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NCI-H358

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (3) ERK (1) Histone Methyltransferase (1) Molecular Glues (1) Monocarboxylate Transporter (1) p38 MAPK (1) PERK (2) Phosphatase (1) Phosphodiesterase (PDE) (1) PROTACs (5) Ras (20) SHP2 (3)
By Research Areas:	Cancer (29)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-147633

KRAS G12C inhibitor 52	Ras	Cancer
KRAS G12C inhibitor 52 (Compound 7) is a KRAS G12C inhibitor .

HY-169312

KRAS inhibitor-38	Ras	Cancer
KRAS inhibitor-38 (Example 18) is a KRAS inhibitor that effectively suppresses the activity of KRAS G12C, KRAS G12D, and KRAS G12V in vivo .

HY-161714

HH0043	Ras	Cancer
HH0043 (Compound 10f) is an orally active and potent SOS1 inhibitor, with IC₅₀ value of 5.8 nM. HH0043 can be used for the research of cancer .

HY-144657

(4S)-PROTAC SOS1 degrader-1	PROTACs Ras	Cancer
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo .

HY-144657A

(4S)-PROTAC SOS1 degrader-1 diTFA	PROTACs Ras	Cancer
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .

HY-163720

KRAS G12C inhibitor 63	Ras Apoptosis	Cancer
KRAS G12C inhibitor 63 (K45) is a KRAS G12C inhibitor. KRAS G12C inhibitor 63 can induce Apoptosis. KRAS G12C inhibitor 63 has antitumor activity .

HY-13945

NVP 231 2 Publications Verification	Apoptosis	Cancer
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC₅₀=12 nM) that competitively inhibits binding of ceramide to CerK . NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage .

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 .

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 .

HY-161111

KVS0001	Others	Cancer
KVS0001 is a potent inhibitor of SMG1 and nonsense mediated decay (NMD) that has anti-tumor activity .

HY-155533

YF704	SHP2	Cancer
YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC₅₀=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells .

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-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-141477

RM-018	Ras	Cancer
RM-018 is a potent, functionally distinct tricomplex KRAS ^G12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRAS ^G12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRAS ^G12C .

HY-147185

PRMT7-IN-1	Histone Methyltransferase	Cancer
PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC₅₀ of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells .

HY-145737

PROTAC SOS1 degrader-1	PROTACs Ras	Cancer
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC₅₀ of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .

HY-145737A

PROTAC SOS1 degrader-1 TFA	PROTACs Ras	Cancer
PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC₅₀ of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .

HY-139612

Opnurasib 3 Publications Verification JDQ-443; NVP-JDQ443	Ras PERK	Cancer
Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity .

HY-139612A

(S)-JDQ-443 (S)-NVP-JDQ443	Ras PERK	Cancer
(S)-JDQ-443 is an isomer of JDQ-443 (HY-139612). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity .

HY-148098

Pan KRas-IN-1	Ras	Cancer
Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .

HY-145321

TMX-4100	Phosphodiesterase (PDE) Molecular Glues	Cancer
TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC₅₀ values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma .

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NCI-H358

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