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PhysioProcesses

Cancer

Cancer is a collection of related genetic diseases that cause cells to divide uncontrollably and spread to surrounding tissues. Phenotypic changes to cancer cells include abnormal shape, fast rate of division, high metabolic rate, and invasion of surrounding tissues. The aberrant genes that lead to cancer can arise from DNA damage caused by environmental sources, errors that occur during cell division, or inherited. Tumor promoting genetic mutations occur in oncogenes that activate pathways related to cell proliferation or inactivate cell death pathways. Mutations in tumor suppressor genes lead to loss of function in growth inhibition, DNA damage repair, and apoptosis activation pathways.

Angiogenesis

Vandetanib | VEGFR2 inhibitor

CAS:
443913-73-3
Catalog Number:
10-2185
Activity:
VEGFR2 inhibitor
Chemical Names:
4-(4-Bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-yl)methoxy]quinazoline
Alternate Name:
ZD6474
Molecular Weight:
475.35
Molecular Formula:
C22H24BrFN4O2
Solubility:
Soluble in DMSO (30 mg/ml); Ethanol (10 mg/ml with warming)
Physical Properties:
White to off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Lycorine HCl | Protein synthesis inhibitor/SCAP degrader

CAS:
2188-68-3
Catalog Number:
10-2608
Activity:
Protein synthesis inhibitor/SCAP degrader
Chemical Names:
Galanthidine; Amarylline; Narcissine
Molecular Weight:
323.77
Molecular Formula:
C16H17NO4·HCl
Solubility:
Soluble in water (15 mg/ml)
Physical Properties:
White to off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in water may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Autophagy

PF-543 HCl | Sphingosine kinase-1 inhibitor

PF-543 (1706522-79-3) is a potent (IC50 = 2.0 nM) and selective (>100-fold over SphK2) reversible inhibitor of sphingosine kinase-1 (SphK1).1 It induced autophagy in head and neck squamous

Vacuolin-1 | Autophagy/PIKfyve inhibitor

Vacuolin-1 (351986-85-1) inhibits autophagy via inhibition of Ca2+-dependent fusion of lysosomes with the plasma membrane and the release of lysosomal content and has no effect on

Verteporfen | YAP Inhibitor

CAS:
129497-78-5
Catalog Number:
10-3487
Activity:
YAP inhibitor
Chemical Name:

(4R,4aS)-18-Ethenyl-4,4a-dihydro-3,4-bis(methoxycarbonyl)-4a,8,14,19-tetramethyl-24H,26H-benzo[b]porphine-9,13-dipropanoic acid monomethyl ester

Alternate Names:
CL 318952; BPD-MA
Molecular Weight:
718.79
Molecular Formula:
C41H42N4O8
Solubility:
Soluble in DMSO (up to 14 mg/ml)
Physical Properties:
Black solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchsae as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Cancer cell metabolism

HC-258 | Covalent TEAD inhibitor

HC-258 is a covalent inhibitor of TEAD (transcriptional enhanced associate domain), an important component of the Hippo pathway.  It was able to reduce gene expression levels

Cancer Stem Cells

STF-118804 | NAMPT inhibitor

STF-118804 (894187-61-2) is a potent and selective next generation inhibitor of nicotinamide phosphoribosyl transferase (NAMPT), inhibiting NAD+ biosynthesis from nicotinamide.1 It reduced the viability of most B-ALL cells

CBL0137 | Inhibitor of the histone chaperone FACT

CBL0137 (1197996-80-7) is an anticancer agent that activates p53 and suppresses NF-kB via trapping of the FACT (facilitates chromatin transcription) complex, an important histone chaperone that mediates nucleosome

Sulconazole | Antifungal/ Prevents cancer stem cell formation

CAS:
61318-91-0
Catalog Number:
10-3955
Activity:
Antifungal/Prevents cancer stem cell formation
Chemical Names:
1-[2-[(4-Chlorophenyl)methylsulfanyl]-2-(2,4-dichlorophenyl)ethyl]imidazole nitrate
Molecular Weight:
460.75
Molecular Formula:
C18H15Cl3N2S·HNO3
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
White solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Cell Cycle

WM-1119 | HAT KAT6A inhibitor

WM-1119 (2055397-28-7) is a potent and selective inhibitor of the MYST family histone acetyltransferase (HAT) KAT6A (MOZ) – IC50 = 6.3 nM.1,2 Induces cell cycle exit and cellular

SU9516 | pan-specific CDK inhibitor

CAS:
SU9516
Catalog Number:
10-5705
Activity:
pan-specific CDK inhibitor
Chemical Names:
(Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-2-one
Molecular Weight:
241.25
Molecular Formula:
C13H11N3O2
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
Orange solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

NG52 | Phosphoglycerate kinase 1 inhibitor

CAS:
212779-48-1
Catalog Number:
10-4681
Activity:
Phosphoglycerate kinase 1 inhibitor
Chemical Names:
2-[[6-(3-Chloroanilino)-9-propan-2-ylpurin-2-yl]amino]ethanol
Molecular Weight:
346.82
Molecular Formula:
C16H19ClN6O
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Cellular Stress

Honokiol-DCA | TRAP1 Inhibitor

Honokiol-DCA (HDCA; 1620160-42-0), a synthetic bis-dichloroacetate ester of the natural product honokiol, is an allosteric inhibitor of the mitochondrial chaperone TRAP1.1 It binds to an allosteric site

Luminespib | HSP90 inhibitor

CAS:
747412-49-3
Catalog Number:
10-4672
Activity:
HSP90 inhibitor
Chemical Names:
5-(2,4-Dihydroxy-5-propan-2-ylphenyl)-N-ethyl-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxamide
Alternate Name:
NVP-AUY922; VER-52296
Molecular Weight:
465.54
Molecular Formula:
C26H31N3O5
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

C-DIM 8 | Nur77 Antagonist

CAS:
151358-47-3
Catalog Number:
10-5157
Activity:
Nur77 antagonist
Chemical Names:
1,1-Bis(3’-indolyl)-1-(p-hydroxyphenyl)methane
Alternate Name:
DIM-C-pPhOH
Molecular Weight:
338.41
Molecular Formula:
C23H18N2O
Solubility:
Soluble in DMSO (35 mg/ml); ethanol (35 mg/ml)
Physical Properties:
Pink solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Chemotherapeutics

Raltitrexed | Thymidylate synthase inhibitor

Raltitrexed (112887-68-0) is an inhibitor of thymidylate synthase with significantly increased potency in many cancer cell lines when compared with 5-fluorouracil.1,2  It is also an inhibitor

MRTX849 | Covalent KRASG12C Inhibitor

MRTX849 (2326521-71-3) is a potent (IC50’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRASG12C inhibitor.1 It showed pronounced

Cytoskeleton

Cytochalasin B | Actin filament disrupting agent

CAS:
14930-96-2
Catalog Number:
10-2069
Activity:
Actin filament disrupting agent
Fermentation product:
from Drechslera dematioidea
Alternate Name:
NSC107658; Phominone
Molecular Weight:
479.61
Molecular Formula:
C29H37NO5
Solubility:
Soluble in DMSO (up to 5 mg/ml); Ethanol (10 mg/ml)
Physical Properties:
White solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Buparlisib | PI3-kinase inhibitor

CAS:
944396-07-0
Catalog Number:
10-4325
Activity:
pan-Class I PI3-kinase inhibitor
Chemical Names:
5-(2,6-Dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridine-2-amine; NVP-BKM120
Molecular Weight:
410.39
Molecular Formula:
C18H21F3N6O2
Solubility:
Soluble in DMSO (15 mg/ml)
Physical Properties:
White solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

DNA Damage/Repair

AOH1996 | PCNA inhibitor

AOH1996 (2089314-64-5) inhibits proliferating cell nuclear antigen (PCNA), an enzyme critical to DNA replication and repair processes.1  It enhances the interaction between PCNA and RPB1 subunit

TH10785 | OGG1 activator

TH10785 (1002801-51-5) is an 8-oxo guanine DNA glycosylase 1 (OGG1) activator. Oxidative DNA damage is recognized by OGG1 which then excises 8-oxoguanine, leaving a substrate for

Ochratoxin A | Mycotoxin

Ochratoxin A (303-47-9) is a mycotoxin that causes widespread contamination in foodstuffs and environments thus causing health risks to humans and animals.1 It has been shown to

Drug resistance

JNK-IN-8 | Covalent JNK inhibitor

JNK-IN-8 (1410880-22-6) is a  potent and selective irreversible JNK inhibitor (IC50s=4.67, 18.7 and 0.98 nM for JNK1, 2 and 3 respectively).1  JNK blockade with JNK-IN-8 overcomes

S07-2010 | pan-AKR1C inhibitor

S07-2010 (1223194-71-5) is a pan-aldo-keto reductase 1C (AKR1C) inhibitor (IC50’s for AKR1C isoforms: 1C1 = 470 nM, 1C2 = 730 nM, 1C3 = 190 nM, 1C4

Epigenetics

BRM014 | BRM/BRG1 ATPase inhibitor

SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as Brahma homologue (BRM), together with its close homologue Brahma-related gene 1 (BRG1),

WM-1119 | HAT KAT6A inhibitor

WM-1119 (2055397-28-7) is a potent and selective inhibitor of the MYST family histone acetyltransferase (HAT) KAT6A (MOZ) – IC50 = 6.3 nM.1,2 Induces cell cycle exit and cellular

Gene Regulation/Transcription

HC-258 | Covalent TEAD inhibitor

HC-258 is a covalent inhibitor of TEAD (transcriptional enhanced associate domain), an important component of the Hippo pathway.  It was able to reduce gene expression levels

BRM014 | BRM/BRG1 ATPase inhibitor

SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as Brahma homologue (BRM), together with its close homologue Brahma-related gene 1 (BRG1),

AOH1996 | PCNA inhibitor

AOH1996 (2089314-64-5) inhibits proliferating cell nuclear antigen (PCNA), an enzyme critical to DNA replication and repair processes.1  It enhances the interaction between PCNA and RPB1 subunit

Growth factors

MRTX849 | Covalent KRASG12C Inhibitor

MRTX849 (2326521-71-3) is a potent (IC50’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRASG12C inhibitor.1 It showed pronounced

Immuno-oncology

LDC1267 | Inhibitor of TAM kinases

LDC1267 (1361030-48-9) is a potent and selective inhibitor of the TAM kinases Tyro3, Axl, and Mer (IC50s respectively: 8 nM, <5 nM, 29 nM).1 It was

Dubermatinib | AXL inhibitor

Dubermatinib (1341200-45-0) is a potent (IC50 = 27 nM) inhibitor of the TAM family kinase AXL.1 It displayed potent activity against the pancreatic tumor cell line PSN-1 (IC50 =

Kinases

JNK-IN-8 | Covalent JNK inhibitor

JNK-IN-8 (1410880-22-6) is a  potent and selective irreversible JNK inhibitor (IC50s=4.67, 18.7 and 0.98 nM for JNK1, 2 and 3 respectively).1  JNK blockade with JNK-IN-8 overcomes

LDC1267 | Inhibitor of TAM kinases

LDC1267 (1361030-48-9) is a potent and selective inhibitor of the TAM kinases Tyro3, Axl, and Mer (IC50s respectively: 8 nM, <5 nM, 29 nM).1 It was

Metastasis

Decoyinine | Inhibitor of GMP synthase

Decoyinine (2004-04-8) is a non-competitive and reversible inhibitor of GMP synthase (GMPS, IC50=17.3 µM).1  GMPS was shown to be a positive regulator of invasiveness in melanoma

P053 | Protein phosphatase 5 inhibitor

P053 (1022417-69-1) is a selective inhibitor of protein phosphatase 5 (PP5) – IC50 = 706 nM.1  PP5 regulates signaling cascades that are responsible for tumor initiation,

C-DIM 8 | Nur77 Antagonist

CAS:
151358-47-3
Catalog Number:
10-5157
Activity:
Nur77 antagonist
Chemical Names:
1,1-Bis(3’-indolyl)-1-(p-hydroxyphenyl)methane
Alternate Name:
DIM-C-pPhOH
Molecular Weight:
338.41
Molecular Formula:
C23H18N2O
Solubility:
Soluble in DMSO (35 mg/ml); ethanol (35 mg/ml)
Physical Properties:
Pink solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

p53 and other tumor suppressors

SR1078 | ROR agonist

SR1078 (1246525-60-9) is an agonist of the orphan nuclear receptors RORα and RORγ.1 It attenuated intrapancreatic pathological changes in mouse models of chronic pancreatitis via restoration of the circadian

CBL0137 | Inhibitor of the histone chaperone FACT

CBL0137 (1197996-80-7) is an anticancer agent that activates p53 and suppresses NF-kB via trapping of the FACT (facilitates chromatin transcription) complex, an important histone chaperone that mediates nucleosome

Programmed cell death

P053 | Protein phosphatase 5 inhibitor

P053 (1022417-69-1) is a selective inhibitor of protein phosphatase 5 (PP5) – IC50 = 706 nM.1  PP5 regulates signaling cascades that are responsible for tumor initiation,

Ubiquitin proteasome

Indisulam | RBM39 Molecular glue

Indisulam (165668-41-7) was originally described as a potent antitumor agent that targeted the G1 phase of cell cycle via suppression of activation of CDK2 and cyclin

Other Cancer

Decoyinine | Inhibitor of GMP synthase

Decoyinine (2004-04-8) is a non-competitive and reversible inhibitor of GMP synthase (GMPS, IC50=17.3 µM).1  GMPS was shown to be a positive regulator of invasiveness in melanoma