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Results for "

H-358

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (3) COX (1) ERK (2) Isotope-Labeled Compounds (1) MAPKAPK2 (MK2) (1) Monocarboxylate Transporter (1) Phosphatase (1) PROTACs (1) Raf (2) Ras (16) SHP2 (2)
By Research Areas:	Cancer (24) Inflammation/Immunology (1) Neurological Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12873

RBC8	Ras	Cancer
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.

HY-114436

MRTX-1257 3 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-12875

BQU57	Ras	Cancer
BQU57 selectively inhibits Ral, with higher selectivity than Ras or Rho. The IC50 values of BQU57 on H2122 and H358 cells are 2.0 μM and 1.3 μM respectively.

HY-148517

AZD0095 1 Publications Verification	Monocarboxylate Transporter	Cancer
AZD0095 is a selective and orally active MCT4 inhibitor (IC₅₀: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .

HY-115907

K20	Ras ERK Apoptosis	Cancer
K20 is a potent and selective KRas G12C inhibitor with an IC₅₀ of 1.16 µM. K20 shows anticancer activity in H358 cells (IC₅₀= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .

HY-145020

KRAS G12C inhibitor 23	Ras	Cancer
KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC₅₀ of 491 nM (WO2021218939A1, compound 1) .

HY-161173

PROTAC SOS1 degrader-5	PROTACs Ras	Cancer
PROTAC SOS1 degrader-5 (compound 4) is a potent PROTAC SOS1 degrader, with the DC₅₀ of 13 nM. PROTAC SOS1 degrader-5 strongly inhibits NCI-H358 cells proliferation with an IC₅₀ of 5 nM .

HY-114436S

MRTX-1257-d6	Isotope-Labeled Compounds	Cancer
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-157888

SHP2-IN-26	SHP2 Phosphatase	Cancer
SHP2-IN-26 (Compound 4b) is a highly selective SHP2 allosteric inhibitor with a IC₅₀ value of 3.2 nM. SHP2-IN-26 inhibits the phosphorylation of ERK and AKT in NCI-H358 cells. SHP2-IN-26 has antitumor activity .

HY-153699

SHP2-IN-14	SHP2	Cancer
SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC₅₀=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty .

HY-164389

SML-10-70-1	Ras	Cancer
SML-10-70-1 is a ligand for RAS, which covalently modifies the K-Ras G12C mutant protein, and inhibits the phosphorylation of ERK and Akt. SML-10-70-1 inhibits the proliferation of cancer cells H23, H358 and A549 with IC₅₀ of 26.6-47.6 μM .

HY-142945

KRAS G12C inhibitor 43	Ras	Cancer
KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC₅₀s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively .

HY-168013

KRASG12C IN-14	Ras	Cancer
KRASG12C IN-14 (compound 15) is an inhibitor targeting the KRAS G12C mutation. KRASG12C IN-14 inhibits CYPA-dependent KRAS-BRAF with an IC₅₀ of 0.002 μM. KRASG12C IN-14 inhibits ERK phosphorylation in NCI-H358 cells with an IC₅₀ of 0.002 μM .

HY-144271

RAF-IN-1	Raf	Cancer
RAF-IN-1 is a potent b/cRAF inhibitor with an IC₅₀s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF ^wt, and bRAF ^V600E. RAF-IN-1 shows cell growth inhibition with GI₅₀s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF ^V600E mutation, respectively .

HY-146061

KRAS G12C inhibitor 48	Ras	Cancer
KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC₅₀ of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC₅₀s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .

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-148278

BI-0474	Ras	Cancer
BI-0474 is a potent KRAS ^G12C inhibitor with an IC₅₀ value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .

HY-144269

SHR902275	Raf	Cancer
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC₅₀s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF ^wt, and bRAF ^V600E, respectively. SHR902275 shows cell growth inhibition with GI₅₀s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .

HY-168577

KRAS G12D inhibitor 25	Ras	Cancer
KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC₅₀ of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC₅₀ of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC₅₀ of 0.1-1 μM .

HY-160023

D3S-001	Ras	Cancer
D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS ^G12C mutant H358 and MIA-PA-CA-2 with an IC₅₀ of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .

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-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-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-121537

CAY10404	COX Akt Apoptosis	Neurological Disease Inflammation/Immunology Cancer
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 1 nM and a selectivity index (SI; COX-1 IC₅₀/COX-2 IC₅₀) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .

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 .

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