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central nervous system (CNS) cancer

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By Targets:	Antibody-Drug Conjugates (ADCs) (1) Bacterial (1) Bcl-2 Family (1) c-Myc (1) CDK (1) DNA/RNA Synthesis (1) Drug Derivative (1) EGFR (4) Epigenetic Reader Domain (1) GABA Receptor (1) HDAC (1) HIV (1) Methionine Adenosyltransferase (MAT) (2) PKC (1) Topoisomerase (1)
By Research Areas:	Cancer (13) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (3) Neurological Disease (9)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-105231

Bryostatin 1 2 Publications Verification	PKC HIV Bacterial	Infection Neurological Disease Inflammation/Immunology Cancer
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with K_is of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties .

HY-170554

ABBV-706	Antibody-Drug Conjugates (ADCs) Topoisomerase DNA/RNA Synthesis	Inflammation/Immunology Cancer
ABBV-706 is a SEZ6-targeted topoisomerase 1 inhibitor Antibody-Drug Conjugates (ADCs), which is composed of the Linker-Payload conjugation (HY-148820) and the Anti-SEZ6 Antibody (SC17) (HY-P991041). ABBV-706 can inhibit cancer cells proliferation and induce DNA damage and G2/M arrest. ABBV-706 exhibits high efficacy against small cell lung cancer (SCLC), neuroendocrine tumors (NENs) and central nervous system (CNS) tumors .

HY-172429

Enozertinib ORIC-114	EGFR	Neurological Disease Cancer
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .

HY-132806

Alogabat RG-7816; RO-7017773	GABA Receptor	Neurological Disease
Alogabat is a positive allosteric modulator (PAM) and agonist (K_i <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .

HY-172429A

Enozertinib hemihydrate ORIC-114 hemihydrate	EGFR	Neurological Disease Cancer
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .

HY-145777

AGI-43192	Methionine Adenosyltransferase (MAT)	Neurological Disease Cancer
AGI-43192 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that limitedly penetrates the blood-brain barrier. AGI-43192 exhibits inhibitory activitity against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC₅₀s of 32 and 14 nM. AGI-43192 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-43192 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer .

HY-145778

AGI-41998	Methionine Adenosyltransferase (MAT)	Neurological Disease Cancer
AGI-41998 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that effectively penetrates the blood-brain barrier. AGI-41998 exhibits inhibitory activities against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC₅₀s of 22 nM and 34 nM. AGI-41998 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-41998 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer .

HY-164307

Pebezertinib BLU 451; LNG-451	EGFR	Cancer
Pebezertinib (BLU 451) is an orally active inhibitor for EGFR. Pebezertinib exhibits the ability to penetrate the central nervous system (CNS). Pebezertinib can be used for research about non-small cell lung cancer carrying EGFR exon 20 insertion .

HY-160446

BET-IN-24	Epigenetic Reader Domain	Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Bet-in-24 (example 2) is a bromodomain and extra-terminal (BET) inhibitor. BET-IN-24 can be used in the study of virology, heart failure, inflammation, central nervous system (CNS) diseases and many cancers

HY-163629

Anticancer agent 224	Drug Derivative	Cancer
Anticancer agent 224 (Compound 16) is an anticancer agent that can effectively inhibit the growth of central nervous system (CNS), kidney and breast cancer cell, with a GI₅₀ value ranging from 0.6 to 12.8 μM .

HY-178499

CDK9-IN-44	CDK c-Myc Bcl-2 Family	Neurological Disease Cancer
CDK9-IN-44 (Compound 7) is a selective CDK9 inhibitor (IC₅₀=7.6 μM). CDK9-IN-44 inhibits CDK9/cyclin T1 kinase activity, blocking transcriptional elongation, reducing the expression of pro-cancer proteins (such as MCL1, c-MYC), and inducing tumor cell apoptosis. CDK9-IN-44 is promising for research of glioblastoma (GBM) and central nervous system (CNS) disorders .

HY-163806

NT376	HDAC	Neurological Disease Cancer
NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC₅₀ value of 32 nM, similar to NT160 (HY-149285) (IC₅₀= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases .

HY-N18126

13b,14-Dihydrorutaecarpine	Others	Cancer
13b,14-Dihydrorutaecarpine is a cytotoxin derived from dihydrorutaecarpine. 13b,14-Dihydrorutaecarpine exerts selective cytotoxicity against central nervous system (CNS) and prostate cancer cell lines (GI₅₀=0.02 μM and 0.2 μM). 13b,14-Dihydrorutaecarpine can be used in the research of central nervous system (CNS) cancer, ovarian cancer, prostate cancer and renal cancer .

HY-109189A

Rezivertinib hydrochloride BPI-7711 hydrochloride	EGFR	Cancer
Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC) .

ABBV-706	Fluorescent Dyes
ABBV-706 is a SEZ6-targeted topoisomerase 1 inhibitor Antibody-Drug Conjugates (ADCs), which is composed of the Linker-Payload conjugation (HY-148820) and the Anti-SEZ6 Antibody (SC17) (HY-P991041). ABBV-706 can inhibit cancer cells proliferation and induce DNA damage and G2/M arrest. ABBV-706 exhibits high efficacy against small cell lung cancer (SCLC), neuroendocrine tumors (NENs) and central nervous system (CNS) tumors .

Bryostatin 1 2 Publications Verification	Anti-inflammation/Immunoregulatory Neurological Disease Classification of Application Fields Marine natural products Other marine organisms Disease Research Infection Macrolide Antibiotics Animals Antibiotics Anticancer Inflammation/Immunology Disease Research Fields Source Classification	PKC HIV Bacterial
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with K_is of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties .

13b,14-Dihydrorutaecarpine	Structural Classification Alkaloids Evodia rutaecarpa (Juss.) Benth. Rutaceae Plants Indole Alkaloids Source Classification	Others
13b,14-Dihydrorutaecarpine is a cytotoxin derived from dihydrorutaecarpine. 13b,14-Dihydrorutaecarpine exerts selective cytotoxicity against central nervous system (CNS) and prostate cancer cell lines (GI₅₀=0.02 μM and 0.2 μM). 13b,14-Dihydrorutaecarpine can be used in the research of central nervous system (CNS) cancer, ovarian cancer, prostate cancer and renal cancer .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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central nervous system (CNS) cancer

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