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Results for "

and G13D

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (4) Autophagy (1) Caspase (1) CDK (1) ERK (1) Isotope-Labeled Compounds (1) MEK (2) Mitochondrial Metabolism (1) p38 MAPK (2) PARP (1) PERK (1) PROTACs (2) Proton Pump (1) Raf (1) Ras (16) TNF Receptor (2)
By Research Areas:	Cancer (20) Inflammation/Immunology (2)
Click Chemistry:	Alkynes (3)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-173632

AMG410	Ras	Cancer
AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC₅₀ values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (K_d(GDP-state) of 1 nM; K_d(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers .

HY-15610

GDC-0623 5+ Cited Publications RG 7421; MEK inhibitor 1	MEK Apoptosis	Cancer
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (K_i=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC₅₀=42 nM) versus A375 (BRAF ^V600E, EC₅₀=7 nM).

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-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-176785S

MCB-294	Ras Apoptosis p38 MAPK Caspase TNF Receptor	Cancer
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-176489

PROTAC pan-KRAS degrader-1	PROTACs Ras	Cancer
PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC₅₀ of 1.1 nM, D_max of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc . Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);

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-145962A

MRTX-EX185 formic	Ras	Cancer
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-161066

*KRAS G13D-IN-1*	Ras	Cancer
KRAS G13D-IN-1 (Compound 41) is a selective and covalently reversible inhibitor of KRAS ^G13D (IC₅₀: 0.41 nM). The selectivity for KRAS ^G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS ^G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades. KRAS G13D-IN-1 can be used in the research of colon cancer .

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-179452

*KRAS G13D-IN-2*	Ras CDK Mitochondrial Metabolism	Cancer
KRAS G13D-IN-2 (compound 8B) is a potent orally active KRAS G13D inhibitor with IC₅₀ values of 1.95 μM (HCT-116 ^G13D) and 2.16 μM (HCT-15 ^G13D). KRAS G13D-IN-2 induces G1-phase arrest and mitochondrial membrane depolarization. KRAS G13D-IN-2 induces senescence through CDK6/TWIST1 inhibition. KRAS G13D-IN-2 inhibits tumor growth in murine models. KRAS G13D-IN-2 can be used for KRAS ^G13D-mutant colorectal cancer research .

HY-145962

MRTX-EX185	Ras	Cancer
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-178497

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

HY-P3129

*KRAS G13D* peptide, 25 mer**	Ras	Inflammation/Immunology Cancer
KRAS G13D peptide, 25 mer, a KRAS activating oncogene mutation peptide, is an immune potentiator extracted from patent WO2018144775A1. KRAS G13D peptide, 25 mer can be used to prepare KRAS vaccine .

HY-162873

MEK/RAF-IN-1	MEK Raf	Cancer
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC₅₀ values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .

HY-173349

TDI-012804	PARP	Cancer
TDI-012804 is a TNKS2 inhibitor that selectively inhibits intracellular endogenous TNKS2 protein. TDI-012804 increases the expression of AXIN1 protein in cells that are heterozygous (Tnks1HET) and completely knocks out (Tnks1KO) for TNKS1. TDI-012804 inhibits the proliferation of ApcQ1405X/Tnks1KO organoids (EC₅₀ of 59.1 nM) and is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids .

HY-176341S

*KRAS 2B G13D* mutant, Arg-13C6,15N4, Lys-13C6,15N2**	Isotope-Labeled Compounds	Cancer
KRAS 2B G13D mutant, Arg-Arg- ¹³C₃₆, ¹⁵N₄, Lys- ¹³C₆, ¹⁵N₂ is the ¹³C- and ¹⁵N-labeled KRAS 2B G13D mutant.

HY-173632A

AMG410 diTFA	Ras	Cancer
AMG410 diTFA is a non-covalent and selective pan-KRAS inhibitor with IC₅₀ values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 diTFA shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 diTFA is a dual GTP(on)- and GDP(off)-state inhibitor (K_d(GDP-state) of 1 nM; K_d(GTP-state) of 22 nM). AMG410 diTFA blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 diTFA can be used for the study of colorectal, pancreatic, and lung cancers .

HY-181704

KRAS-IN-54	PERK Ras	Cancer
KRAS-IN-54 is a macrocyclic KRAS inhibitor. KRAS-IN-54 exhibits activity against cell viability and pERK inhibition in cells with KRAS ^G12D and KRAS ^G13D mutations. KRAS-IN-54 can be used in the research of KRAS-mutant cancers, including pancreatic adenocarcinoma, colorectal cancer, non-small cell lung cancer, esophageal cancer, gallbladder cancer, melanoma, ovarian cancer and endometrial cancer .

Cat. No.	Product Name	Target	Research Area

HY-P3129

*KRAS G13D* peptide, 25 mer**	Ras	Inflammation/Immunology Cancer
KRAS G13D peptide, 25 mer, a KRAS activating oncogene mutation peptide, is an immune potentiator extracted from patent WO2018144775A1. KRAS G13D peptide, 25 mer can be used to prepare KRAS vaccine .

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 .

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-176341S

*KRAS 2B G13D* mutant, Arg-13C6,15N4, Lys-13C6,15N2**
KRAS 2B G13D mutant, Arg-Arg- ¹³C₃₆, ¹⁵N₄, Lys- ¹³C₆, ¹⁵N₂ is the ¹³C- and ¹⁵N-labeled KRAS 2B G13D mutant.

Cat. No.	Product Name		Classification

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-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-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) .

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