DNA alkylator/crosslinker is a molecule that alkylates DNA or can cross link with DNA. DNA alkylator/crosslinker can have mutagenic, pharmaceutical, or other effects. Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion or a carbene. Alkylating agents are widely used in chemistry because the alkyl group is probably the most common group encountered in organic molecules. Selective alkylation, or adding parts to the chain with the desired functional groups, is used, especially if there is no commonly available biological precursor. Alkylation with only one carbon is termed methylation. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Crosslinking of DNA occurs when various exogenous or endogenous agents react with two different positions in the DNA. This can either occur in the same strand (intrastrand crosslink) or in the opposite strands of the DNA (interstrand crosslink). Crosslinks also occur between DNA and protein. DNA replication is blocked by crosslinks, which causes replication arrest and cell death if the crosslink is not repaired. The RAD51 family plays a role in repair.


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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
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NF-κB >
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PROTAC >
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Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
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Vitamin D Related >
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Melflufen

Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells[1][2].

  • CAS Number: 380449-51-4
  • MF: C24H30Cl2FN3O3
  • MW: 498.41800
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Melflufen hydrochloride

Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells[1][2].

  • CAS Number: 380449-54-7
  • MF: C24H31Cl3FN3O3
  • MW: 534.88
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methylnitronitrosoguanidine

Methylnitronitrosoguanidine (MNNG) is an alkylating agent with toxic and mutagenic effects[1].

  • CAS Number: 70-25-7
  • MF: C2H5N5O3
  • MW: 147.09
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 207.8±23.0 °C at 760 mmHg
  • Melting Point: 118°C (dec.)
  • Flash Point: 79.5±22.6 °C

LP-284

LP-284 is a potent DNA alkylating agent that kills solid tumours. LP-284 can be used in the studies of hematologic cancers with compromised DNA repair, such as mantle cell lymphoma (MCL)[1][2].

  • CAS Number: 2412580-47-1
  • MF: C16H20N2O4
  • MW: 304.34
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PR-104A

PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity[1]. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL)[2].

  • CAS Number: 680199-06-8
  • MF: C14H19BrN4O9S
  • MW: 499.29100
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Procarbazine hydrochloride

Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.

  • CAS Number: 366-70-1
  • MF: C12H20ClN3O
  • MW: 257.760
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: 384.6ºC at 760 mmHg
  • Melting Point: 223ºC
  • Flash Point: 148.9ºC

SJG-136

SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA; SJG-136 has potent antitumor activity.

  • CAS Number: 232931-57-6
  • MF: C31H32N4O6
  • MW: 556.60900
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.36g/cm3
  • Boiling Point: 805.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 441ºC

Duocarmycin GA

Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines.

  • CAS Number: 1613286-59-1
  • MF: C26H25ClN4O3
  • MW: 476.95
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mafosfamide Sodium Salt

Mafosfamide sodium salt (Z 7557 sodium salt) targets nuclear DNA, forms DNA cross-links and inhibits DNA synthesis. Mafosfamide sodium salt, a cyclophosphamide analogue, induces apoptosis in lymphoblastoid cells. Mafosfamide sodium salt has antitumor activity[1][2].

  • CAS Number: 84211-05-2
  • MF: C9H18Cl2N2NaO5PS2
  • MW: 401.26700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Phenylacetic acid mustard

Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil (HY-13593). Chlorambucil is an alkylating agent with antitumor activity[1].

  • CAS Number: 10477-72-2
  • MF: C12H15Cl2NO2
  • MW: 276.15900
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: 195.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 89.6ºC

(+)-CBI-CDPI2

(+)-CBI-CDPI2 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI2 is an antibody drug conjugates (ADCs) toxin.

  • CAS Number: 128300-15-2
  • MF: C36H28N6O4
  • MW: 608.64500
  • Catalog: ADC Cytotoxin
  • Density: 1.64g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mitomycin C

Mitomycin C is an antitumor drug and antibiotic that shows extraordinary ability to inhibit DNA synthesis.

  • CAS Number: 50-07-7
  • MF: C15H18N4O5
  • MW: 334.327
  • Catalog: Bacterial
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 532.0±60.0 °C at 760 mmHg
  • Melting Point: 360 °C
  • Flash Point: 275.5±32.9 °C

PR-104

PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A[1].

  • CAS Number: 851627-62-8
  • MF: C14H20BrN4O12PS
  • MW: 579.27100
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+)-CBI-CDPI1

(+)-CBI-CDPI1 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI1 is an antibody drug conjugates (ADCs) toxin.

  • CAS Number: 128300-14-1
  • MF: C25H20N4O3
  • MW: 424.45
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mipicoledine

Mipicoledine is a potential neuro-alkylating agent for study of glioblastoma and metastatic cancers involving the central nervous system[1].

  • CAS Number: 942149-56-6
  • MF: C35H48Cl5NO4
  • MW: 724.02
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 689.2±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 370.6±31.5 °C

N-Nitroso-N-methylurea

N-Nitroso-N-methylurea (NMU;MNU;NMH) is a potent carcinogen, mutagen and teratogenand. N-Nitroso-N-methylurea is a direct-acting alkylating agent that interacts with DNA. N-Nitroso-N-methylurea targets multiple animal organs to cause various cancer and/or degenerative disease. N-Nitroso-N-methylurea is also a precursor in the synthesis of diazomethane[1][2][3][4].

  • CAS Number: 684-93-5
  • MF: C2H5N3O2
  • MW: 103.080
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 164.3±23.0 °C at 760 mmHg
  • Melting Point: 119-124°C
  • Flash Point: 53.1±22.6 °C

2-Iodoacetamide-d4

2-Iodoacetamide-d4 is the deuterium labeled 2-Iodoacetamide[1]. 2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics[2][3].

  • CAS Number: 1219802-64-8
  • MF: C2D4INO
  • MW: 188.99
  • Catalog: DNA Alkylator/Crosslinker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,6-DIBROMO-1,6-DIDEOXY-D-MANNITOL

Mitobronitol (Myelobromol; DBM) is a brominated analog of mannitol, also known as an anticancer agent that is classified as an alkylating agent. Mitobronitol has potential for myelosuppression associated with significantly decreased risk for several complications of allogeneic bone marrow transplantation in accelerated chronic granulocytic leukemia[1][2].

  • CAS Number: 488-41-5
  • MF: C6H12Br2O4
  • MW: 307.96500
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 2.117g/cm3
  • Boiling Point: 511.2ºC at 760mmHg
  • Melting Point: 176-178°
  • Flash Point: 263ºC

Duocarmycin MB

Duocarmycin MB is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MB can be used against multi-drug resistant cell lines.

  • CAS Number: 1613286-58-0
  • MF: C27H26ClN3O4
  • MW: 491.97
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ranimustine

Ranimustine (MCNU) is a nitrosourea alkylating agent, can be used for research of chronic myelogenous leukemia and polycythemia vera[1][3][4].

  • CAS Number: 58994-96-0
  • MF: C10H18ClN3O7
  • MW: 327.71900
  • Catalog: DNA Alkylator/Crosslinker
  • Density: 1.69 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Duocarmycin MA

Duocarmycin MA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-drug resistant cell lines.

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A