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TMZ

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (8) Autophagy (5) Bcl-2 Family (1) Caspase (1) DNA Alkylator/Crosslinker (4) DNA Methyltransferase (2) DNA/RNA Synthesis (4) Dopamine Receptor (2) Drug Derivative (1) Drug Metabolite (4) Endogenous Metabolite (1) Environmental Pollutants (1) ERK (2) FAK (1) Fungal (1) HDAC (2) Hedgehog (1) Histone Methyltransferase (1) Isotope-Labeled Compounds (2) Ligands for Target Protein for PROTAC (1) MDM-2/p53 (1) MMP (1) mTOR (2) PARP (3) PDGFR (2) Phosphatase (1) PROTACs (1) Reference Standards (2) Somatostatin Receptor (2) Src (1)
By Research Areas:	Cancer (26) Neurological Disease (7)

By Targets:

Apoptosis (8)

Autophagy (5)

Bcl-2 Family (1)

Caspase (1)

DNA Alkylator/Crosslinker (4)

DNA Methyltransferase (2)

DNA/RNA Synthesis (4)

Dopamine Receptor (2)

Drug Derivative (1)

Drug Metabolite (4)

Endogenous Metabolite (1)

Environmental Pollutants (1)

ERK (2)

FAK (1)

Fungal (1)

HDAC (2)

Hedgehog (1)

Histone Methyltransferase (1)

Isotope-Labeled Compounds (2)

Ligands for Target Protein for PROTAC (1)

MDM-2/p53 (1)

MMP (1)

mTOR (2)

PARP (3)

PDGFR (2)

Phosphatase (1)

PROTACs (1)

Reference Standards (2)

Somatostatin Receptor (2)

Src (1)

By Research Areas:

Cancer (26)

Neurological Disease (7)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17364

Temozolomide Maximum Cited Publications 189 Publications Verification NSC 362856; CCRG 81045; TMZ	DNA Alkylator/Crosslinker Autophagy Apoptosis	Cancer
Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects .

HY-B0896

Triacetin Glyceryl triacetate; 1,2,3-Triacetoxypropane	Environmental Pollutants Fungal Endogenous Metabolite	Cancer
Triacetin (Glyceryl triacetate) is a synthetic compound that is a triester of glycerol and acetic acid, orally active. Triacetin increases acetate bioavailability in glioma cells. Triacetin induces glioma cell growth arrest and Apoptosis. Triacetin freely crosses the blood brain barrier/plasma membrane. Triacetin increases histone acetylation and enhances Temozolomide (HY-17364) (TMZ) chemotherapeutic efficacy .

HY-119696

MTIC	Drug Metabolite	Neurological Disease Cancer
MTIC, the active metabolite of Temozolomide (TMZ), is a DNA alkylating agent. MTIC has antitumor activity .

HY-15588

L189 3 Publications Verification	DNA/RNA Synthesis	Cancer
L189 is a DNA ligase inhibitor. L189 has inhibition effect for DNA Ligase I, III and IV with IC₅₀ values of 5 μM, 9 μM and 5 μM, respectively. L189 has no cytotoxicity and individually increase cell death. L189 can be used for the research of cancer .

HY-163317A

*MMC(TMZ)-TOC TFA*	Somatostatin Receptor	Cancer
MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC TFA targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC TFA can be used for the research of cancer .

HY-120105

NSC666715	DNA/RNA Synthesis Apoptosis MDM-2/p53 Bcl-2 Family Caspase PARP	Cancer
NSC666715 is a DNA polymerase β (Pol-β) inhibitor. NSC666715 directly and specifically interacts with Pol-β, interferes with its binding to damaged DNA, blocks its dRP lyase activity, and inhibits Pol-β-mediated SN- and LP-BER. NSC666715 induces AP site accumulation and S-phase cell cycle arrest, and triggers senescence and apoptosis (apoptosis) via the p53/p21 pathway in colorectal cancer cells. NSC666715 enhances TMZ (HY-17364)-induced DNA damage, senescence and apoptosis, and potentiates the cytotoxicity of TMZ. NSC666715 inhibits tumor growth in colon cancer xenograft models. NSC666715 can be used in research related to colorectal cancer .

HY-162384

EPIC-0628	Histone Methyltransferase	Cancer
EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency .

HY-163317

*MMC(TMZ)-TOC*	Somatostatin Receptor	Cancer
MMC(TMZ)-TOC has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC can be used for the research of cancer .

HY-17364R

Temozolomide (Standard) NSC 362856 (Standard); CCRG 81045 (Standard); TMZ (Standard)	Reference Standards DNA Alkylator/Crosslinker Autophagy Apoptosis	Cancer
Temozolomide (Standard) is the analytical standard of Temozolomide. This product is intended for research and analytical applications. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects .

HY-175299

Hedgehog IN-11	Hedgehog Apoptosis DNA Methyltransferase	Cancer
Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM) .

HY-115690

K-TMZ	Drug Derivative	Cancer
K-TMZ is a derivative of methyl ketone, which exhibits antitumor efficacy against O ⁶ -methylguanine DNA methyltransferase (MGMT) deficient cell. K-TMZ can be used for research of glioblastoma .

HY-10615

A-620223 1 Publications Verification	PARP	Cancer
A-620223 is a PARP-1 inhibitor with a K_i of 8 nM against PARP-1 and EC₅₀ of 3 nM in a whole cell assay. A-620223 demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with Temozolomide (TMZ) (HY-17364) and in an MX-1 breast xenograph model in combination with Cisplatin (HY-17394). A-620223 can be used for the studies of melanoma and breast cancer .

HY-169433

Naph-Se-TMZ	PROTACs HDAC	Cancer
Naph-Se-TMZ is a PROTAC-like HDAC1 degrader. Naph-Se-TMZ can reduce the total HDAC activity in glioma cells and enhance the inhibitory effect of Temozolomide (HY-17364). Naph-Se-TMZ consists of the target protein ligand (red part) Temozolomide (HY-17364), the DNA-targeting intercalator (blue part) Nitro-Naphthalimide-C2-acylamide (HY-169437) and the molecular linker (black part). At the same time, the active control of the target protein ligand is: Temozolomide-amino hydrochloride (HY-169439), and the DNA targeting intercalator + linker is: NNISC-2 (HY-169438) .

HY-169002

PP5-IN-2	Phosphatase	Cancer
PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC₅₀ value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .

HY-119696S

MTIC-d3	Isotope-Labeled Compounds Drug Metabolite	Neurological Disease Cancer
MTIC-d₃ is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane .

HY-169439

Temozolomide-amino hydrochloride	Ligands for Target Protein for PROTAC HDAC	Cancer
Temozolomide-amino hydrochloride (compound 8) is an activity control for the target protein ligand of Naph-Se-TMZ (HY-169433) .

HY-164402

NSC-124854	DNA/RNA Synthesis	Cancer
NSC-124854 is a DNA polymerase β (Pol-β) inhibitor with an IC₅₀ of 5.3 μM. NSC-124854 has antitumor activity .

HY-119696R

MTIC (Standard)	Reference Standards Drug Metabolite	Neurological Disease Cancer
MTIC (Standard) is the analytical standard of MTIC. This product is intended for research and analytical applications. MTIC, the active metabolite of Temozolomide (TMZ), is a DNA alkylating agent. MTIC has antitumor activity [1][2][3][4].

HY-169437

Nitro-Naphthalimide-C2-acylamide	DNA Alkylator/Crosslinker	Cancer
Nitro-Naphthalimide-C2-acylamide is a DNA intercalator. Nitro-Naphthalimide-C2-acylamide can be used for the synthesis of PROTAC-like Naph-Se-TMZ (HY-169433) .

HY-169438

NNISC-2	DNA Alkylator/Crosslinker	Cancer
NNISC-2 (compound 4) is a DNA intercalator-linker conjugate of Naph-Se-TMZ (HY-169433), which is composed of DNA intercalator (blue part) Nitro-Naphthalimide-C2-acylamide (HY-169437) and a linker (black part) .

HY-149003

PARP1-IN-10	PARP Apoptosis	Cancer
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC₅₀ value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .

HY-101349

L 741742	Dopamine Receptor Apoptosis Autophagy PDGFR ERK mTOR	Neurological Disease Cancer
L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with K_i values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .

HY-101349A

L 741742 hydrochloride	Dopamine Receptor Apoptosis Autophagy PDGFR ERK mTOR	Neurological Disease Cancer
L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with K_i values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .

HY-180540

MGMT-IN-1	DNA Methyltransferase	Neurological Disease Cancer
MGMT-IN-1 (Compound 2) is a light-activated MGMT inhibitor. MGMT-IN-1 can effectively enhance the cytotoxicity of Temozolomide (TMZ) (HY-17364) only under light conditions, significantly increasing the DNA damage caused by TMZ. MGMT-IN-1 can be used for the study of chordoma .

HY-119696S1

MTIC-13C	Isotope-Labeled Compounds Drug Metabolite	Neurological Disease Cancer
MTIC- ¹³C is the ¹³C-labeled MTIC (HY-119696). MTIC, the active metabolite of Temozolomide (TMZ), is a DNA alkylating agent. MTIC has antitumor activity

HY-138195

NEO212	DNA/RNA Synthesis Apoptosis FAK Src MMP Autophagy	Cancer
NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0896

Triacetin Glyceryl triacetate; 1,2,3-Triacetoxypropane	Structural Classification Natural Products Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Environmental Pollutants Fungal Endogenous Metabolite
Triacetin (Glyceryl triacetate) is a synthetic compound that is a triester of glycerol and acetic acid, orally active. Triacetin increases acetate bioavailability in glioma cells. Triacetin induces glioma cell growth arrest and Apoptosis. Triacetin freely crosses the blood brain barrier/plasma membrane. Triacetin increases histone acetylation and enhances Temozolomide (HY-17364) (TMZ) chemotherapeutic efficacy .

Cat. No.	Product Name	Chemical Structure

HY-119696S

MTIC-d3
MTIC-d₃ is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane .

HY-119696S1

MTIC-13C
MTIC- ¹³C is the ¹³C-labeled MTIC (HY-119696). MTIC, the active metabolite of Temozolomide (TMZ), is a DNA alkylating agent. MTIC has antitumor activity

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TMZ

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Isotope-Labeled Compounds

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