Structure of KN-93
CAS No.: 139298-40-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
KN-93 is a potent Ca2+/calmodulin-dependent protein kinase II (CaMKII) selective inhibitor with Ki of 370 nM.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 139298-40-1 |
Formula : | C26H29ClN2O4S |
M.W : | 501.04 |
SMILES Code : | O=S(C1=CC=C(OC)C=C1)(N(C2=CC=CC=C2CN(CC=CC3=CC=C(Cl)C=C3)C)CCO)=O |
MDL No. : | MFCD00236424 |
InChI Key : | LLLQTDSSHZREGW-AATRIKPKSA-N |
Pubchem ID : | 5312122 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H312-H332 |
Precautionary Statements: | P280 |
Target |
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In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
BAP1-KO MeT-5A cells | 7.5 µM | 48 h | KN-93 significantly induced apoptosis in BAP1-KO cells by increasing intracellular Ca2+ concentration and inhibiting CAMK2D activity. | PMC10362017 |
BAP1-KO HOMC-D4 cells | 7.5 µM | 48 h | KN-93 significantly induced apoptosis in BAP1-KO cells by increasing intracellular Ca2+ concentration and inhibiting CAMK2D activity. | PMC10362017 |
Y-MESO-9 cells | 7.5 µM | 48 h | KN-93 significantly induced apoptosis in BAP1-KO cells by increasing intracellular Ca2+ concentration and inhibiting CAMK2D activity. | PMC10362017 |
Human AC-16 cardiomyocytes | 50 μM | 1 h | Pre-treatment with KN-93 reduced doxorubicin-induced ROS generation and cell death in RGS11 knockout AC-16 cells. | PMC9557029 |
U251 cells | 10 µM | 15 min | Inhibition of CaMKII activity, reducing MLC1 protein phosphorylation | PMC9454758 |
Mouse astrocytes | 10 µM | 15 min | Inhibition of CaMKII activity, reducing MLC1 protein dimerization | PMC9454758 |
HEK293 cells | 10 μM | 14 h | To investigate the inhibitory effect of KN-93 on CaMKII, it was found that KN-93 aggravated the accumulation of ubiquitinated proteins. | PMC11466968 |
HeLa cells | 10 μM | 14 h | To investigate the inhibitory effect of KN-93 on CaMKII, it was found that KN-93 aggravated the accumulation of ubiquitinated proteins. | PMC11466968 |
HEK293T cells | 10 μM | 4 h | To screen the upstream kinase for PRMT6 | PMC7979509 |
NRVM (neonatal rat ventricular myocytes) | 10 μM | 24 h | KN-93 treatment significantly reduced the p-CaMKII levels in PRMT1-depleted cells, restored cell size, and attenuated the increase in ANP and β-MHC gene expression. | PMC6269446 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | LPS-induced acute lung injury model | Intraperitoneal injection | 10mg/kg | The first injection was performed 2h before LPS administration, followed by injections every 24h for 48h. | KN-93 suppressed the phosphorylation of CaMK4 and significantly inhibited NLRP3 inflammasome activation, leading to reduced IL-1β and IL-18 production, and ameliorated LPS-induced acute lung injury. | PMC9207179 |
SCID mice | BAP1-KO Y-MESO-9 xenograft model | intraperitoneal injection | 15 mg/kg | Administered on days 0, 4, 8,13, and 16, lasting 16 days | KN-93 significantly suppressed tumor growth of BAP1-KO Y-MESO-9 cells without causing weight loss and inhibited tumor growth by promoting apoptosis. | PMC10362017 |
Mice | Diabetic myocardial ischemia model | Direct injection into the left ventricle | 300 μg/kg | Single dose 10 minutes before surgery | KN-93 significantly increased the concentration levels of circulating myocardial enzymes and infarct size in DM hearts, decreased the release of CGRP, attenuated the recovery of cardiac function, and increased the interstitial fibrosis area, indicating that CaMKII plays an important role in PF-mediated cardioprotection. | PMC4888521 |
Mice | Isoflurane anesthesia model | Intracerebroventricular injection | 1 mM | Single injection, lasting 7 days | KN93 significantly diminished the protective effect of GLYX-13 on cognitive function and NR2B, CaMKII, and CREB levels, indicating that GLYX-13 ameliorates isoflurane-induced cognitive dysfunction via the NR2B/CaMKII/CREB signaling pathway. | PMC6862406 |
Mice | Chronic doxorubicin-induced cardiotoxicity model | Intraperitoneal injection | 8 mg/kg | Every 4 days, total of 2 doses | KN-93 treatment significantly alleviated cardiac fibrosis in RGS11 knockdown mice. | PMC9557029 |
Nude mice | MDA-MB-231 xenograft model | Intraperitoneal injection | 10 mg/kg | Once every three days for 12 days | To investigate the anti-tumor efficacy of KN-93 in combination with proteasome inhibitors, it was found that the combination significantly enhanced anti-tumor activity. | PMC11466968 |
Mice | Cardiac-specific PRMT1 knockout mice | Intraperitoneal injection | 10 μM/kg | Once daily for 8 days | KN-93 treatment improved cardiac function in PRMT1-deficient mice, reduced left ventricular dilation and fibrosis, and decreased the expression of ANP and BNP. | PMC6269446 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.00mL 0.40mL 0.20mL |
9.98mL 2.00mL 1.00mL |
19.96mL 3.99mL 2.00mL |
Tags: KN-93 | KN93 | KN 93 | CaMK | Calmodulin-dependent protein kinases | Calmodulin-dependent kinases | CaMKII inhibitor | calcium signaling | synaptic plasticity | cardiovascular diseases | neuronal function | calmodulin-dependent protein kinase II | cell-permeable | synaptic plasticity | Ca2+dependent protein kinase II | 139298-40-1
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Response | |
Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
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P341 | If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P342 | If experiencing respiratory symptoms: |
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P376 | Stop leak if safe to do so. Oxidising gases (section 2.4) 1 |
P377 | Leaking gas fire: Do not extinguish, unless leak can be stopped safely. |
P378 | |
P380 | Evacuate area. |
P381 | Eliminate all ignition sources if safe to do so. |
P390 | Absorb spillage to prevent material damage. |
P391 | Collect spillage. Hazardous to the aquatic environment |
P301 + P310 | IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
P370 + P378 | In case of fire: |
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H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
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H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
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Health hazards | |
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H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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