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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

Results for "

H358 cell

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (3) ERK (2) Isotope-Labeled Compounds (1) MAPKAPK2 (MK2) (1) PERK (1) Phosphatase (1) PROTACs (2) Raf (2) Ras (18) SHP2 (1)
By Research Areas:	Cancer (24)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: Itk TOPK NAMPT ALCAM/CD166 GDNF Receptor VISTA BCL6 Tim3 BMI1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-160220S

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

HY-163595

Pan-RAS-IN-4	Ras	Cancer
Pan-RAS-IN-4 (compound 2) is a potent inhibitor of RAS, with the IC₅₀ of ＜ 100 nM for KRAS G12D. Pan-RAS-IN-4 plays an important rile in cancer research .

HY-144323

YF135	PROTACs PERK	Cancer
YF135 is an efficient and reversible-covalent KRAS ^G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS ^G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .

HY-132979

KRAS G12C inhibitor 18	Ras	Cancer
KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities .

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 .

Cat. No.	Product Name	Chemical Structure

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-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 .

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