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SHP2+inhibitor

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By Targets:	Akt (3) Apoptosis (8) ERK (7) Fluorescent Dye (1) JAK (1) Ligands for Target Protein for PROTAC (1) MEK (1) p38 MAPK (1) Phosphatase (18) Ras (1) Reference Standards (2) SHP1 (4) SHP2 (47) STAT (1)
By Research Areas:	Cancer (47) Cardiovascular Disease (2) Metabolic Disease (1)

Inhibitors & Agonists

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100388

SHP099 Maximum Cited Publications 75 Publications Verification	SHP2 Phosphatase	Cancer
SHP099 is an allosteric *SHP2* inhibitor, with IC₅₀s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2 ^D61Y, SHP2E69K, SHP2 ^A72V, SHP2 ^E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC₅₀: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth ^[2].

HY-132844

Tunlametinib HL-085	MEK	Cancer
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC₅₀=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) ^[2].

HY-141523

Vociprotafib RMC-4630; SHP2-IN-7	SHP2 Phosphatase	Cancer
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase *SHP2* inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice ^[2] .

HY-100388A

SHP099 monohydrochloride Maximum Cited Publications 75 Publications Verification	SHP2 Phosphatase	Cancer
SHP099 hydrochloride is a potent, selective and orally available *SHP2* inhibitor with an IC₅₀ of 70 nM .

HY-161952

Sitneprotafib JAB-3312	SHP2	Cancer
Sitneprotafib (JAB-3312) is an orally effective anticancer phosphatase *SHP2* inhibitor (IC₅₀: 1.9 nM) with anti-cancer activity. Sitneprotafib has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .

HY-144903

Migoprotafib GDC-1971	SHP2 Phosphatase p38 MAPK ERK	Cancer
Migoprotafib (GDC-1971) (compound 199) is a *SHP2* inhibitor. Migoprotafib inhibits the MAPK/ERK signaling pathway, and exhibits antitumor activity ^[2].

HY-131132

JAB-3068 SHP2-IN-6	SHP2 Phosphatase	Cancer
JAB-3068 (SHP2-IN-6) is a potent *SHP2* inhibitor, extracted from patent WO2017211303A1, compound 7, has an IC₅₀ of 25.8 nM .

HY-112368

PHPS1 5 Publications Verification	SHP2 SHP1 Phosphatase	Cardiovascular Disease Cancer
PHPS1 is a potent and selective *Shp2* inhibitor with K_is of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively .

HY-153740

PF-07284892 ARRY-558	SHP2	Cancer
PF-07284892 (ARRY-558) is a potent and orally active *SHP2* inhibitor with an IC₅₀ value of 21 nM. PF-07284892 decreases the expression of pERK ^[2].

HY-131132A

JAB-3068 hydrochloride SHP2-IN-6 hydrochloride	SHP2 Phosphatase	Cancer
JAB-3068 (SHP2-IN-6) hydrochloride is a potent *SHP2* inhibitor with an IC₅₀ of 25.8 nM. JAB-3068 hydrochloride is extracted from patent WO2017211303A1, compound 7 .

HY-21336

3-Azetidinemethanol hydrochloride	SHP2	Others
3-Azetidinemethanol hydrochloride, an intermediate, can be used in the synthesis of SHP2 inhibitor .

HY-132901

IACS-15414	SHP2 Phosphatase	Cancer
IACS-15414 is a potent and orally bioavailable *SHP2* inhibitor with an IC₅₀ value of 122 nM.

HY-120901

II-B08	SHP2 SHP1	Cancer
II-B08 is a reversible and noncompetitive *SHP2* inhibitor (IC₅₀: 5.5 μM, 15.7, 14.3 μM for SHP2, SHP1, PTP1B). II-B08 can be used for cancer research .

HY-152208

BPDA2	SHP1 SHP2	Cancer
BPDA2 is a highly selective and competitive active site *SHP2* inhibitor with IC₅₀s of 92.0 nM, 33.39 μM, 40.71 μM for SHP2, SHP1, SHP1B, respectively. DBDA2 downregulates mitogenic and cell survival signaling and RTK expression. BPDA2 suppresses SHP2 mediated signaling and breast cancer cell phenotypes .

HY-115925

SHP2-IN-9	SHP2 Phosphatase	Cancer
SHP2-IN-9 is a specific *SHP2* inhibitor (IC₅₀ =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo .

HY-173571

TK-685	SHP2 Apoptosis	Cancer
TK-685 is an orally active, selective, and allosteric *SHP2* inhibitor with an IC₅₀ of 2.1 nM. TK-685 inhibits esophageal cancer cell proliferation and induced apoptosis by targeting *SHP2*-mediated AKT and ERK signaling pathways .

HY-125257

SHP2 inhibitor LY6 LY6	Phosphatase SHP2 ERK Akt STAT JAK Apoptosis	Cancer
SHP2 inhibitor LY6 (LY6) is a selective *SHP2* inhibitor with an IC₅₀ of 9.8 μM, showing 7-fold selectivity over SHP1. SHP2 inhibitor LY6 inhibits *SHP2*-mediated cell signaling pathways and suppresses cell proliferation. SHP2 inhibitor LY6 elicits induces apoptosis and G2/M cell cycle arrest in lung cancer cells. SHP2 inhibitor LY6 can be used for the research of B cell acute lymphoblastic leukemia, acute myeloid leukemia, and lung cancer .

HY-114453

SHP389	SHP2 Phosphatase	Others
SHP389 is an allosteric *SHP2* inhibitor, with an IC₅₀ of 36 nM for both SHP2 and p-ERK .

HY-125260

SHP844	SHP2	Cancer
SHP844 is a SHP2 inhibitor with the IC₅₀ of 18.9 µM. SHP2 is a protein tyrosine phosphatase (PTP) that regulates tyrosine phosphorylation levels and is involved in cell proliferation, differentiation and survival .

HY-176796

SHP2-IN-43	Ligands for Target Protein for PROTAC SHP2	Cancer
SHP2-IN-43 (Compound 5) is a *SHP2* inhibitor with an IC₅₀ of 98.7 nM. SHP2-IN-43 can be used as a PROTAC target ligand in the synthesis of SHP2-D26 (HY-145162) .

HY-174239

SHP2-IN-41	SHP2	Cancer
SHP2-IN-41 (Compound 4) is a *SHP2* inhibitor with an IC₅₀ of less than 0.1 μM. SHP2-IN-41 has an IC₅₀ against KYSE-520 cells also less than 0.1 μM. SHP2-IN-41 can be used in the study of cancer .

HY-141524

RMC-3943	SHP2 Phosphatase	Cancer
RMC-3943 is an allosteric *SHP2* inhibitor (inhibition of full-length SHP2 in biochemical assay, IC₅₀ = 2.19 nM) .

HY-157535

SHP2-IN-24	SHP2	Cancer
SHP2-IN-24 (compound 111675) is a potent *SHP2* inhibitor with an IC₅₀ value of 0.878 µM and a K_i value of 0.118 µM .

HY-155276

SHP2-IN-20	SHP2	Cancer
SHP2-IN-20 (compound 193) is a *SHP2* inhibitor with an IC₅₀ value of 3 nM. SHP2-IN-20 can be used for glioblastoma research .

HY-155272

SHP2-IN-16	SHP2	Cancer
SHP2-IN-16 (compound 222) is a *SHP2* inhibitor with an IC₅₀ value of 1 nM. SHP2-IN-16 can be used for glioblastoma research .

HY-161360

LXQ-217	SHP2 Apoptosis	Cancer
LXQ-217 is an oral active *SHP2* inhibitor with the IC₅₀ of 2.01 μM. LXQ-217 induces apoptosis and inhibits cell growth in vivo and in vitro .

HY-155273

SHP2-IN-17	SHP2	Cancer
SHP2-IN-17 (compound 192) is a *SHP2* inhibitor with an IC₅₀ value of 2 nM. SHP2-IN-17 can be used for glioblastoma research .

HY-155275

SHP2-IN-19	SHP2	Cancer
SHP2-IN-19 (compound 183) is a *SHP2* inhibitor with an IC₅₀ value of 3 nM. SHP2-IN-19 can be used for glioblastoma research .

HY-155277

SHP2-IN-21	SHP2	Cancer
SHP2-IN-21 (compound 208) is a *SHP2* inhibitor with an IC₅₀ value of 3 nM. SHP2-IN-21 can be used for glioblastoma research .

HY-155274

SHP2-IN-18	SHP2	Cancer
SHP2-IN-18 (compound 183) is a *SHP2* inhibitor with an IC₅₀ value of 3 nM. SHP2-IN-18 can be used for glioblastoma research .

HY-100388AR

SHP099 monohydrochloride (Standard)	SHP2 Reference Standards Phosphatase	Cancer
SHP099 (monohydrochloride) (Standard) is the analytical standard of SHP099 (monohydrochloride). This product is intended for research and analytical applications. SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM .

HY-169111

SHP2-IN-32	SHP2	Cancer
SHP2-IN-32 (compound C6) is an orally active, allosteric *SHP2* inhibitor with an IC₅₀ value of 0.13 nM. SHP2-IN-32 exhibits antitumor activity .

HY-169918

SHP2-IN-34	SHP2	Cancer
SHP2-IN-34 (compound A8) is a phenyl urea *SHP2* inhibitor with anti-cancer activity. SHP2-IN-34 significantly suppresses tumor growth in CT26 mouse model .

HY-149759

SHP2-IN-23	SHP2 ERK	Cancer
SHP2-IN-23 (compound 30) is an orally active *SHP2* inhibitor (IC₅₀=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC₅₀=5 nM .

HY-N12915

SHP2-IN-29	SHP2 Phosphatase	Metabolic Disease Cancer
SHP2-IN-29 (Compound 3) is a potent *SHP2* inhibitor with an IC₅₀ value of 0.18 μM. SHP2-IN-29 also has inhibitory activity against PTP1B and TCPTP, with IC₅₀ values of 4.27 and 4.74 μM, respectively.

HY-173573

TK-684	Apoptosis SHP2	Cancer
TK-684 is a potent and selective allosteric *SHP2* inhibitor with IC₅₀ values of 2.1, ＞1000 nM for SHP2 ^WT, SHP22 ^PTP, respectively. TK-684 inhibits cell proliferation and induces apoptosis. TK-684 decreases the protein expression of p-AKT, p-ERK .

HY-125108

PHPS1 sodium 5 Publications Verification	SHP2 SHP1 Phosphatase	Cardiovascular Disease Cancer
PHPS1 sodium is a potent and selective *Shp2* inhibitor with K_is of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively .

HY-158762

TK-642	SHP2	Cancer
TK-642 is a highly active, selective, orally activity *SHP2* inhibitor based on pyrazole and pyrazine (IC₅₀=2.7 nmol/L). TK-642 can effectively inhibit the proliferation of esophageal carcinoma cells and induce cell apoptosis. TK-642 can be used in the study of esophageal cancer .

HY-175520

SHP2-IN-42	SHP2 Phosphatase Apoptosis	Cancer
SHP2-IN-42 is a src homology 2 domain-containing phosphatase 2 (SHP2) inhibitor with an IC₅₀ of 15 nM. SHP2-IN-42 inhibits cell proliferation and induces apoptosis and G1 phase cell cycle arrest. SHP2-IN-42 can be used for the research of cancer, such as acute myeloid leukemia (AML) .

HY-162755

SHP2-IN-30	SHP2 Apoptosis	Cancer
SHP2-IN-30 (compound 14i) is an allosteric *SHP2* inhibitor with an IC₅₀ of 104 nM. SHP2-IN-30 shows low inhibitory effect on SHP2-PTP. SHP2-IN-30 induces cell apoptosis and arrests the cell cycle at the G0/G1 phase .

HY-164427

SHP2-IN-31	SHP2 ERK	Cancer
SHP2-IN-31 is a *SHP2* inhibitor, with IC₅₀s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models .

HY-144396

SHP2-IN-8	SHP2 Phosphatase Akt Apoptosis	Cancer
SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric *SHP2* inhibitor with IC₅₀ value of 23 nM and K_i of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 °C. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells .

HY-175803

SHP2-IN-44	SHP2 ERK	Cancer
SHP2-IN-44 (Compound 26) is an allosteric and orally active SHP2 inhibitor with an IC₅₀ of 27 ?nM. SHP2-IN-44 also inhibits ERK phosphorylation (IC₅₀ of 299 ?nM) without off-target hERG activity. SHP2-IN-44 has a broad-spectrum anticancer activity, such as juvenile myelomonocytic leukemia, neuroblastoma and breast cancer. SHP2-IN-44 can be used for Noonan syndrome, LEOPARD syndrome and cancers research .

HY-100388R

SHP099 (Standard)	SHP2 Reference Standards Phosphatase	Cancer
SHP099 (Standard) is the analytical standard of SHP099. This product is intended for research and analytical applications. SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth ^[2].

HY-174322

SHP2-IN-38	SHP2 ERK Fluorescent Dye	Cancer
SHP2-IN-38 is a novel green-fluorescent *SHP2* inhibitor with IC₅₀ values of 2.89 μM (SHP2), 8.73 μM (SHP1), 11.08 μM (PTP1B), 33.07 μM (TCPTP). SHP2-IN-38 blocks the SHP2-mediated ERK signaling pathway and inhibits MV4-11 cells proliferation in vitro with IC₅₀ of 7.90 μM. SHP2-IN-38 has an excitation wavelength of 360 nm, with a maximum emission wavelength of 550 nm in DMSO and 540 nm in DMF. SHP2-IN-38 shows green fluorescence imaging in HeLa cells and zebrafish.

HY-182617

NSC-13030	SHP2	Cancer
NSC-13030 is a *SHP2* inhibitor with an IC₅₀ value of 3.2 μM. NSC-13030 reduces the proliferation and viability of breast cancer cells. NSC-13030 is applicable to breast cancer-related research .

HY-181250

SHP2-IN-46	SHP2	Cancer
SHP2-IN-46 is an orally active *SHP2* inhibitor (IC₅₀ = 11.76 μM). SHP2-IN-46 inhibits *SHP2* enzymatic activity and mediates anti-tumor activity. SHP2-IN-46 suppresses cell proliferation in various cancer cells. SHP2-IN-46 can be used in research related to lung adenocarcinoma, pancreatic cancer and hepatoblastoma .

HY-181800

SHP2-IN-47	SHP2 Akt ERK Apoptosis	Cancer
SHP2-IN-47 is a selective and potent *SHP2* inhibitor with an IC₅₀ of 0.80 μM. SHP2-IN-47 exhibits potent inhibitory activity against SHP2 ^E76K(IC₅₀ = 0.37 μM). SHP2-IN-47 functionally inhibits protein tyrosine phosphatase domains and downregulates SHP2-mediated phosphorylation of AKT and ERK. SHP2-IN-47 induces apoptosis and suppresses proliferation of cancer cells. SHP2-IN-47 can be used for the research of cancer, such as acute myelocytic leukemia .

HY-186086

RM-041	Ras	Cancer
RM-041 is a selective, orally active KRAS ^G13C (ON) inhibitor that forms a covalent complex with KRAS ^G13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRAS ^G13C mutant cancer cells. RM-041 induces regression of KRAS ^G13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N12915

SHP2-IN-29	Monophenols Microorganisms Phenols Source Classification	SHP2 Phosphatase
SHP2-IN-29 (Compound 3) is a potent *SHP2* inhibitor with an IC₅₀ value of 0.18 μM. SHP2-IN-29 also has inhibitory activity against PTP1B and TCPTP, with IC₅₀ values of 4.27 and 4.74 μM, respectively.

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SHP2+inhibitor

Inhibitors & Agonists

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