Cell Cycle includes many processes necessary for successful self-replication, and consists of DNA synthesis (S) and mitosis (M) phases separated by gap phases in the order G1–S–G2–M. S phase and M phase are usually separated by gap phases called G1 and G2, when cell-cycle progression can be regulated by various intracellular and extracellular signals. In order to move from one phase of its life cycle to the next, a cell must pass through numerous checkpoints. At each checkpoint, specialized proteins determine whether the necessary conditions exist. Progression through G1 phase is controlled by pRB proteins, and phosphorylation of pRB proteins by CDKs releases E2F factors, promoting the transition to S phase. The G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition, many proteins, such Wee1, PLK1 and cdc25, is involved the regulation of this process. The best-understood checkpoints are those activated by DNA damage and problems with DNA replication.

DNA damage response (DDR) is a series of regulatory events including DNA damage, cell-cycle arrest, regulation of DNA replication, and repair or bypass of DNA damage to ensure the maintenance of genomic stability and cell viability. Genome instability arises if cells initiate mitosis when chromosomes are only partially replicated or are damaged by a double-strand DNA break (DSB). To prevent cells with damaged DNA from entering mitosis, ATR inhibits cyclin B/Cdk1 activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1, besides, ATM and ATR also initiate DNA repair by phosphorylating several other substrates.

In cancer cells, the cell cycle regulators as well as other elements of the DDR pathway have been found to protect tumor cells from different stresses and to promote tumor progression. Thus, cell cycle proteins that directly regulate cell cycle progression (such as CDKs), as well as checkpoint kinases, Aurora kinases and PLKs, are promising targets in cancer therapy.

References:
[1] Rhind N, et al. Cold Spring Harb Perspect Biol. 2012 Oct; 4(10): a005942.
[2] Duronio RJ, et al. Cold Spring Harb Perspect Biol. 2013 Mar; 5(3): a008904.
[3] Liu W, et al. Mol Cancer. 2017 Mar 14;16(1):60.
[4] Ghelli Luserna di Rora' A, et al. J Hematol Oncol. 2017 Mar 29;10(1):77.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
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Apoptosis >
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Autophagy >
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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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3-Phenyl-2-propen-1-ol

trans-Cinnamyl alcohol is a trans-isomer of Cinnamyl alcohol. Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity. trans-Cinnamyl alcohol, belongs to the class of organic compounds known as cinnamyl alcohols, is a primary metabolite[1].

  • CAS Number: 4407-36-7
  • MF: C9H10O
  • MW: 134.175
  • Catalog: PPAR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 250.0±0.0 °C at 760 mmHg
  • Melting Point: 34°C
  • Flash Point: 124.8±14.5 °C

6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride

Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma[1][3][4].

  • CAS Number: 571189-11-2
  • MF: C24H31Cl2N7O2
  • MW: 520.45500
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD1152

AZD1152 is a pro-drug of Barasertib-hQPA, which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

  • CAS Number: 722543-31-9
  • MF: C26H31FN7O6P
  • MW: 587.540
  • Catalog: Aurora Kinase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-(6-amino-8-methylamino-purin-9-yl)-2-(hydroxymethyl)oxolan-3-ol

2'-Deoxy-8-methylamino-adenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 13389-10-1
  • MF: C11H16N6O3
  • MW: 280.28
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.85g/cm3
  • Boiling Point: 634.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 337.5ºC

7-n-Butyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine

7-n-Butyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 2389988-45-6
  • MF: C14H21N5O6
  • MW: 355.35
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMT-locG(ib) Phosphoramidite

DMT-locG(ib) Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 206055-77-8
  • MF: C45H54N7O9P
  • MW: 867.93
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GW1929

GW1929 is a potent PPAR-γ activator, with pKis of 8.84, < 5.5, and < 6.5 for human PPAR-γ, PPAR-α, and PPAR-δ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively.

  • CAS Number: 196808-24-9
  • MF: C30H29N3O4
  • MW: 495.569
  • Catalog: PPAR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 749.2±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 406.9±32.9 °C

Topoisomerase II inhibitor 10

Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells[1].

  • CAS Number: 2488208-96-2
  • MF: C27H20N6O7S
  • MW: 572.55
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-Azido-2’-deoxy-5-methyl cytidine

2’-Azido-2’-deoxy-5-methyl cytidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 2095417-75-5
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mivobulin

Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity[1].

  • CAS Number: 122332-18-7
  • MF: C17H19N5O2
  • MW: 315.40700
  • Catalog: Microtubule/Tubulin
  • Density: 1.36
  • Boiling Point: 483ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 245.9ºC

Palmitic acid-d17

Palmitic acid-d17 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].

  • CAS Number: 81462-28-4
  • MF: C16H15D17O2
  • MW: 273.53
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Diaveridine

Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

  • CAS Number: 5355-16-8
  • MF: C13H16N4O2
  • MW: 260.292
  • Catalog: Bacterial
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 506.1±60.0 °C at 760 mmHg
  • Melting Point: 232 - 236ºC
  • Flash Point: 259.9±32.9 °C

Lycobetaine(Ungeremine)

Ungeremine, a phenanthridine type alkaloid, is extracted of the bulbs of Pancratium Illyricum. Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases. Ungeremine displays cytotoxic activity towards the 9 cancer cell lines, including drug-sensitive and MDR phenotypes. Ungeremine induced ferroptosis, necroptosis, autophagy as well as apoptosis mediated by caspase activation, MMP alteration and increase ROS production[1][2].

  • CAS Number: 2121-12-2
  • MF: C16H12NO3
  • MW: 266.27100
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 270-272ºC (dec.)
  • Flash Point: N/A

Itf3756

ITF3756 is a selective histone deacetylase 6 (HDAC6) inhibitor bearing a pentaheterocyclic scaffold.

  • CAS Number: 2247608-27-9
  • MF: C13H11N5O2S
  • MW: 301.32
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GW-8510

GW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities[1][2][3].

  • CAS Number: 222036-17-1
  • MF: C21H15N5O3S2
  • MW: 449.51
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BML-266

JFD00244 is a sirtuin 2 (SIRT2) inhibitor. Anti-tumor effect[1].

  • CAS Number: 96969-83-4
  • MF: C30H26N2O4
  • MW: 478.538
  • Catalog: Sirtuin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 780.2±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 425.7±32.9 °C

MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan

MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a drug-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM)[1].

  • CAS Number: 2414254-51-4
  • MF: C55H60FN9O13
  • MW: 1074.12
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Taxinine B

Taxinine B is a taxoid that can be isolated from Japanese Yew Taxus Cuspid. Taxinine B inhibits CaCl2-induced depolymerization of microtubule. Taxinine B is useful for overcoming multidrug resistance in tumor cells[1].

  • CAS Number: 18457-44-8
  • MF: C37H44O11
  • MW: 664.74
  • Catalog: Microtubule/Tubulin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 705.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 286.7±32.9 °C

GW297361

GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells. GW297361 inhibits yeast Cdk1 and Pho85 with IC50s of 20 nM and 400 nM in vitro, respectively[1].

  • CAS Number: 388627-21-2
  • MF: C16H12N4O3S2
  • MW: 372.42
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methyl 4-C-hydroxymethyl-2,3-O-isopropylidene-beta-D-ribofuranoside

Methyl 4-C-hydroxymethyl-2,3-O-isopropylidene-beta-D-ribofuranoside is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 55797-67-6
  • MF: C10H18O6
  • MW: 234.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

THAL SNS 032

THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN)[1].

  • CAS Number: 2139287-33-3
  • MF: C40H52N8O10S2
  • MW: 869.02
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KIRA6

KIRA6 allosterically inhibits IRE1α RNase kinase activity with an IC50 of 0.6 µM.

  • CAS Number: 1589527-65-0
  • MF: C28H25F3N6O
  • MW: 518.533
  • Catalog: IRE1
  • Density: 1.4±0.1 g/cm3
  • 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

5'-O-(4,4'-DIMETHOXYTRITYL)-N2-ISOBUTYRYL-2'-DEOXYGUANOSINE-3'-(METHYL-N,N-DIISOPROPYL)PHOSPHORAMIDITE

2'-Deoxyguanosine-(N-iBu)-3'-methyl-phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.

  • CAS Number: 84416-84-2
  • MF: C42H53N6O8P
  • MW: 800.88
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-(3-Trifluoromethylbenzyl)-3’-deoxyadenosine

N6-(3-Trifluoromethylbenzyl)-3’-deoxyadenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 2305415-80-7
  • MF: C18H18F3N5O3
  • MW: 409.36
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(3aR,5R,6aS)-5-[[tert-butyl(diphenyl)silyl]oxymethyl]-2,2-dimethyl-3a,6a-dihydrofuro[2,3-d][1,3]dioxol-6-one

5-O-TBDPS-1,2-di-O-isopropy lidene-3-keto-alpha-D-xylofuranoside is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 75783-45-8
  • MF: C24H30O5Si
  • MW: 426.58
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Indimitecan

Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities[1].

  • CAS Number: 915360-05-3
  • MF: C25H21N3O6
  • MW: 459.45100
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

T2AA

T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that prevents DNA repair, increases double-strand break (DSB) formation and promotes necroptosis and cell cycle arrest in G1 phase[1].

  • CAS Number: 1380782-27-3
  • MF: C15H15I2NO3
  • MW: 511.093
  • Catalog: DNA/RNA Synthesis
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 568.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 297.4±30.1 °C

(11aS)-7-Methoxy-8-hydroxy-2,3,5,11aβ-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one

Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct[1][2].

  • CAS Number: 81307-24-6
  • MF: C13H14N2O3
  • MW: 246.26200
  • Catalog: Apoptosis
  • Density: 1.43g/cm3
  • Boiling Point: 520.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 268.6ºC

LY3023414

LY3023414 potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. LY3023414 potently inhibits mTORC1/2 at low nanomolar concentrations.

  • CAS Number: 1386874-06-1
  • MF: C23H26N4O3
  • MW: 406.478
  • Catalog: DNA-PK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 591.7±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 311.6±30.1 °C