ras	Cancer
KRAS G12D inhibitor 16 is a KRAS G12D inhibitor. KRAS G12D inhibitor 16 has inhibitory activity against KRAS G12D and KRAS G12D mutation with IC₅₀ value of 0.7 nM and 0.35 μM, respectively. KRAS G12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC) .

HY-158703

KRAS G12D inhibitor 24	Ras	Cancer
KRAS G12D inhibitor 24 (compound 103) is a potent inhibitor of KRAS G12D, with the IC₅₀ of 0.004 μM. KRAS G12D inhibitor 24 has oral bioactivity .

HY-147636

KRAS G12C inhibitor 55	Ras	Cancer
KRAS G12C inhibitor 55 (Compound 1) is a KRAS G12C inhibitor .

HY-158701

KRAS G12D inhibitor 23	Ras	Cancer
KRAS G12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRAS G12D, with the IC₅₀ of 0.007 μM. KRAS G12D inhibitor 23 plays an important role in cancer research .

HY-142946

KRAS G12C inhibitor 44	Ras	Cancer
KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC₅₀s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo .

HY-112494

KRas G12C inhibitor 4	Ras	Cancer
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.

HY-162971

KRAS inhibitor-33	Ras	Cancer
KRAS inhibitor-33 (compound 115a) is an inhibitor of pyridopyrimidine kras (IC₅₀ ≤ 100nM) .

HY-142458

KRAS G12C inhibitor 27	Ras	Cancer
KRAS G12C inhibitor 27 is a KRAS G12C inhibitor with antitumor effects (WO2021109737) .

HY-142457

KRAS G12C inhibitor 26	Ras	Cancer
KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737) .

HY-168442

KRAS inhibitor-40	Ras PERK	Cancer
KRAS inhibitor-40 (Compound 41) is a *KRAS* inhibitor that interferes with the KRAS G12C-BRAF complex. KRAS inhibitor-40 inhibits the ERK phosphorylation of *KRAS* downstream signaling pathway. KRAS inhibitor-40 can inhibit the proliferation of tumor cells with different *KRAS* mutation types and has antitumor activity .

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-156002

LUNA18 Paluratide	Ras ERK	Cancer
LUNA18 is an orally-available cyclic peptide *KRAS* and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with *KRAS* genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .

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-P3277

KRpep-2d	Ras	Cancer
KRpep-2d is a potent *K-Ras* inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer 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-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-P10847

KS-58	Ras	Cancer
KS-58 is a KRpep-2d (HY-P3277) derivative. KS-58 is a *K-Ras* (G12D) inhibitory peptide that selectively binds *K-Ras. KS-58 can enter cells and block intracellular Ras* interaction with effector proteins. KS-58 inhibits the proliferation of tumor cells and has antitumor activity .

HY-P3277A

KRpep-2d TFA	Ras	Cancer
KRpep-2d (TFA) is a potent *K-Ras* inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .

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	Category	Target	Chemical Structure

HY-N0735

Phellodendrine chloride 2 Publications Verification	Alkaloids Phellodendron amurense Rupr. Classification of Application Fields Rutaceae Phenols Polyphenols Plants Isoquinoline Alkaloids Disease Research Fields Source Classification Cancer	Autophagy Apoptosis AMPK mTOR STAT Interleukin Related PKC p38 MAPK NF-κB COX Reactive Oxygen Species (ROS) PI3K Akt MMP
Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway .

HY-125847

Salvianolic acid F 1 Publications Verification	Stilbenes Classification of Application Fields Labiatae Samanea saman (Jacq.) Merr. Phenols Polyphenols Plants Disease Research Fields Source Classification Cancer	Ras PI3K Akt Caspase Apoptosis Bcl-2 Family NF-κB MMP
Salvianolic acid F is a *KRAS* inhibitor, especially for *KRAS* G12D. Salvianolic acid F inhibits NF-kB, MMP-9, and NO simultaneously. Salvianolic acid F inhibits cancer cell growth, invasion, and migration and induces apoptosis via the EP300/PI3K/AKT pathway in vitro. Salvianolic acid F inhibits the growth of *KRAS*-dependent lung cancer cells via the PI3K/AKT signaling pathway in vivo. Salvianolic acid F can be used in the research of various cancers, including *KRAS* G12D-driven non-small cell lung cancer (NSCLC) and ovarian cancer .

HY-N0427

Phellodendrine	Alkaloids Phellodendron amurense Rupr. Classification of Application Fields Rutaceae Phenols Polyphenols Quinoline Alkaloids Plants Inflammation/Immunology Disease Research Fields Source Classification	Akt NF-κB AMPK mTOR PKC STAT Interleukin Related p38 MAPK COX Reactive Oxygen Species (ROS) Apoptosis Autophagy PI3K MMP
Phellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway .

HY-135700

Mevalonolactone	Structural Classification Microorganisms Other Phenylpropanoids Phenylpropanoids Source Classification	Calcineurin Ras HMG-CoA Reductase (HMGCR)
Mevalonolactone is an intermediate metabolite in the eukaryotic mevalonate pathway, serving as the stable δ-lactone form of mevalonate with oral activity. Mevalonolactone exhibits binding affinity for ZNF384 (K_a = 12.6 μM) and inhibitory activity against aconitase (aconitase). Mevalonolactone promotes the nuclear localization of ZNF384 and enhances its binding to the GGPPS promoter. Mevalonolactone induces insulin resistance, disrupts glucose and lipid metabolism, enhances the isoprenylation of *K-Ras, and inhibits* the activation of the insulin signaling pathway. Mevalonolactone inhibits polypeptide synthesis of HMG-CoA reductase in isolated rat hepatocytes, promotes its degradation, and reduces its enzymatic activity. Mevalonolactone impairs mitochondrial function in rat brains. Mevalonolactone promotes the development of metabolically unhealthy obesity. Mevalonolactone can be used in research related to metabolically abnormal obesity, mevalonic aciduria, HMGCR-related limb-girdle myopathy, and statin-induced myopathy .

HY-178224

Morindone	Quinones Structural Classification Morinda citrifolia Linn. Rubiaceae Benzene Quinones Plants Source Classification	Apoptosis DNA/RNA Synthesis
Morindone is an anthraquinone found in Morinda citrifolia L. Morindone can inhibit cancer cells proliferation, induce apoptosis and cause G1 phase arrest. Morindone can inhibit activities of DNA polymerase and downregulate mutated TP53 and KRAS gene expression. Morindone can be used for the research of cancer, such as colon cancer .

HY-N0735R

Phellodendrine chloride (Standard)	Alkaloids Structural Classification Phellodendron amurense Rupr. Rutaceae Phenols Polyphenols Plants Isoquinoline Alkaloids Source Classification	Reference Standards Autophagy mTOR AMPK Apoptosis STAT Interleukin Related PKC p38 MAPK NF-κB COX Reactive Oxygen Species (ROS) PI3K Akt MMP
Phellodendrine chloride (Standard) is the analytical standard of Phellodendrine chloride (HY-N0735). Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

HY-N8387

Neogrifolin	Human Gut Microbiota Metabolites Microorganisms Phenols Polyphenols Endogenous metabolite Source Classification	Ras
Neogrifolin is an inhibitor of *KRAS. Neogrifolin suppress KRAS* expression in human colon cancer cells. Neogrifolin has anti-cell viability activity against HeLa, SW480 and HT29 cells wih IC₅₀s of 24.3, 34.6, and 30.1 μM, respectively .

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 .

HY-112541

21-Hydroxyoligomycin A	Microorganisms Macrolide Antibiotics Antibiotics Source Classification	Ras Antibiotic
21-Hydroxyoligomycin A is a potent inhibitor of K-Ras PM localization with an IC₅₀ value of 4.82 nM. 21-Hydroxyoligomycin A has cytotoxicity and can be isolated from Streptomyces .

HY-134505

Avicin G	Structural Classification Acacia victoriae Benth. Terpenoids Plants Pentacyclic Triterpenoids Fabaceae Source Classification	Ras Phospholipase ERK Akt
Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer .

Cat. No.	Product Name	Chemical Structure

HY-176785S

MCB-294

MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with K_ds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC₅₀s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .

HY-179253

KRAS-IN-47
KRAS-IN-47 is a *KRAS* inhibitor with IC₅₀ < 50 nM against KRAS G12V. KRAS-IN-47 can be used for the study of cancers .

HY-114277S

Sotorasib-d7

Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

HY-157029S

KRASG12D-IN-1
KRASG12D-IN-1 (compound 22) is a KRAS ^G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .

HY-157031S

KRASG12D-IN-2
KRASG12D-IN-2 (compound 28) is a KRAS ^G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .

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-114277S2

Sotorasib-d3
Sotorasib-d₃ (AMG-510-d₃) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .

HY-160220S

KRAS inhibitor-23
KRAS inhibitor-23 (Isomer 2 of compound i) is a potent inhibitor of KRAS that plays an important role in cancer research .

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-173637

AZD0022		Alkynes
AZD0022 is a selective and orally active KRAS ^G12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model .

HY-16373

CP-609754 LNK-754; OSI-754		Alkynes
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC₅₀ for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL . CP-609754 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-176786

MCB-36		Alkynes
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities K_d ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .

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-159652

KRAS inhibitor-31 1 Publications Verification		Alkynes
KRAS inhibitor-31 (compound 33) is a *KRAS* inhibitor, with K_D (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRas G12V, respectively .

HY-176785S

MCB-294		Alkynes
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with K_ds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC₅₀s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .

HY-179253

KRAS-IN-47		Alkynes
KRAS-IN-47 is a *KRAS* inhibitor with IC₅₀ < 50 nM against KRAS G12V. KRAS-IN-47 can be used for the study of cancers .

HY-115880A

KRAS G12D inhibitor 3 TFA		Alkynes
KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC₅₀ of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-134654

MRTX849 analog 24		Alkynes
MRTX849 analog 24 is an alkyne-containing click probe analogue of KRAS G12C inhibitor MRTX849, which is used to research MRTX849 function .

HY-159474

KRAS inhibitor-24		Azide
KRAS inhibitor-24 (compound 115c) is a pyridopyrimidine *KRAS* inhibitor, with an IC₅₀ of < 100 nM for KRas G12V, KRas WT and KRas G12R .

HY-145962A

MRTX-EX185 formic		Alkynes
MRTX-EX185 formic is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 formic can binds both GDP-loaded and active GNP states of *KRAS* and KRAS (G12D). MRTX-EX185 formic exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 formic also binds GDP-loaded HRAS. MRTX-EX185 formic can be used to study various RAS-driven tumors (such as pancreatic cancer) .

HY-157029S

KRASG12D-IN-1		Alkynes
KRASG12D-IN-1 (compound 22) is a KRAS ^G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .

HY-115880

KRAS G12D inhibitor 3		Alkynes
KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC₅₀ of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-157031S

KRASG12D-IN-2		Alkynes
KRASG12D-IN-2 (compound 28) is a KRAS ^G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .

HY-159476

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

HY-134811

KRAS G12D inhibitor 1		Alkynes
KRAS G12D inhibitor 1 is a KRAS ^G12D inhibitor with an IC₅₀ value of 0.4 nM. KRAS G12D inhibitor 1 inhibits KRas ^G12D-mediated ERK phosphorylation. KRAS G12D inhibitor 1 can be used for cancer research .

HY-147595

KRAS G12D inhibitor 15		Alkynes
KRAS G12D inhibitor 15 is a potent inhibitor of KRAS G12D. KRAS G12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243) . KRAS G12D inhibitor 15 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-156555

pan-KRAS-IN-3		Alkynes
pan-KRAS-IN-3 (Example 84) is a pan-KRAS inhibitor. pan-KRAS-IN-3 can be used for research of cancers . pan-KRAS-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-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-145962

MRTX-EX185		Alkynes
MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of *KRAS* and KRAS (G12D). MRTX-EX185 exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic cancer) .

HY-158701

KRAS G12D inhibitor 23		Alkynes
KRAS G12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRAS G12D, with the IC₅₀ of 0.007 μM. KRAS G12D inhibitor 23 plays an important role in cancer research .

HY-163488

KRASG12D-IN-4		Alkynes
KRASG12D-IN-4 (example 38) is a KRas ^G12D inhibitor with an IC₅₀ of 3.3 nM. KRASG12D-IN-4 inhibits proliferation of pancreatic cancer ASPC-1 cells with an IC₅₀ of 12 nM .

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-162446

pan-KRAS-IN-13		Alkynes
pan-KRAS-IN-13 (compound 2) is a potent inhibitor of *KRAS, with IC₅₀*s of 2.75 nM and 2.89 nM for G12D and G12V, respectively

HY-159475

KRAS inhibitor-25		Azide
KRAS inhibitor-25 (compound 151a) is a pyridopyrimidine *KRAS* inhibitor, with an IC₅₀ of < 100 nM against KRas G12V, KRas WT and KRas G12R .

HY-159473

K-Ras-IN-3		Alkynes
K-Ras-IN-3 (compound 3) is a potent *GDP-KRAS* G12V** inhibitor with an IC₅₀ value of 0.371 nM. K-Ras-IN-3 has the potential for the research of cancer .

HY-179404

KRASG12C IN-18		Alkynes
KRASG12C IN-18 is an orally active covalent KRAS ^G12C inhibitor that achieves complete covalent engagement of KRAS ^G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS ^G12C and resistance-associated variants, including KRAS ^G12C/R68S, with low-nanomolar IC₅₀ values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS ^G12C-driven solid tumor and KRAS ^G12C/R68S xenograft models and can be used for colorectal cancer research .

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-180920

KRAS G12D-IN-36		Alkynes
KRAS G12D-IN-36 (Compound 53a) is a highly selective and orally active *KRAS-G12D* inhibitor with an IC₅₀ of 1.63 nM. KRAS G12D-IN-36 effectively inhibits p-ERK with an IC₅₀ of 8.4 nM. KRAS G12D-IN-36 shows potent anti-proliferative activity against AsPC-1 cells. KRAS G12D-IN-36 can be used for research on pancreatic cancer .

HY-179534

G13Ci-22		Alkynes
G13Ci-22 is a MRTX1133 (HY-134813) based KRAS G13C inhibitor. G13Ci-22 can be used for non-small cell lung cancer (NSCLC) research .

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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