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intracranial

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Acyltransferase (1) Akt (1) Apoptosis (1) Dopamine Transporter (1) EGFR (3) Enolase (1) ERK (3) FAK (1) MMP (1) Molecular Glues (1) NF-κB (2) p38 MAPK (1) Parasite (1) Raf (1) RET (1) Ribosomal S6 Kinase (RSK) (1) ROS Kinase (1) SDCBP (1)
By Research Areas:	Cancer (10) Cardiovascular Disease (1) Infection (1) Metabolic Disease (1) Neurological Disease (6)

Inhibitors & Agonists

Fluorescent Dye

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153268

Silevertinib 1 Publications Verification BDTX-1535; EGFR-IN-76	EGFR	Cancer
BDTX-1535 (EGFR-IN-76) is an orally available, blood-brain permeable, selective EGFR inhibitor with anti-tumor activity. BDTX-1535 is indicated in a variety of models including non-small cell lung cancer, glioblastoma patient-derived tumors, and intracranial tumors .

HY-131904A

Hex	Enolase Parasite	Infection Cancer
Hex is an enolase inhibitor and antimalarial agent with K_i values of 74.4 nM and 269.4 nM for ENO2 and ENO1, respectively. Hex is a NfENO and TbENO inhibitor with IC₅₀s value of 0.14 μM and 2.1 μM, respectively. Hex has antimalarial activity against Plasmodium falciparum 3D7, Naegleria fowleri trophozoites and Plasmodium berghei ANKA strain. Hex has anti-tumor effects against intracranial tumors .

HY-117902

SRI-31142	Dopamine Transporter	Neurological Disease
SRI-31142 is a putative, brain-penetrant allosteric inhibitor of the dopamine transporter (DAT). In behavioral studies using intracranial self-stimulation (ICSS), SRI-31142 did not produce the abuse-related effects seen with cocaine and GBR-12935, but instead reduced ICSS responses and dopamine levels in the nucleus accumbens (NAc) at effective doses. SRI-31142 also blocked cocaine-induced increases in ICSS and NAc dopamine .

HY-161275

BI-4732	EGFR Akt ERK Ribosomal S6 Kinase (RSK)	Cancer
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC₅₀ values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-124813

PDZ1i 113B7	FAK EGFR MMP NF-κB SDCBP	Cancer
PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer .

HY-175599

Z6466608628	Molecular Glues	Cardiovascular Disease Cancer
Z6466608628 is a selective PPIL4 molecular glue degrader with an EC₅₀ of 0.34  μM. PPIL4 is a regulator of the B ^ACR spliceosome and it is essential for brain angiogenesis. Z6466608628 can be used for intracranial aneurysm (IA) research .

HY-150639

Everafenib	Raf	Cancer
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of ^V600EBRAF melanoma cell lines with IC₅₀ values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .

HY-178391

SMU-037	ROS Kinase p38 MAPK ERK Apoptosis	Cancer
SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .

HY-178061

APS03118	ERK RET	Cancer
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC₅₀ values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .

HY-149696

IR-Crizotinib	NF-κB	Cancer
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC₅₀=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .

HY-117656

ESI-05 4 Publications Verification NSC 116966	Acyltransferase	Neurological Disease Metabolic Disease
ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC₅₀ of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders .

Cat. No.	Product Name	Type

HY-149696

IR-Crizotinib	Dyes
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC₅₀=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .

IR-Crizotinib

Dyes

IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC₅₀=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .

Cat. No.	Product Name	Target	Research Area

HY-P5118A

Tat-peptide 190-208 TFA	Peptides	Neurological Disease
Tat-peptide 190-208 TFA is a cell-permeable and Tat-labeled fusion peptide, corresponding to residues 190-208 of rat G3BP1. Tat sequence from HIV, is placed at the least conserved end of the sequence, for cell permeability. Tat-peptide 190-208 TFA increases axon growth and increases the number of neurites per neuron. Tat-peptide 190-208 TFA likely exhibits an axon intrinsic mechanism. Tat-peptide 190-208 TFA can be used for ischemic protection during endovascular repair for intracranial aneurysms .

HY-P5118

Tat-peptide 190-208	Peptides	Neurological Disease
Tat-peptide 190-208 is a cell-permeable and Tat-labeled fusion peptide, corresponding to residues 190-208 of rat G3BP1. Tat sequence from HIV, is placed at the least conserved end of the sequence, for cell permeability. Tat-peptide 190-208 increases axon growth and increases the number of neurites per neuron. Tat-peptide 190-208 likely exhibits an axon intrinsic mechanism. Tat-peptide 190-208 can be used for ischemic protection during endovascular repair for intracranial aneurysms .

HY-P11029

CES	Peptides	Cancer
CES (CESPLLSEC) is a homing peptide targeting Synaptosomal associated protein 25 (SNAP25). CES specifically homes in intracranial U87MG and the WT-glioblastoma (GBM) model. CES can be used as a targeting peptide for drug delivery for cancers research .

HY-P5119

Tat-peptide control 168-189	Peptides	Neurological Disease
Tat-peptide 168-189 is a cell-permeable and Tat-labeled fusion peptide, corresponding to residues 168-189 of rat G3BP1. Tat sequence from HIV, is placed at the least conserved end of the sequence, for cell permeability. Tat-peptide 168-189 is the negtive control of Tat-peptide 190-208 (HY-P5118), as Tat-peptide 190-208 increases axon growth and increases the number of neurites per neuron .

HY-P5119A

Tat-peptide control 168-189 TFA	Peptides	Neurological Disease
Tat-peptide 168-189 is a cell-permeable and Tat-labeled fusion peptide, corresponding to residues 168-189 of rat G3BP1. Tat sequence from HIV, is placed at the least conserved end of the sequence, for cell permeability. Tat-peptide 168-189 is the negtive control of Tat-peptide 168-189 TFA (HY-P5118A), as Tat-peptide 168-189 TFA increases axon growth and increases the number of neurites per neuron .

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