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 >
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Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
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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
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Aurora kinase inhibitor-9

Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity[1].

  • CAS Number: 2419107-09-6
  • MF: C19H17Cl2N3O4S
  • MW: 454.33
  • Catalog: Aurora Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Naphthyl-beta-methylaminocarbony-3’-O-acetyl-2’-O-methyl-5’-O-DMTr-uridine

5-Naphthyl-beta-methylaminocarbony-3’-O-acetyl-2’-O-methyl-5’-O-DMTr-uridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].

  • CAS Number: 2095417-00-6
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Shepherdin 79-87

Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity[1].

  • CAS Number: 861224-28-4
  • MF: C41H64N12O12S
  • MW: 949.09
  • Catalog: Survivin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3,7,4'-trihydroxyflavone

3,7,4'-Trihydroxyflavone, isolated from Rhus javanica var. roxburghiana, is a flavonoid with DNA strand-scission activity[1].

  • CAS Number: 2034-65-3
  • MF: C15H10O5
  • MW: 270.24
  • Catalog: DNA/RNA Synthesis
  • Density: 1.579g/cm3
  • Boiling Point: 539.7ºC at 760mmHg
  • Melting Point: 310-311ºC
  • Flash Point: 210.6ºC

2'-OMe-ibu-G Phosphoramidite

2'-OMe-G(ibu) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.

  • CAS Number: 150780-67-9
  • MF: C45H56N7O9P
  • MW: 869.941
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IXA4

IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation[1].

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

2-Methoxyestradiol

2-Methoxyestradiol is an angiogenesis inhibitor and apoptosis inducer with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.

  • CAS Number: 362-07-2
  • MF: C19H26O3
  • MW: 302.408
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 464.4±45.0 °C at 760 mmHg
  • Melting Point: 188-190°C
  • Flash Point: 234.7±28.7 °C

5’-Deoxy-5’-iodo-2’-O-methyl-5-methyluridine

5’-Deoxy-5’-iodo-2’-O-methyl-5-methyluridine 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: 187733-72-8
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMT-dC(bz) Phosphoramidite-13C9,15N3

DMT-dC(bz) Phosphoramidite-13C9,15N3 is the 13C and 15N labeled DMT-dC(bz) Phosphoramidite[1]. DMT-dC(bz) Phosphoramidite is typically used in the synthesis of DNA[2].

  • CAS Number: 2483830-14-2
  • MF: C3713C9H52N215N3O8P
  • MW: 845.82
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4,6-Diamino-1-(2-deoxy-beta-D-ribofuranosyl)-1H-pyrazolo[3,4-d]pyrimidine

4,6-Diamino-1-(2-deoxy-beta-D-ribofuranosyl)-1H-pyrazolo[3,4-d]pyrimidine is a pyrimidine nucleoside analog. Pyrimidine nucleoside analogs have a wide range of biochemical and anticancer activities. These include DNA synthesis inhibition, RNA synthesis inhibition, antiviral effects, and immunomodulatory effects[1].

  • CAS Number: 117818-23-2
  • MF: C10H16N6O3
  • MW: 268.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.1±0.1 g/cm3
  • Boiling Point: 717.7±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 387.8±35.7 °C

6-Hydroxy-DL-DOPA

6-Hydroxy-DOPA is a selective and effective allosteric inhibitor of the RAD52 ssDNA binding domain. 6-Hydroxy-DOPA can be used for the research of cancer[1].

  • CAS Number: 21373-30-8
  • MF: C9H11NO5
  • MW: 213.18700
  • Catalog: DNA/RNA Synthesis
  • Density: 1.606g/cm3
  • Boiling Point: 515.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 265.4ºC

2’-Deoxy-2’-fluoro-N3-(2S)-(2-amino-3-carbonyl] propyl-beta-D-arabinouridine

2’-Deoxy-2’-fluoro-N3-(2S)-(2-amino-3-carbonyl] propyl-beta-D-arabinouridine 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: 2072145-25-4
  • MF: C13H18FN3O7
  • MW: 347.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-(N-PhenethylthiocarbaMoyl)-L-cysteine

S-(N-PhenethylthiocarbaMoyl)-L-cysteine, a anticarcinogenic agent, has antileukaemic activity with a GC50 value of 336 nM. S-(N-PhenethylthiocarbaMoyl)-L-cysteine inhibits DNA synthesis in HL60 cells [1].

  • CAS Number: 53330-02-2
  • MF: C12H16N2O2S2
  • MW: 284.40
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

8beta,9alpha-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide

8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility[1].

  • CAS Number: 956707-04-3
  • MF: C15H18O4
  • MW: 262.301
  • Catalog: LIM Kinase (LIMK)
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 465.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 178.6±22.2 °C

3'-O-TBDMS-dT

3’-O-t-Bulyldimethylsilylthymidine 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: 40733-27-5
  • MF: C16H28N2O5Si
  • MW: 356.49
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

hypoxanthine-9-beta-d-arabinofuranoside

Arabinosylhypoxanthine 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: 7013-16-3
  • MF: C10H12N4O5
  • MW: 268.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.08g/cm3
  • Boiling Point: 732.8ºC at 760 mmHg
  • Melting Point: 259-260 °C (lit.)
  • Flash Point: 397ºC

CHK1-IN-2

CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.

  • CAS Number: 912367-45-4
  • MF: C20H22N4OS
  • MW: 366.48
  • Catalog: Checkpoint Kinase (Chk)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5’-O-Acetyl-2’,3’-dideoxy-2’,3’-didehydro-5-fluoro-uridine

5’-O-Acetyl-2’,3’-dideoxy-2’,3’-didehydro-5-fluoro-uridine 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: 160203-74-7
  • MF: C11H11FN2O5
  • MW: 270.21
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Xanthopterin Hydrate

Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm[2]. Xanthopterin hydrate(XPT) causes renal growth and hypertrophy in rat[1].Xanthopterin hydrate inhibits RNA synthesis[4].

  • CAS Number: 5979-01-1
  • MF: C6H7N5O3
  • MW: 197.15100
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: 458.7ºC at 760 mmHg
  • Melting Point: >300 °C(lit.)
  • Flash Point: 231.2ºC

Exoenzyme C3, clostridium botulinum

Exoenzyme C3, clostridium botulinum is a promising agent to inactivate RhoA in neurons due to preventing the detrimental effect of active Rho in the recovery of injured neuronal systems. Exoenzyme C3, clostridium botulinum is used for the study of post-traumatic neuro-regeneration[1].

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

Cdc7-IN-8

Cdc7-IN-8 is a potent inhibitor of Cdc7. Cdc7 is a serine/threonine kinase which activates MCM promotion by phosphorylating the microchromosome maintenance protein (MCM protein), an important element of the DNA replication initiator. Cdc7-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021032170A1, compound 1-1/1-2)[1].

  • CAS Number: 2606780-38-3
  • MF: C19H21N5O2
  • MW: 351.40
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N4-BENZOYL-3'-DEOXYCYTIDINE

N4-Benzoyl-3’-deoxycytidine 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: 161110-00-5
  • MF: C16H17N3O5
  • MW: 331.32
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.503 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Deoxy-2’-fluoroisocytidine

2-Deoxy-2’-fluoroisocytidine 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: 1668560-65-3
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BChE/HDAC6-IN-1

BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research[1].

  • CAS Number: 2925457-27-6
  • MF: C34H43N5O5
  • MW: 601.74
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

sulfo-DGN462 sodium

sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML)[1].

  • CAS Number: 1401203-09-5
  • MF: C53H60N5NaO12S2
  • MW: 1046.19
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MMAF

MMAF (Monomethylauristatin F) is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.

  • CAS Number: 745017-94-1
  • MF: C39H65N5O8
  • MW: 731.962
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 896.8±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 496.2±34.3 °C

[5'-O-(4,4'-dimethoxytriphenylmethyl)-2'-O-(2-methoxyethyl)-N6-benzoyladenosin-3'-O-yl]-2-cyanoethyl-N,N-diisopropylphosphoramidite

DMT-2'O-MOE-rG(ib) Phosphoramidite (1g), belonging to the amide family of trivalent phosphate H3PO3, is a derivative of nucleotides and guanosine and can be used in the stereochemical synthesis of phosphorothioate oligonucleotides[1].

  • CAS Number: 251647-55-9
  • MF: C47H60N7O10P
  • MW: 913.99400
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-28

Tubulin polymerization-IN-28 (compound-4) is a microtubule protein polymerization inhibitor with highly selective anticancer activity. Tubulin polymerization-IN-28 can be activated by NQO1 and effectively release combretastatin A-4 to kill tumor cells. Tubulin polymerization-IN-28 can induce cell apoptosis and be used in anti-cancer research[1].

  • CAS Number: 2481404-89-9
  • MF: C37H46N2O9
  • MW: 662.77
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JG-231

JG-231 is an allosteric inhibitor that disrupts the Hsp70-BAG3 interaction (Ki=0.11 uM), inhibits breast cancer cells MCF-7 and MDA-MB-231 with IC50 of 0.12 and 0.25 uM, respectively; reduces tumor burden in an MDA-MB-231 xenograft model (4 mg/kg, ip).

  • CAS Number: 1627126-59-3
  • MF: C22H18BrCl2N3OS4
  • MW: 619.45
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-O-Methyluridine

3’-O-Methyluridine 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: 6038-59-1
  • MF: C10H14N2O6
  • MW: 258.23
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.53g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A